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LECTURE No. 1. General provisions

1. Introduction. The subject of pharmacology, its history and tasks

Pharmacology - the science of the action of medicinal substances on living organisms and the ways of finding new drugs. It is one of the most ancient sciences. It is known that in ancient Greece (XNUMXrd century BC), Hippocrates used various medicinal plants to treat diseases. In the XNUMXnd century n. e. Roman physician Claudius Galen widely used various extracts from medicinal plants in medical practice. The famous physician of the Middle Ages Abu Ali ibn Sina (Avicenna) in his writings mentions a large number of herbal medicines (camphor, preparations of henbane, rhubarb, ergot, etc.). XV-XVI centuries - Paracelsus uses in medical practice already inorganic medicinal substances: compounds of iron, mercury, lead, copper, arsenic, sulfur, antimony. Experimental research methods are gradually being developed, thanks to which it has become possible to obtain pure high-quality substances (papaverine, strychnine, etc.) and synthetic compounds from plants. Of great importance were the reforms of Peter I, which served as the beginning of the emergence of the pharmaceutical industry in Russia.

At the end of the XNUMXth - beginning of the XNUMXth centuries. The first manuals on medication management appeared, written in Russia by N. M. Maksimovich-Ambodik and A. P. Nelyubin. The development of pharmacology was facilitated by the achievements of chemistry and physiology in the XNUMXth century. Pharmacological laboratories were opened. Clinicians N.I. Pirogov and A.M. Filomafitsky showed a certain interest in experimental pharmacology. They experimentally studied the effect of the first narcotic drugs - ether and chloroform - on the body of animals. I. P. Pavlov’s research in the field of physiology of the cardiovascular system and his teaching on conditioned reflexes were of great importance for the development of pharmacology.

Under his leadership and with direct participation in the clinic of S. P. Botkin, many medicinal plants (Adonis, lily of the valley, strophanthus, etc.) were investigated.

In addition, I. P. Pavlov created a large school of domestic pharmacologists. After I. P. Pavlov, the department was headed by N. P. Kravkov, and both of them are the founders of modern domestic pharmacology. Studying the action of medicinal substances in conditions of artificially induced pathological conditions, N. P. Kravkov created a new direction in the development of experimental pharmacology. His use of non-volatile narcotic substances as basic drugs formed the basis of modern principles of pain relief. A great contribution to the further development of domestic pharmacology was made by many students and followers of N. P. Kravkov: M. P. Nikolaev, A. I. Kuznetsov, N. V. Vershinin, S. V. Anichkov, A. I. Cherkes, academicians V V. Zakusov, M. D. Mashkovsky, A. V. Valdman, professors D. A. Kharkevich, A. N. Kudrin, etc. They created new schools and directions of national pharmacology and enriched it with fundamental works.

2. Clinical pharmacology, its tasks. Types of pharmacotherapy

Clinical Pharmacology - a science that studies the effect of drugs on the body of a sick person.

Her tasks:

1) testing of new pharmacological agents;

2) development of methods for the most effective and safe use of drugs;

3) clinical trials and re-evaluation of old drugs;

4) information support and advisory assistance to medical workers.

Resolves issues such as:

1) the choice of a medicinal product for the treatment of a particular patient;

2) determination of the most rational dosage forms and the mode of their application;

3) determination of the route of administration of the medicinal substance;

4) monitoring the effect of the medicinal product;

5) prevention and elimination of adverse drug reactions.

Clinical pharmacology is closely related to various fields of medicine and biology. Pharmacodynamics and pharmacokinetics are the main branches of clinical pharmacology.

Pharmacodynamics studies the totality of the effects of a medicinal substance and the mechanisms of its action.

Pharmacokinetics - ways of receipt, distribution, biotransformation and excretion of drugs from the human body.

Pharmacotherapy - the science of the use of medicinal substances for therapeutic purposes. The following types of pharmacotherapy are distinguished: etiotropic, pathogenetic, symptomatic, substitution and prophylactic.

Etiotropic therapy aimed at eliminating the cause (etiology) of the disease.

pathogenetic directs the action of drugs to eliminate or suppress the mechanisms of disease development.

Symptomatic therapy eliminates or reduces individual symptoms of the disease.

Replacement therapy It is used when there is a deficiency in the patient’s body of biologically active substances - hormones, enzymes, etc.

Preventive therapy carried out to prevent diseases.

LECTURE No. 2. Dosage forms

1. The concept of drugs. Recipe, rules for its design

Sweet Pill A substance used to treat or prevent a disease.

Medicinal substance is a single substance or a mixture of substances of natural or synthetic origin.

Medicinal preparation is a drug in ready-to-use form.

Dosage form - This is a medicinal substance in the most convenient form for taking by patients.

All medicines are divided into three groups:

1) list A (Venena - poisons);

2) list B (heroica - potent);

3) medicines dispensed without a doctor's prescription.

Recipe - this is an appeal from a doctor to a pharmacist about dispensing medicines to a patient, indicating the dosage form, dose and method of administration. It is a medical, legal and monetary document in the case of free or preferential dispensing of medicines.

Prescription and dispensing of medicines on them is carried out in accordance with the requirements of the Order of the Ministry of Health of August 23, 1999 No. 328 "On the rational prescription of medicines, the rules for writing prescriptions for them and the procedure for their dispensing by pharmacies (organizations) and the order of the Ministry of Health of Russia of November 12, 1997 . No. 330".

Dose expressed in mass or volume units of the decimal system and denoted by Arabic numerals. The number of whole grams is separated by a comma (1,0). More often used: 0,1 - one decigram; 0,01 - one centigram; 1,001 is one milligram. The drops that make up the medicine are designated by a Roman numeral, preceded by gtts. The biological units of action in the recipe thus indicate 500 units.

Liquid substances in recipes are indicated in ml (0,1 ml). The recipe is certified by a signature and a personal seal. The prescription must indicate: the age of the patient, the date of issue of the prescription, the patient's surname and initials; surname and initials of the doctor, the procedure for paying for the medicine. Moreover, preferential prescriptions are issued on special forms with a stamp and seal.

On special forms of a different sample, drugs from the list of narcotic substances, hypnotics, anorexigenic drugs are also prescribed.

Moreover, the prescription is written by the doctor himself, puts his signature and certifies with a personal seal. In addition, it is signed by the chief physician or his deputy, the prescription has a round seal and a stamp of the medical institution.

The same order of prescribing is defined for anabolic drugs, as well as phenobarbital, cyclodol, ephedrine hydrochloride, clonidine (eye drops, ampoules), sunoref ointment. Antipsychotics, tranquilizers, antidepressants, preparations containing ethyl alcohol, etc. are prescribed on other forms of prescription forms.

It is forbidden to prescribe ether for anesthesia, chloroethyl, fentanyl, sombrevin, ketamine to outpatients. The prescription begins with the word Recipe (Rp. - abbreviated), which means "take", then the names and quantities of prescribed medicinal substances are listed in the genitive case. First called the main, then auxiliary.

Next, the required dosage form is indicated. For example, Misce ut fiat pulvis (M. f. pulvis) - “mix to make a powder.”

For those who are dosed they write: “Da tales doses numero 10” - “give out such doses in number 10.” At the end of the recipe, after the word Signa (S) - “designate” in Russian (or national) language, indicate the method of using the medicine.

A prescription for narcotic and poisonous drugs is valid for 5 days; for ethyl alcohol - 10 days; for all others - up to 2 months from the date of discharge.

Dosages of medications are written taking into account age characteristics. Higher doses for adults over 25 years of age. Over 60 years old - 1/2 of adult age. Up to a year - 1/24 - 1/12 - dose for an adult.

2. Solid dosage forms

Solid dosage forms include tablets, dragees, powders, capsules, granules, etc. Pills (Tabulette, Tab.) is obtained by pressing a mixture of drug and excipient. Distinguish between simple and complex composition.

1. Rp.: Tab. Analgini 0,5 No. 10

DS 1 tablet 2-3 times a day.

2. Rp.: Amidopyrini

Butadioni a.a. 0,125

No. 20 in tab.

S. 1 tablet 3 times a day (after meals).

dragee (Dragee) is made by layering drugs and excipients on granules.

Rp.: Nitroxolini 0,05

D. td no. 50 in dragee

S. 2 tablets 4 times a day with meals.

Powders (Pulveres, Pulv.) are intended for internal, external or injection (after dissolution) use. There are undosed, simple and complex powders, including powders, and dosed, simple and complex powders.

The mass of the dosed powder should be 0,1-1,0. At a dose of less than 0,1, indifferent substances are added to the composition, most often sugar (Saccharum).

Volatile, hygroscopic dosed powders are dispensed in special paper (waxed, waxed or parchment) and the recipe indicates: D. td No. 20 in charta (paraffinata, pergaminata).

1. Rp.: Streptocidi 10,0

DS For dressing wounds.

2.Rp.: Pul. foliorum Digitalis 0,05

D. td No. 30

S. 1 powder 2 times a day.

Capsules (Capsulae) - gelatin shells, which include dosed powdered, granular, pasty, semi-liquid and liquid medicinal substances.

Rp.: Olei Ricini 1,0

D. td No. 30 in capsules gelatinosis

S. 1 capsule per dose.

Granules (Granulae) is a solid dosage form in the form of particles 0,2-0,3 mm in size, intended for oral administration.

The composition of the granules includes both medicinal and excipients.

Rp.: Granulum urodani 100,0

S. 1 tsp. 4 times a day (before meals, in 0,5 cups of water).

In addition, there are films и records (Membranulae et Lamellae) - special solid dosage forms that contain medicinal substances on a polymer basis; glossets (Glossetes) - small tablets intended for sublingual or buccal use; caramel (Caramela) are prepared in the form of sweets containing sugar and molasses.

Used to treat oral diseases poultices (Cataplasmata) - semi-solid drugs that have anti-inflammatory and antiseptic effects.

Soluble tablets (Solvellenae) are dissolved in water. The solution is applied externally (for example, furacilin tablets).

3. Liquid dosage forms

These include solutions, herbal and novogalenic preparations, dispersed systems, etc.

solutions (Solutiones, Sol.) is obtained by dissolving drugs in a solvent.

They can be written in expanded, abbreviated or semi-abbreviated way.

Concentration in an abbreviated form is expressed as a percentage or as a ratio of mass and volume. Distinguish between aqueous and alcoholic solutions.

1. Rp.: Natrii bromidi 3% - 200 ml

DS 10 drops 2 times a day with meals.

2. Rp.: Sol. Ergocalciferoli spirituosae 0,5% - 10 ml

DS 1 tbsp. l. 3 times a day.

Herbal preparations - these are extracts from plant materials obtained by heating or dissolving the corresponding extracts. Water or alcohol is used as a solvent.

Infusions (Infusa, Inf.) and broths (Decocta, Dec.) are aqueous extracts from the dry parts of medicinal plants.

Rp.: Inf. herbae Leonuri 15,0: 200 ml

DS 1 tbsp. l. 1-4 times a day.

Tinctures (Tincturae, T-rae) and extracts (Extracta, Extr.) - alcohol (alcohol-water or alcohol-ether) extracts from medicinal raw materials without heating.

Rp.: T-rae Leonuri 3% - 200 ml

T-rae Valerianae 10ml

MDS 1 tbsp. l. 3 times a day.

Extracts (Extractum, Extr.). There are liquid, thick and dry extracts.

Rep.: Extr. Eleutherococci fluidi 50 ml

DS 40 drops 2 times a day (30 minutes before meals).

Novogalenic preparations obtained as a result of special testing with a high degree of purification of drugs (Adonisidum).

Disperse systems There are systems where the dispersion medium is liquid (water, oil, gas, etc.), and the dispersed phase is insoluble small particles. These are suspensions, aerosols, mixtures.

Liquid dosage forms also include applications, balms, collodions, creams, soft drinks, syrups. Applications (Applications) - liquid or ointment-like preparations used for application to the skin for therapeutic purposes.

Balms (Balsama) - liquids obtained from plants and having an aromatic odor, antiseptic and deodorizing properties.

Rp.: Balsami contra tussim 30 ml

DS 10 drops 3 times a day.

collodions (Collodia) - solutions of nitrocellulose in alcohol with ether (1: 6), containing medicinal substances. Applied externally.

Creams (Cremores) - semi-liquid preparations containing drugs, oils, fats and other substances, but less viscous than ointments.

Lemonade (Limonata) - sweet-tasting liquids or acidified for oral administration. Syrups (Sirupi) - thick, clear, sweet liquids for oral administration.

4. Dosage forms for injections. Soft dosage forms

Dosage forms for injection include sterile aqueous and oily solutions. Distinguish between simple and complex composition.

Rp.: Sol. Glucosi 5% - 500 ml;

Rp.: Sol. Camphorae oleosae 20% - 2 ml

Steril! D. td No. 10 in amp.

DS drip

Solutions in ampoules, having a code name, but different from the dissolved drug.

Rp.: Cordiamini 2 ml

D. td No. 10 in amp.

S. Under the skin - 2 ml 2 times a day.

К soft dosage forms include ointments, pastes, liniments, suppositories, patches. Fats and fat-like substances obtained from oil, synthetic polymers are used as forming bases.

The bases of animal origin are pork fat, lanolin, spermaceti, yellow wax, vegetable oils, and substances from petroleum are petroleum jelly, petroleum jelly, refined petroleum (naftalan) and products from synthetic substances (polyethylene glycols or polyethylene oxide).

Ointment (Unguenta, Ung.) - a soft dosage form of a viscous consistency used for external use and containing less than 25% dry (powder) substances.

There are simple and complex in composition, in addition, they are divided into official simple in composition and official branded ones.

Simple:

Rp.: Ung. Tetracyclini hydrochloridi 1% - 3,0

DS Lay behind the eyelid 4 times a day.

Complex:

Rp.: Methyluracili 2,5

Furacilini 0,1

Vasellini

Lanolini aa 25,0

M.f. ung.

DS Apply to the wound.

Pastes (Pastae, Past.) contain at least 25% solids.

Rp.: Pastae Lassari 30,0

DS Apply to affected areas.

Liniments (Linimtnta, Lin.) - liquid ointments in which the dissolved substances are evenly distributed in a liquid ointment base. It is shaken before use. Candles (suppositories, Suppositoria, Supp.) - the dosage form is solid at room temperature, but melts at body temperature. According to the manufacturing method, there are pharmacy and factory; by method of application - rectal and vaginal. Bandages (Emplastra) - a dosage form in the form of a plastic mass that softens at body temperature and adheres to the skin.

LECTURE No. 3. Pharmacodynamics and pharmacokinetics

1. Types of action of medicinal substances

Pharmacodynamics is the study of the effect that drugs have on the body. The action of a substance at the site of its administration before absorption into the general circulation is called local action, while the reaction of the body can develop both at the injection site and away from it (for example, local anesthetic effect, astringent effect). The action of a substance after absorption and distribution throughout the body is called resorptive, or common. An example of such an effect is sleep that develops after taking sleeping pills. Under reflex action understand the effect that is realized as a result of a reflex that has arisen due to the effect of a medicinal substance on nerve receptors at the injection site or after absorption. For example, when ammonia is inhaled, respiratory excitation is observed. There are also direct and indirect effects, or primary and secondary reactions. Under direct, or primary, action is understood as the result of the direct influence of a substance on organs and tissues. Indirect, or secondary, reactions are the body's response to primary changes caused by a drug, but it is not always possible to distinguish between primary and secondary reactions. For example, the action of foxglove, a remedy for heart disease, is primary. It is not a diuretic and in a healthy person does not cause an increase in diuresis, but in a patient suffering from heart disease with tissue edema, improved blood circulation leads to a decrease in edema and increased fluid excretion by the kidneys. The diuretic effect of foxglove in this case will be secondary. Adverse events in the body caused by a medicinal substance are called side effects, which are of a serious nature, are called a complication. Side effects and complications are sometimes not detected with a single application, but may develop when taking the medication for a long time. If the drug acts on most cells and tissues in approximately the same way, then they talk about general cellular action of the substance (drugs, etc.). When a drug affects a limited group of cells, we are talking about selective (selective) action (analgesic effect of morphine). If the action of a medicinal substance passes without a trace after a certain time, then such an action is called reversible (for example, a narcotic action), otherwise the action is called irreversible (for example, cauterizing action).

2. Routes of drug administration

There are enteral and parenteral routes of drug administration. enteral route - the introduction of the drug inside through the mouth (per os), or orally; under the tongue (sub lingua), or sublingually; into the rectum (per rectum), or rectally.

Taking the drug through the mouth. Advantages: ease of use; comparative safety, absence of complications inherent in parenteral administration.

Disadvantages: slow development of the therapeutic effect, the presence of individual differences in the rate and completeness of absorption, the effect of food and other drugs on absorption, destruction in the lumen of the stomach and intestines (insulin, oxytocin) or when passing through the liver.

Take medicinal substances inside in the form of solutions, powders, tablets, capsules and pills.

Application under the tongue (sublingually). The drug enters the systemic circulation, bypassing the gastrointestinal tract and liver, starting to act after a short time.

Insertion into the rectum (rectal). A higher concentration of drugs is created than with oral administration.

Suppositories (suppositories) and liquids are administered using enemas. The disadvantages of this method: fluctuations in the speed and completeness of the absorption of drugs, characteristic of each individual, inconvenience in use, psychological difficulties.

parenteral route - different types of injections; inhalation; electrophoresis; surface application of drugs to the skin and mucous membranes.

Intravenous administration (in / in). Medicines are administered in the form of aqueous solutions.

Advantages: rapid entry into the blood, if a side effect occurs, it is possible to quickly stop the action; the possibility of using substances that are destroyed, non-absorbable from the gastrointestinal tract. Disadvantages: with prolonged intravenous administration along the vein, pain and vascular thrombosis may occur, the risk of infection with hepatitis B viruses and human immunodeficiency.

Intra-arterial administration (in / a). It is used in cases of diseases of certain organs (liver, limb vessels), creating a high concentration of the drug only in the corresponding organ.

Intramuscular administration (in / m). Aqueous, oily solutions and suspensions of medicinal substances are administered. The therapeutic effect occurs within 10-30 minutes. The volume of the injected substance should not exceed 10 ml.

Disadvantages: the possibility of the formation of local soreness and even abscesses, the danger of accidentally entering the needle into a blood vessel.

Subcutaneous administration. Enter water and oil solutions. Do not inject subcutaneously solutions of irritating substances that can cause tissue necrosis.

Inhalation. Gases (volatile anesthetics), powders (sodium cromoglycate), aerosols are administered in this way. Inhalation of an aerosol achieves a high concentration of a medicinal substance in the bronchi with a minimal systemic effect.

Intrathecal administration. The drug is injected directly into the subarachnoid space. Application: spinal anesthesia or the need to create a high concentration of a substance directly in the central nervous system.

Local application. To obtain a local effect, drugs are applied to the surface of the skin or mucous membranes.

Electrophoresis It is based on the transfer of medicinal substances from the surface of the skin to deep-lying tissues using galvanic current.

3. The mechanism of action of drugs

The action of most drugs is based on the process of influencing the physiological systems of the body, expressed by a change in the rate of natural processes. The following mechanisms of action of drugs are possible.

Physical and physico-chemical mechanisms. We are talking about a change in the permeability and other qualities of cell membranes due to the dissolution of a medicinal substance in them or its adsorption on the cell surface; about changes in the colloidal state of proteins, etc.

chemical mechanisms. The medicinal substance enters into a chemical reaction with the constituent parts of tissues or body fluids, while they act on specific receptors, enzymes, cell membranes or directly interact with cell substances.

Action on specific receptors is based primarily on the fact that macromolecular structures are selectively sensitive to certain chemical compounds. Drugs that increase the functional activity of receptors are called agonists, and drugs that interfere with the action of specific agonists - antagonists. Distinguish between competitive and non-competitive antagonism. In the first case, the drug substance competes with the natural mediator for junctions in specific receptors. Receptor blockade caused by a competitive antagonist can be reversed by high doses of the agonist or natural mediator.

Effect on enzyme activity due to the fact that some medicinal substances are able to increase and inhibit the activity of specific enzymes.

Physico-chemical effect on cell membranes (nervous and muscular) is associated with the flow of ions that determine the transmembrane electrical potential. Some drugs are able to change the transport of ions (antiarrhythmic drugs, anticonvulsants, general anesthesia drugs).

Direct chemical drug interaction possibly with small molecules or ions inside cells. The principle of direct chemical interaction is the basis of antidote therapy for chemical poisoning.

4. Doses of medicinal substances. The significance of the state of the body and external conditions for the action of the drug

There are threshold, therapeutic and toxic doses. For each substance, there is a minimum effective, or threshold, dose, below which the action is not shown. Doses above the threshold may be used for therapeutic purposes if they do not cause poisoning. These doses are called therapeutic. Doses that cause poisoning are called toxic; leading to death - lethal (from lat. letum - "death"). Breadth of therapeutic action called the range between the threshold and minimum toxic dose. The greater the breadth of the therapeutic action of the drug, the less the risk of toxic effects during treatment. Average therapeutic doses - these are the doses used in medical practice and giving a good therapeutic effect. For poisonous and potent drugs, special regulations of the State Pharmacopoeia Committee establish the so-called higher therapeutic doses (one-time and daily), abbreviated as V. R. D. and V. S. D. A pharmacist does not have the right to release a medicine in excess of these doses without a special order from a doctor. When dosing the drug, it is necessary to take into account the age and weight of the patient, a more accurate dose is calculated per 1 kg of body weight. It is known that the sensitivity of people to medicinal substances is very different. Idiosyncrasy - extremely high sensitivity to medicines. It can be congenital or the result of sensitization, i.e., the development of a sharp increase in sensitivity to the drug as a result of its use. There are large differences in the effect of drugs depending on age (adults and children), gender (for example, women are more sensitive to drugs than men, especially during the menstrual period and pregnancy). The human constitution is of great importance. Well-fed and calm people tolerate large doses of the drug better than lean and excitable people. Diet is essential. On an empty stomach, insulin acts more strongly than after a meal. With a lack of vitamin C in food, cardiac glycosides act much more strongly; protein starvation dramatically changes the body's reactivity to medicinal substances. External conditions also have a significant impact on the action of drugs. Thus, disinfectants act on microbes much stronger at human body temperature than at room temperature. Irradiation of the body changes its sensitivity to drugs. Significant changes in barometric pressure also affect, so there are seasonal fluctuations in the action of medicinal substances.

5. Absorption and distribution of drugs

Absorption of a medicinal substance is the process of its entry from the injection site into the bloodstream, which depends not only on the routes of administration, but also on the solubility of the medicinal substance in the tissues, the blood flow rate in these tissues and on the injection site. There are a number of successive stages in the absorption of drugs through biological barriers:

1. passive diffusion. In this way, medicinal substances that are well soluble in lipoids penetrate, and the rate of their absorption is determined by the difference in its concentration from the outer and inner sides of the membrane.

2. active transport. In this case, the movement of substances through the membranes occurs with the help of transport systems contained in the membranes themselves.

3. Filtration. Drugs penetrate through the pores present in the membranes, and the filtration rate depends on the hydrostatic and osmotic pressure.

4. Pinocytosis. The transport process is carried out through the formation of special vesicles from the structures of cell membranes, which contain particles of the drug substance, moving to the opposite side of the membrane and releasing their contents. The passage of drugs through the digestive tract is closely related to their lipid solubility and ionization. It has been established that when drugs are taken orally, the rate of their absorption in different parts of the gastrointestinal tract is not the same. Having passed through the mucous membrane of the stomach and intestines, the substance enters the liver, where it undergoes significant changes under the action of liver enzymes. The process of drug absorption in the stomach and intestines is influenced by pH. So, in the stomach the pH is 1-3, which contributes to easier absorption of acids, and an increase in pH in the small and large intestines to 8 - bases. At the same time, in the acidic environment of the stomach, some drugs can be destroyed, for example benzylpenicillin. Gastrointestinal enzymes inactivate proteins and polypeptides, and bile salts can accelerate the absorption of drugs or slow them down, forming insoluble compounds. The rate of absorption in the stomach is affected by the composition of food, gastric motility, and the time interval between meals and taking medications. After administration into the bloodstream, the drug is distributed throughout all tissues of the body, and its solubility in lipids, the quality of its connection with blood plasma proteins, the intensity of regional blood flow and other factors are important. A significant part of the medicine in the first time after absorption enters the organs and tissues that are most actively supplied with blood (heart, liver, lungs, kidneys), and muscles, mucous membranes, adipose tissue and skin are saturated with medicinal substances slowly. Water-soluble drugs that are poorly absorbed from the digestive system are administered only parenterally (for example, streptomycin). Fat-soluble drugs (gaseous anesthetics) are quickly distributed throughout the body.

6. Biotransformation and excretion of medicinal substances. The concept of pharmacogenetics

Biotransformation is a complex of physicochemical and biochemical transformations of drugs, during which metabolites (water-soluble substances) are formed that are easily excreted from the body. There are two types of metabolism: non-synthetic and synthetic. Non-synthetic reactions of drug metabolism are divided into those catalyzed by enzymes (microsomal) and those catalyzed by enzymes of other localization (non-microsomal).

Non-synthetic reactions are oxidation, reduction and hydrolysis. Synthetic reactions are based on the conjugation of drugs with endogenous substrates (such as glycine, sulfates, water, etc.). All drugs taken orally pass through the liver, where they are further converted. Biotransformation is influenced by the nature of nutrition, liver disease, gender characteristics, age and a number of other factors, and with liver damage, the toxic effect of many drugs on the central nervous system increases and the incidence of encephalopathy increases sharply. Microsomal and non-microsomal biotransformation are distinguished. Fat-soluble substances undergo microsomal transformation most easily. Non-microsomal biotransformation occurs mainly in the liver. There are several ways of removal (excretion) of drugs and their metabolites from the body. The main ones are excretion with feces and urine, exhaled air, sweat, lacrimal and mammary glands. They are excreted in the urine by glomerular filtration and tubular secretion, and their reabsorption in the renal tubules is important. In case of renal failure, glomerular filtration decreases, which leads to an increase in the concentration of various drugs in the blood, so the dose of the drug should be reduced. Drugs leave the liver in the form of metabolites or, without changing, enter the bile and are excreted in the feces. Under the influence of enzymes and bacterial microflora of the gastrointestinal tract, drugs can be converted into other compounds, again delivered to the liver, where a new cycle takes place.

The degree of excretion of medicinal substances should be taken into account in the treatment of patients suffering from liver diseases and inflammatory diseases of the biliary tract. Clinical observations have shown that the efficacy and tolerability of the same drugs in different patients is not the same. The study of the genetic basis of the sensitivity of the human body to medicinal substances and deals with pharmacogenetics.

Hereditary factors that determine unusual reactions to drugs are mainly biochemical and are most often manifested by enzyme deficiencies. Atypical reactions can also occur with hereditary metabolic disorders.

Biotransformation of drugs in the human body occurs under the influence of specific proteins (enzymes).

The synthesis of enzymes is under strict genetic control. When the corresponding genes are mutated, hereditary violations of the structure and properties of enzymes occur - fermentopathy.

7. Side effects of drugs

There are the following types of side effects and complications caused by drugs:

1) side effects associated with the pharmacological activity of drugs;

2) toxic complications caused by drug overdose;

3) secondary effects associated with a violation of the immunobiological properties of the body (decreased immunity, dysbacteriosis, etc.;

4) allergic reactions;

5) withdrawal syndrome that occurs when you stop taking the drug.

Side effects of drugs depend on the nature of the underlying disease. Systemic lupus erythematosus is more often accompanied by steroid arterial hypertension. Toxic complications occur more often when prescribing drugs in large doses. However, there are drugs that cause toxic reactions when used in average therapeutic doses (streptomycin, kanamycin, etc.). In some cases, for some drugs, it is generally impossible to avoid toxic complications. For example, cytostatics not only inhibit the growth of tumor cells, but also inhibit the bone marrow and damage all rapidly dividing cells. Allergic reactions are caused by the interaction of an antigen with an antibody and are not related to the dose of drugs. There are two types of drug-induced immunopathological reactions, such as:

1) immediate reaction (urticaria, bronchospasm, anaphylactic shock, rash);

2) delayed-type reaction (arthritis, nephritis, vasculitis, lymphadenopathy).

Withdrawal syndrome is manifested by a sharp exacerbation of the underlying disease. Thus, stopping the use of clonidine in case of hypertension can provoke the occurrence of a hypertensive crisis. Many drugs cause changes in the blood. Hemolytic anemia occurs with the use of penicillin, insulin, and other drugs. Agranulocytosis often develops with the appointment of non-steroidal anti-inflammatory drugs (indomethacin, butadione), as well as in the treatment of captopril, tseporin, etc. Thrombocytopenia occurs during therapy with cytostatics, a number of antibiotics, and anti-inflammatory drugs. Vascular thrombosis develops as a result of taking contraceptives containing estrogens and histogens. Many drugs cause gastrointestinal disturbances. So, methotrexate leads to serious damage to the mucous membrane of the small intestine. Cytostatics, some antibiotics, a number of anti-inflammatory and painkillers have a toxic effect on the liver.

LECTURE No. 4. Means acting primarily on the central nervous system

1. Means for anesthesia

Anesthesia in therapeutic doses causes reversible depression of spinal reflexes, loss of consciousness, all types of sensitivity, decreased tone of skeletal muscles while maintaining the activity of the respiratory and vasomotor centers. The basis of the action of narcotic drugs is processes leading to disruption of interneuron synaptic transmission. Depending on the depth, there are four levels of surgical anesthesia.

First level - light anesthesia: consciousness and perception of pain are absent, but strong pain stimuli can cause response motor and autonomic reactions, muscle tone is reduced, but not completely lost. This level of anesthesia is not suitable for major surgical operations without the use of additional funds.

Second level - pronounced anesthesia: pharyngeal, laryngeal, corneal and conjunctival reflexes are absent, the eyeballs are motionless, the conjunctiva is moist, but there is no lacrimation, the pupils are constricted, they react to light, reflexes from the peritoneum are preserved, muscle tone is sharply reduced, breathing is even and deep, pulse and arterial pressure is close to normal. This anesthesia can be used for most surgical procedures.

Third level - deep anesthesia: there is no skeletal muscle tone, breathing acquires an abdominal type, the pupils are slightly dilated and gradually stop responding to light, there are no reflexes from the peritoneum, the cornea is dry, the pulse is frequent, correct, blood pressure is somewhat reduced. At this level of anesthesia, any operation can be performed, but its maintenance requires a lot of experience and attention.

Fourth level - overdose: breathing becomes superficial, convulsive contractions of the diaphragm are noted, the pupils are sharply dilated, do not respond to light, the skin and mucous membranes are cyanotic, the pulse is rapid, thready, blood pressure drops sharply.

stage of bulbar palsy. Further deepening of anesthesia leads to respiratory arrest. The activity of the heart continues for some time after the cessation of breathing. Finally, the heart stops and death occurs. Means for anesthesia, depending on their physical and chemical properties and methods of application, are divided into inhalation and non-inhalation. To inhalants include volatile liquids and gaseous substances.

Non-inhalation anesthesia occurs when drugs are administered intravenously, less often intramuscularly and rectally.

Non-inhalation according to the duration of action are divided into short-acting agents (propanide, ketamine); medium duration of action (thiopental sodium, predion); long-acting (sodium hydroxybutyrate).

Basic anesthesia can be single-component or multi-component. There are four ways to use inhalation anesthetics:

1) open method using the Esmarch mask;

2) semi-open method, similar to the open one, but it does not mix with air vapors, the formation of small amounts of CO2 is observed;

3) semi-closed method. The narcotic mixture enters the tank in doses as it is inhaled and is characterized by the accumulation of CO2 in the tank and its repeated inhalation;

4) a closed method that requires the use of complex equipment, since a chemical is used to neutralize CO2 present in the inhaled air.

2. Means for inhalation anesthesia

Ether for anesthesia (Aether pro narcosi, diethyl ether).

Application: for surgical intervention, for long-term anesthesia. It is currently rarely used.

Fluorothane Phtorothanum (Halothanum, Narcotan).

A powerful narcotic drug is used in surgical interventions, diagnostic studies, and in dentistry.

Mode of application: in a mixture with oxygen using anesthesia machines (for induction anesthesia 3-4 vol.% in the inhaled mixture, to maintain the surgical stage - 0,5-1,5 vol.%.

Side effects: hypothermia, hypotension, bradycardia, ventricular fibrillation, nausea, vomiting, headache.

Contraindications: pheochromocytoma, severe hyperthyroidism, liver dysfunction, hypotension, cardiac arrhythmias, I trimester of pregnancy, use during childbirth.

Product form: in vials of 50 ml.

nitrous oxide (Nitrogenium oxydulatum).

Does not cause deep anesthesia.

Application: birth control. Minor surgical interventions. Mode of application: nitrous oxide is inhaled using a mask or intubation mixed with oxygen (70-50% nitrous nitrogen and 30-50% oxygen, respectively).

Side effects: slight negative effect on the respiratory and cardiovascular systems, liver, kidneys. Rarely - nausea and vomiting.

Contraindications: diseases of the nervous system, chronic alcoholism, acute alcohol intoxication.

Product form: metal cylinders with a capacity of 1,0 at a pressure of 50 atm. Store at room temperature, away from fire.

3. Means for non-inhalation anesthesia

Thiopental sodium (Thiopentalum-natrium).

It has a sleeping pill, and in large doses a narcotic effect. Used for induction anesthesia, endoscopic examinations, small-scale surgical procedures.

Mode of application: administered intravenously in the form of a 2-2,5% solution (for children, debilitated patients - 1% solution).

Side effects: laryngospasm, hypotension, respiratory and cardiac depression.

Contraindications: diseases of the liver and kidneys, bronchial asthma, hypotension, hypovolemia, febrile conditions, inflammatory diseases of the nasopharynx.

Product form: in vials of 1 g, in a package No. 10.

calypsol (Calypsol).

It has a fast, pronounced, but not long-lasting effect.

Application: induction and basic anesthesia for short-term surgical interventions, instrumental studies.

Mode of application: administered intravenously, intramuscularly in individual doses.

Side effects: increased blood pressure, increased heart rate, respiratory failure, hallucinations, psychomotor agitation, impaired consciousness.

Contraindications: eclampsia, arterial hypertension, cerebrovascular accident.

Product form: 5% solution of 10 ml in vials.

Brietal (Brietal).

For intravenous anesthesia of ultrashort action.

Application: induction anesthesia, anesthesia for short-term surgical interventions, for diagnostic purposes.

Mode of application: for intravenous jet administration, a 1% solution of the drug is used; for drip injection - 0,2% solution. The average dose for adults is 1-1,5 mg/kg.

Side effects: hypotension, tachycardia, cough, laryngospasm, headache, agitation, nausea and vomiting, allergic reactions.

Contraindications: severe liver damage, hypersensitivity to barbiturates.

Product form: in vials of 100 mg and 500 mg of dry matter for intravenous administration.

Sombrevin (Sombrevin).

Very short acting anesthetic.

Application: short-term and induction anesthesia.

Mode of application: administered intravenously, quickly inject a 5% solution (5-10 mg/kg); for debilitated elderly patients and children - a 2,5% solution. The surgical stage of anesthesia lasts 5-7 minutes, followed by rapid awakening.

Side effects: hyperemia and soreness along the vein at the injection site, sometimes nausea and vomiting.

Contraindications: shock, hemolytic jaundice, severe renal and hepatic dysfunction, severe heart disease, arterial hypertension.

Product form: 10 ml ampoules of 5% solution No. 5. List B.

Diprivan (Diprivan), Propofol.

It has a short action, causes a rapid onset of drug-induced sleep within about 30 seconds.

Application: induction anesthesia, maintenance of anesthesia, provision of sedation in patients undergoing mechanical ventilation.

Mode of application: for introductory anesthesia - 4 ml (40 mg) every 10 seconds until clinical signs of anesthesia appear. Maintaining adequate anesthesia is provided with an injection rate in the range of 4-12 mg/kg per hour. Children are administered the drug at a rate of 9-15 mg / kg per hour.

Side effects: hypotension, during the period of recovery from anesthesia - nausea, vomiting, headache, bronchospasm, muscle twitching.

Contraindications: allergic reaction to diprivan in history.

Product form: aqueous isotonic oil-in-water emulsion for intravenous administration, white, 10 mg per 1 ml of active ingredient.

LECTURE No. 5. Pharmacology of hypnotics

1. Sleeping pills

These are substances that promote the onset of sleep, normalize its depth, phase, duration, and prevent night awakenings. The following groups are distinguished:

1) derivatives of barbituric acid (phenobarbital, etc.);

2) drugs of the benzodiazepine series (nitrazepam, etc.);

3) preparations of the pyridine series (ivadal);

4) preparations of the pyrrolon series (imovan);

5) ethanolamine derivatives (donormil).

Barbituric acid derivatives facilitate falling asleep, dramatically change the structure of sleep: reduce the duration and phases of REM sleep. After awakening, drowsiness, weakness, and impaired coordination of movements are observed. With prolonged use, the development of mental and physical dependence is possible.

Phenobarbital (Phenobarbitalum) has a sedative, hypnotic and pronounced anticonvulsant effect.

Application: sleep disturbance, epilepsy, chorea, increased excitability of the nervous system.

Mode of application: 0,05-0,1 1 hour before bedtime.

Side effects: headache, ataxia, addiction with prolonged use.

Contraindications: liver and kidney diseases with impaired function.

Product form: powder, tablets No. 6, 0,05 each, 0,1 each; 0,005 each - for children. List B.

Etaminal sodium (Aethaminalum-natrium).

A sedative.

Application: sleep disorders.

Mode of application: orally 0,1-0,2 g, children 0,01-0,1 g, per rectum 0,2-0,3, IV 5-10 ml of solution. V.R.D - 0,3 g, V.S.D. - 0,6 g.

Contraindications: the same as for phenobarbital.

Product form: powder. List B.

Benzodiazepines.

Nitrozepam (Nitrozepanum), Neozepam, Eunoctin, Radedorm, etc.

It has a hypnotic, sedative, anticonvulsant, muscle-relaxing effect, etc.

Application: sleep disorders of various etiologies, neurosis, psychopathy with a predominance of anxiety and restlessness.

Mode of application: single dose for adults 0,005-0,01 g, maximum single dose - 0,02 g 30 minutes before bedtime. The course of treatment is 30-45 days.

Side effects: drowsiness, lethargy, ataxia, loss of coordination of movements, headache, rarely - itching, nausea.

Contraindications: myasthenia gravis, pregnancy, drivers of vehicles, persons whose activities require a quick response.

Product form: tablets of 0,005 g No. 20 and 0,01 g No. 10. List B.

Rohypnol (Rohypnol).

The active substance is flunitrazepam. Shortens the period of falling asleep, reduces the number of night awakenings.

Application: sleep disorders.

Mode of application: prescribed orally at 0,5-1 mg immediately before bedtime, for patients with prolonged sleep disorders - 1-2 mg.

Side effects: increased fatigue, headache, muscle weakness, paresthesia, severe violations of the liver, kidneys, pregnancy, lactation.

Product form: tablets 1 mg No. 20; solution for injection in 1 ml, 2 mg of flunitrozepam.

Halcyon (halcion).

Shortens the period of falling asleep, reduces the number of night awakenings, increases the duration of sleep.

For adults, the initial oral dose is 250 mcg once a day at bedtime. The maximum dose is 1 mg. The course of treatment is from 1 days to 4 months.

Side effects: like all sleeping pills.

Product form: tablets 250 mcg No. 30.

2. Hypnotics of the pyridine, pyrrolon series and ethanolamine derivatives

Pyridine preparations.

Ivadal (Ivadal).

Shortens the time to fall asleep, improves the quality of sleep.

Mode of application: Prescribe 10 mg orally at bedtime, up to 15-20 mg. The course of treatment is no more than 4 weeks.

Side effects: abdominal pain, nausea, vomiting, diarrhea, confusion, memory impairment, headache.

Contraindications: age up to 15 years, pregnancy, lactation.

Product form: tablets 10 mg No. 20.

Pyrrolone preparations.

Imovan (Imovan).

Shortens the period of falling asleep, reduces the number of night awakenings, while maintaining the quality of sleep. For sleep disorders, 7,5 mg is administered orally at bedtime, but up to 15 mg is possible.

Side effects: metallic taste in the mouth, confusion, depressed mood, dizziness, incoordination.

Contraindications: severe respiratory failure, age up to 15 years, pregnancy.

Product form: tablets 7,5 mg No. 20.

Derivatives of ethanolamine.

Donormil (Donormyl).

Reduces the time to fall asleep, increases the duration and quality of sleep, while not changing the phase of sleep. For sleep disorders, insomnia, take 15 mg orally 15-30 minutes before bedtime, dissolving the tablet in 0,5 cups of water, you can up to 30 mg.

Side effects: drowsiness, dry mouth, blurred vision, constipation, urinary retention.

Contraindications: glaucoma, prostate adenoma, lactation, age up to 15 years.

Product form: tablets 0,15 mg No. 20.

LECTURE No. 6. Psychotropic drugs

1. Psychotropic drugs. Antipsychotics

Drugs that selectively affect the complex mental functions of a person, regulating his emotional state, motivation, behavior and psychomotor activity, are referred to as psychotropic drugs. These drugs are used mainly for the treatment and prevention of mental disorders, as well as somatic diseases. Classification of psychotropic drugs:

1) neuroleptics;

2) anxiolytic sedatives;

3) antidepressants;

4) psychostimulants;

5) psychodysleptics.

From a practical point of view, drugs are divided into the following groups:

1) neuroleptics;

2) tranquilizers;

3) sedatives;

4) antidepressants;

5) psychostimulants.

Antipsychotics (antipsychotics).

Antipsychotics differ from sedatives in the presence of antipsychotic activity, the ability to suppress delusions, hallucinations, automatism and other psychopathological syndromes and to have a therapeutic effect in patients with schizophrenia and other mental illnesses. They do not have a pronounced sleeping pill, but they contribute to the onset of sleep; enhance the effect of sleeping pills and other sedatives; potentiate the action of drugs, analgesics, local anesthetics and weaken the effects of psychostimulant drugs. They are characterized by antiemetic, hypotensive, antihistamine and other effects.

Derivatives of phenothiazine.

Aminazine (Aminazinum).

It has a pronounced sedative effect, as well as antiemetic, antihistamine, hypotensive, enhances the effect of sleeping pills, painkillers.

Application: mental illness accompanied by psychomotor agitation is taken orally after meals at 0,025-0,05 1-3 times a day. In / m enter 1-5 ml of a 2,5% solution. In / in 2-3 ml (with 20 ml of 40% glucose solution) slowly with psychomotor agitation. Doses for children are individual.

Side effects: hypotension, extrapyramidal disorders, allergic reactions, dyspepsia, hepatitis.

Contraindications: diseases of the liver and kidneys, hypotension, cardiovascular decompensation, dysfunction of the stomach.

Product form: dragee 0,025 No. 30; 0,05 No. 30; tablets 0,01 No. 50 for children; 2,5% solution, 1 ml. List B.

Tizercin (Tisercin).

Indications. Psychomotor agitation, psychosis, schizophrenia, depression and neurotic reactions with feelings of fear, anxiety, insomnia. Take orally 0,025-0,4 g per day; IM 2-4 ml of 2,5% solution; if necessary - up to 0,5-0,75 g.

Side effects: extrapyramidal disorders, vascular hypotension, dizziness, constipation, dry mouth, allergic reactions.

Contraindications: diseases of the liver, hematopoietic system; hypotension, decompensation of the cardiovascular system.

Product form: dragee 0,025 g No. 50; 1 ml ampoules of 2,5% solution No. 10. List B.

2. Antipsychotic drugs

Etaperazine (Aethaperazinum, Perphenazini hydrocloridum).

It is more active than chlorpromazine in its antiemetic effect and in its ability to soothe hiccups.

Application: neurosis accompanied by fear, tension, indomitable vomiting and hiccups, vomiting of pregnant women, skin itching in dermatology.

Mode of application: taken orally in tablet form after meals. For those taking doses - 0,004-0,01 1-2 times a day. When excited, the daily dose may be 30-40 mg. The course of treatment is from 1 to 4 months. Maintenance therapy 0,01-0,06 per day.

Side effects and contraindications: the same as for chlorpromazine.

Product form: coated tablets, 0,004 each; 0,006 and 0,01 No. 50, No. 100, No. 250. List B.

Moditen, fluorophenazine (Moditen, Phthorphenazinum).

It is similar in structure to etapirazine and has a strong antipsychotic effect, combined with some activating effect. The sedative effect is moderately pronounced. In terms of its effect on delusions and hallucinations, it is less active than triftazin.

Application: various forms of schizophrenia, depressive-hypochondriac states. Small doses in neurotic conditions, accompanied by fear and tension.

Mode of application: taken orally starting from 0,001-0,002 g per day and gradually increasing the dose to 10-30 mg per day (in 3-4 doses at intervals of 6-8 hours). Maintenance therapy - 1-5 mg per day; IM is administered starting from 1,25 mg (0,5 ml of 0,25% solution) to 10 mg per day.

Side effects: convulsive reactions, extrapyramidal disorders, allergic phenomena.

Contraindications: acute inflammatory diseases of the liver, diseases of the cardiovascular system with severe decompensation, acute blood diseases, pregnancy.

Product form: tablets 1; 2,5 and 5 mg; ampoules of 1 ml of a 0,25% solution. List B.

Moditen-depot, Fluorphenazine-decanoate (Phthorphenazinum decanoate).

A strong antipsychotic with a prolonged action, the drug after a single intramuscular injection acts depending on the dose up to 1-2 weeks or more.

Application: the same as that of moditen, convenient for patients who find it difficult to prescribe neuroleptics in the usual form.

Dosing and Administration: appoint / m at 12,5-25 mg, and sometimes 50 mg (0,5-2 ml of a 2,5% solution) 1 time in 1-3 weeks.

Side effects: parkinsonism, akathisia, tremor of the fingers. To prevent and stop these phenomena, cyclodol or other antiparkinsonian drugs are taken.

Contraindications: The same.

Product form: in 1 ml ampoules of a 2,5% solution in oil (25 mg in 1 ampoule).

3. Stelazin. Haloperidol. Droperidol. Thioxanthene derivatives

Stelazin (Stelazine).

Active antipsychotic agent.

Application: schizophrenia and other mental illnesses that occur with delusions and hallucinations.

Mode of application: taken orally at 0,005, followed by an increase in dose by an average of 0,005 per day (average therapeutic dose of 0,03-0,05 g per day); in / m injected 1-2 ml of a 0,2% solution.

Side effects: extrapyramidal disorders, vegetative disorders, in some cases toxic hepatitis, agranulocytosis and allergic reactions.

Contraindications: diseases of the liver and kidneys, heart disease with impaired conduction and in the stage of decompensation, pregnancy.

Product form: coated tablets, 0,005 and 0,01 g No. 50; 10 ml ampoules of 0,2% solution No. 10; 0,5% solution No. 12.

Haloperidol (Haloperidol).

Neuroleptic with a pronounced antipsychotic effect.

Application: schizophrenia, manic, hallucinatory, delusional states, acute and chronic psychoses of various etiologies, in complex therapy.

Mode of application: take orally 0,002-0,003 g per day, intramuscularly and intravenously, 1 ml of a 0,5% solution is injected.

Side effects: extrapyramidal disorders. Drowsiness.

Contraindications: CNS diseases, depression, cardiac conduction disorders, liver and kidney diseases.

Product form: tablets of 0,0015 and 0,005 g No. 50; 1 ml ampoules of 0,5% solution No. 5; vials of 10 ml of a 0,02% solution. List B.

Droperidol (Dropidolum).

This antipsychotic has a fast, strong, but short-lived effect.

Possesses antishock and antiemetic action.

It lowers blood pressure, has an antiarrhythmic effect, and has a strong cataleptic activity.

Application: psychomotor agitation, hallucinations, relief of hypertensive crises; in anesthesiology in combination with the analgesic fentanyl for premedication, during the operation itself and after it. Enter intravenously for 30-60 minutes for premedication and neuroleptanalgesia (before surgery) 2,05-10 mg (1-4 ml of 0,25% solution) together with 0,05-0,1 mg (12 ml of 0,005% - a solution) of fentanyl or 20 mg (1-2% solution) of promedol. At the same time, 0,5 mg (0,5 ml of a 0,1% solution) of atropine is administered. Apply only in a hospital setting.

Side effects: possibly lowering blood pressure and respiratory depression.

Contraindications: severe atherosclerosis, conduction disorders of the heart muscle, diseases of the cardiovascular system.

Product form: ampoules of 5 and 10 ml of a 0,25% solution (12,5 or 25 mg; 2,5 mg in 1 ml). List A.

Derivatives of thioxanthene.

Chlorprothixene (Chlorprothixen).

It has antipsychotic, antidepressant and sedative effects.

Application: depression with anxiety symptoms, delirium delirium, sleep disturbance, somatic diseases with neurosis-like disorders, itchy skin. Take 0,025-0,05 g orally 3-4 times a day, if necessary - 0,6 g per day with a gradual dose reduction.

Side effects: hypotension, dry mouth, drowsiness, tachycardia, blurred vision, dizziness, pruritus.

Contraindications: alcohol and barbiturate poisoning, epilepsy, parkinsonism, old age, heart disease.

Product form: tablets of 0,015 and 0,05 g No. 50. List B.

4. Derivatives of the benzamide series. tranquilizers

Derivatives of the benzamide series.

Prosulpin (Prosulpin).

Blocks dopamine receptors in the brain, causes an antipsychotic effect.

It has antidepressant, antiemetic and disinhibitory effects.

Application: psychosis, depression, neurotic conditions, migraine.

Mode of application: take orally 200-600 mg per day (in 2-3 doses). M.S.D. - 2 y.

Side effects: dizziness, sleep disorders, mental agitation, dry mouth, constipation, vomiting, hypertension.

Contraindications: pheochromocytoma, arterial hypertension, pregnancy, epilepsy.

Product form: tablets 200 mg No. 30.

Benzodiazepines.

Leponex (Leponex).

It has a pronounced antipsychotic and sedative effect.

Application: schizophrenia.

Mode of application: taken orally in several doses; the average dose is 300 mg per day, the maximum is 600 mg per day, maintenance is 150-300 mg per day.

Side effects: drowsiness, fatigue, headache, dizziness, tachycardia, hypotension, nausea, vomiting, constipation, urination disorders.

Contraindications: agranulocytosis, severe liver and kidney disease, coma, toxic psychosis, heart disease.

Product form: tablets of 25 and 100 mg No. 50; ampoules of 2 ml (50 mg in solution for injection) No. 50.

Tranquilizers (anxiolytics)

Tranquilizers (anticonvulsants) are synthetic substances that weaken the feeling of fear, anxiety, internal tension, but at the same time activate positive emotions.

The main representatives are benzodiazepine derivatives that act on specific receptors localized in the limbic system and hypothalamus, used in the treatment of neurotic and borderline conditions; sleep disorders; diseases of the cardiovascular system.

Substances that do not have hypnotic, muscle relaxant and anticonvulsant properties that do not reduce attention and performance are called daytime tranquilizers.

Benzodiazepines.

Sibazon (Sibazonum).

Synonyms: diazepam, seduxen; has a pronounced tranquilizing effect; relatively strong anticonvulsant activity, antiarrhythmic action.

Application: neurotic and neurosis-like states; normalization of sleep; in combination with other anticonvulsants for the treatment of epilepsy; withdrawal syndrome in alcoholism; preoperative preparation of patients; itchy dermatoses; as a sedative and sleeping pill for patients with peptic ulcer.

Mode of application: appoint inside starting with a dose of 0,0025-0,005 g 1-2 times a day. A single dose for adults is from 0,005 to 0,015 g, for children 0,002-0,005 g. The daily dose should not exceed 0,025 g in 2-3 doses.

Side effects: drowsiness, nausea, dizziness, menstrual disorders, decreased libido.

Contraindications: acute diseases of the liver and kidneys, severe myasthenia gravis, pregnancy; alcohol intake.

Product form: tablets 0,005 g No. 50, 0,001 and 0,002 No. 20. List B.

5. Tranquilizers

Xanax (Xanax).

The active substance is alprazolam. Reduces anxiety, feelings of anxiety, fear, tension. It has antidepressant properties, central muscle relaxant and moderate hypnotic activity.

Application: a state of fear and anxiety; neurotic and reactive depressions; depression that developed against the background of somatic diseases. In states of anxiety, take orally 250 mcg 3 times a day.

The average maintenance dose is 500 mcg (4 mg per day in divided doses); with depression - 500 mcg 3 times a day; if necessary - up to 1-4 mg per day. Cancel the drug to produce gradually.

Side effects: drowsiness, dizziness, urinary retention or incontinence, changes in body weight.

Product form: tablets of 250 and 500 mcg, 1, 2, 3 mg No. 30.

Tranxen (Tranzene).

The active substance is dipotassium clorazepate. It has a sedative, anticonvulsant and muscle relaxant effect.

Application: same as xanax; for the prevention of delirium in patients with alcoholism.

Mode of application: appoint inside 25-100 mg per day.

Side effects: drowsiness, muscle weakness, nausea, vomiting.

Contraindications: respiratory failure, pregnancy.

Product form: capsules of 5 and 10 mg No. 30.

Phenazepam (Phenazepanum).

It has a pronounced hypnotic, tranquilizing, hypnotic and muscle relaxant effect.

Application: same as xanax.

Mode of application: take orally 0,0005-0,001 g to 0,002-0,005 g 2-3 times a day.

Side effects: the same.

Contraindications: severe myasthenia gravis, impaired liver and kidney function, pregnancy, work that requires a quick reaction, alcohol poisoning, sleeping pills.

Product form: tablets 0,0005 and 0,001 No. 50; 1 ml ampoules of 3% solution No. 10.

This group also includes Chlozepidum, or Elenium, Nozepamum, their synonyms are tazepam, oxazepam. As a daytime tranquilizer - Mezapamum, synonym - rudotel. Its calming effect is combined with some activating effect. As an outpatient, adults are prescribed 0,005 in the morning and at noon, and 0,01 in the evening. The maximum dose is 0,06-0,07 g.

Contraindications: the same as for other drugs in this group.

6. Sedatives (sedatives)

These are natural and synthetic substances that eliminate hyperexcitability, irritability. The main mechanism of action is an increase in the processes of inhibition or a decrease in the processes of excitation, providing a regulatory effect on the functions of the central nervous system. They enhance the effect of sleeping pills, analgesics and other neurotropic sedatives, facilitate the onset of natural sleep and deepen it. It is used to treat a mild degree of neuroses, neurasthenia, the initial stage of hypertension, neuroses of the cardiovascular system, spasms of the gastrointestinal tract. Sedatives include bromides and preparations derived from plants.

Sodium bromide (Sodium bromidum).

It has the ability to concentrate and enhance the processes of inhibition in the cerebral cortex, to restore the balance between the processes of excitation and inhibition.

Application: neurasthenia, hysteria, increased irritability, insomnia, initial forms of hypertension, as well as epilepsy and chorea. Prescribed orally before meals in solutions (potions). The dose for adults is from 0,1 to 1 g 3-4 times a day, in the form of a 3% solution - 1-2 tbsp. l. at night or 2-3 times a day.

Side effects: bromism, which is expressed in the form of a runny nose, cough, general lethargy, memory loss, skin rash and conjunctivitis. In this case, with a large amount of sodium chloride (10-20 g per day) and water (3-5 liters per day), it is necessary to rinse your mouth and wash your skin often, empty your intestines regularly.

Product form: powder from which solutions and mixtures are prepared.

Bromocamphor (Bromcamphora).

Indications, application: the same as sodium bromide, but also improves cardiac activity.

Product form: powders and tablets of 0,15 and 0,25.

Belloid (belloid).

Combined drug that has a calming and adrenolytic effect.

Application: disorders of the autonomic nervous system, insomnia, increased irritability. Assign inside 1 tablet 3-4 times a day.

Side effects: nausea, vomiting, diarrhea, dry mouth.

Product form: dragees in a package of 50 pieces.

This group also includes the drug bellataminal (Bellataminalum), which is also used for neurodermatitis and menopausal neurosis.

Contraindications: pregnancy, glaucoma.

The group of sedatives includes magnesium sulfate (Magnesii sulfas), available in the form of powders and ampoules; solution of 25%, 5 and 10 ml. When administered parenterally, it has a calming effect on the central nervous system. Depending on the dose, a sedative, hypnotic or narcotic effect is observed. It has a choleretic effect, in large doses it has a curare-like effect.

Application: as a sedative, laxative, anticonvulsant, antispasmodic, choleretic, for the treatment of hypertension in the initial stage and for the relief of hypertensive crises; for labor pain relief. In magnesium sulfate poisoning, calcium chloride is used.

7. Herbal sedatives

Rhizome with valerian roots (Rhizoma cum radicibus Valerianae).

Valerian preparations reduce the excitability of the central nervous system, enhance the effect of sleeping pills, and have an antispasmodic effect.

Application: increased nervous excitability, insomnia, cardioneurosis, spasms of the gastrointestinal tract. Assign inside an infusion of 20 g of root per 200 ml of water, 1 tbsp. l. 3-4 times a day; tincture on 70% alcohol in vials of 20-30 drops 3-4 times a day; thick extract in tablets of 0,02-0,04 per dose.

Product form: rhizome with valerian roots, 50 g per pack; in briquettes of 75 g; tincture of 30 or 40 ml; thick extract in tablets of 0,02 No. 10 and No. 50.

This group includes preparations made from motherwort herb (Herba Leonuri), passionflower herb (Herba Passiflorae) and peony tincture (Tinctura Paeoniae).

Also apply combination herbal medicines.

Novopassit (Novo Passit).

Combined preparation consisting of a complex of extracts of medicinal plants and guaifenesin.

Application: mild forms of neurasthenia, sleep disorders, headaches caused by nervous strain. I take 1 tsp inside. (5 ml) 3 times a day, up to 10 ml per day.

Side effects: dizziness, lethargy, drowsiness, nausea, vomiting, diarrhea, pruritus, constipation.

Contraindications: myasthenia gravis, hypersensitivity to the components of the drug.

Product form: solution of 100 ml in a vial.

This group also includes the drug phytosed 100 ml.

Application: the same as that of the novopassitis.

Corvalol (Corvalolum) is similar to the imported product valocordin (Valocardinum), belongs to the group of combined drugs. Valocordin also includes hop oil, which enhances the effect. Both drugs have a mild hypnotic effect, reflex and vasodilating and antispasmodic activity, but valocordin acts more strongly.

Application: neuroses, states of excitation, functional disorders of the cardiovascular system. Prescribe 15-20 drops orally, for tachycardia and spasms - up to 40 drops.

Side effects: in some cases, drowsiness and slight dizziness can be observed, with a decrease in the dose, these phenomena disappear.

Product form: corvalol 15 ml; valocordin 20 and 50 ml.

This group also includes the drug valocormide (Valocormidum). Combined drug, which also includes sodium bromide.

Application: same as Corvalol.

Side effects and contraindications: like sodium bromide. Produced in bottles of 30 ml.

8. Antidepressants

These are medicinal substances that eliminate symptoms of depression in neuropsychic and somatic patients. In most cases, drug interactions occur at the level of synaptic neurotransmission. Moreover, some antidepressants block metabolic pathways for the destruction of neurotransmitters (norepinephrine, serotonin, dopamine), while others block their reuptake by the presynaptic membrane. Antidepressants are divided into the following groups: monoamine oxidase inhibitors, tricyclic antidepressants, tetracyclics, selective serotonin reuptake inhibitors, combined and transitional antidepressants and mood stabilizers.

Tricyclic and tetracyclic antidepressants.

Imizin (Imizinum).

Synonym: Melipramin. The main representative of this group. It inhibits the reverse neuronal uptake of monoamines - neurotransmitters.

Application: depressive states of various etiologies, neutrogenic enuresis in children. Prescribed orally starting from 0,075-0,1 g per day (after meals), gradually increasing the dose to 0,2-0,25 g per day. The course of treatment is 4-6 weeks. 0,025 g 1-4 times a day - maintenance therapy. In a hospital setting, for severe depression, 2 ml of a 1,25% solution is administered intramuscularly, 1-3 times a day. V.R.D. orally - 0,1, V.S.D. - 0,3 g, intramuscular one-time - 0,05, daily - 0,2 g.

Side effects: headaches, sweating, dizziness, palpitations, dry mouth, disturbance of accommodation, urinary retention, delirium, hallucinations.

Contraindications: monoamine oxidase inhibitors, thyroid drugs, acute diseases of the liver, kidneys, hematopoietic organs, glaucoma, cerebrovascular accidents, infectious diseases, prostate adenoma, atony of the bladder. Careful use is required for epilepsy, in the XNUMXst trimester of pregnancy.

Product form: tablets of 0,025 g and 1,25% solution in ampoules of 2 ml. List B.

Amitriptyline (Amitriptylinum).

In structure and action, it is close to imizin.

Application: the same as imizin.

Side effects: the same, but unlike imizin does not cause delirium, hallucinations.

Product form: dragee 25 mg No. 50; injection solution for 2 ml in ampoules No. 10 (1 ml contains 10 mg of the active substance).

Maprotiline (Maprotilinum).

Synonym: Ludiomil. Enhances the pressor action of norepinephrine, selectively inhibits the capture of norepinephrine by presynaptic nerve endings. It has a moderate tranquilizing and anticholinergic activity.

Application: depression of various etiologies; prescribed orally 25 mg 3 times a day with a gradual increase in dose to 100-200 mg per day. When administered intravenously, the daily dose is 25-150 mg.

Side effects: the same as for imizin and amitriptyline.

Contraindications: the same as imizin and amitritriptyline.

Product form: dragee 10, 25, 50 mg No. 50, solution for injection in ampoules of 2 ml No. 10.

9. Other drugs from the group of antidepressants

monoamine oxidase inhibitors.

The action is manifested in the inhibitory effect on the deamination of monoamines. There are inhibitors of irreversible and reversible action, the latter being non-selective and selective action (type A).

Aurorix (Aurorix).

Antidepressant, reversible type A inhibitor.

Application: depressive syndromes. Take 150 mg orally 2 times a day after meals, if necessary - up to 600 mg per day.

Side effects: dizziness, sleep disturbances and others characteristic of antidepressants.

Contraindications: childhood, acute cases of confusion.

Product form: 150 and 300 mg film-coated tablets, No. 30.

Selective serotonin reuptake inhibitors.

Fluoxetine (Fluozetine).

Application: depression of various origins, obsessive thoughts. Take orally 1 capsule (20 mg per day in the morning). M. S. D. - no more than 80 mg.

Side effects and contraindications: the same as other antidepressants.

Product form: capsules, tablets of 20 mg No. 14 and 28.

Combined and transitional antidepressants.

Amixid (Amixid).

A combination drug of amitriptyline and chlordiazepoxide.

Application: depression of various origins with anxiety syndrome. Prescribe 1 tablet orally 2-3 times a day, if necessary - up to 6 tablets a day.

Side effects: the same as other antidepressants.

Contraindications: acute period of myocardial infarction, simultaneous administration of MAO inhibitors.

Product form: tablets in package number 100.

Heptral (Heptral).

Antidepressant and hepatoprotector.

Application: depression, liver disease, withdrawal syndrome.

Average doses - 1200-1600 mg per day; IV drip or IM 200-400 mg.

The course of treatment is 2-3 weeks.

Side effects: discomfort in the epigastric region, sleep disturbance.

Product form: tablets No. 20. Lyophilized dry substance for injection in a vial in combination with a solvent, 5 pieces per pack.

10. Normothymic drugs

lithium carbonate (Lithii carbonas).

Prevents the development of the depressive phase of psychosis. Mechanism of action: inhibits the transmembrane transfer of sodium ions, which stabilize the membrane of the nerve cell and increase its excitability; accelerates the metabolism of norepinephrine, reduces the level of serotonin, increases the sensitivity of brain neurons to dopamine.

Application: manic and hypomanic states of various origins, chronic alcoholism. For medicinal purposes, from 0,6-0,9 g per day, gradually increasing the dose, bring it to a daily dose of 1,5-2,1 g, sometimes up to 2,4 g, making sure that the concentration of lithium in the blood does not exceed 1,6 .XNUMX µv/l.

After the disappearance of manic symptoms, the daily dose is gradually reduced.

Can be taken simultaneously with antipsychotics and antidepressants.

It is necessary to control the water-salt balance.

Side effects: dyspeptic disorders, a temporary increase in body weight, increased thirst are possible.

Contraindications: kidney and cardiovascular disorders, pregnancy, salt-free diet.

Product form: tablets 0,3 No. 10.

kontemnol (Contemporol).

Application: manic-depressive psychosis, psychopathy, chronic alcoholism, migraine. The average oral dose is 1 g per day for 1 dose.

Side effects and contraindications: like a lithium preparation.

Product form: retard tablets 500 mg No. 100.

LECTURE No. 7. Means that stimulate the central nervous system (psychostimulants)

1. Means that stimulate the central nervous system

They are divided into the following groups.

1. Psychostimulants that have a stimulating effect on the functions of the brain and activate the mental and physical activity of the body and are divided into two subgroups.

The first includes caffeine, phenamine, sydnocarb and sydnofen, which have a fast-acting stimulating effect. In drugs of the second subgroup, the action develops gradually. These are nootropic drugs: piracetam, aminalon, sodium oxybutyrate, phenibut, pantogam, encephabol, acephene.

2. Analeptics excite primarily the centers of the medulla oblongata - vascular and respiratory; in large doses, they also stimulate the motor areas of the brain and cause convulsions. These are corazol, cordiamine, camphor. From the group of analeptics, a group of respiratory analeptics (cytiton, lobelin) is distinguished, they are characterized by a stimulating effect on the respiratory center.

3. Means that act primarily on the spinal cord. The main representative of this group is strychnine. There is another group of different herbal remedies that have a stimulating effect on the central nervous system. These are lemongrass fruits, ginseng root, pantocrine, etc.

psychomotor stimulants.

Caffeine (Coffinum).

Strengthens and regulates the processes of excitation in the cerebral cortex, leading to an increase in mental and physical performance.

Application: drug poisoning, insufficiency of the cardiovascular system, cerebral vascular spasms, increased mental and physical performance. Taken orally, the average dose of caffeine for adults is 0,05-0,1 g 2-3 times a day. V.R.D. - 0,3; V.S.D. - 1 year

Side effects: with prolonged use, the effect decreases, and with sudden cessation of use, inhibition increases with symptoms of fatigue, drowsiness, and depression; decrease in blood pressure.

Contraindications: irritability, insomnia, severe hypertension, atherosclerosis, organic diseases of the cardiovascular system, old age, glaucoma.

Product form: tablets number 10.

Caffeine-sodium benzoate (Coffeinum-natrii benzoas).

Similar to caffeine, but more soluble in water.

Product form: tablets 0,1 and 0,2 No. 5; in the form of a 10 and 20% solution in 1-2 ml ampoules.

2. Nootropics

They activate the higher integrative activity of the brain, improve its functions, increase the resistance of the brain to extreme influences. They are used in the treatment of neurological and mental diseases.

Pyracetam (Pyracetanum).

Synonym: (Nootropin). It enhances the metabolic processes of the brain, accelerates the transmission of nerve impulses in the brain, improves microcirculation, without exerting a vasodilating effect.

Application: chronic and acute disorders of cerebral circulation, craniocerebral trauma, depression of various etiologies, alcoholism and drug addiction. In severe conditions, intramuscularly or intravenously, 2-6 g per day is administered.

In chronic conditions - 1,02-2,04 g, sometimes up to 3,2 g per day in 3-4 doses.

Side effects: increased irritability, excitability, sleep disturbances, dyspeptic phenomena.

Contraindications: severe renal dysfunction, pregnancy, lactation.

Product form: capsules 0,4 No. 60; tablets of 0,2 No. 60, ampoules of a 20% solution of 5 ml No. 10.

Aminalon (Aminalonum).

Synthetic analogue - GABA (γ-aminobutyric acid).

Application: the same as that of piracetam, in addition, it is used for motion sickness.

Side effects: sleep disturbance, sensation of heat, fluctuations in blood pressure.

Product form: tablets 0,25 No. 100.

Cerebrolysin (Cerebrolysinum).

Nootropic agent. This is a complex of peptides derived from the brain of pigs. Helps improve metabolism in the brain tissue.

Application: central nervous system diseases, brain injuries, memory loss, dementia. Inject 1-2 ml intramuscularly every other day. The course of treatment is 30-40 injections, with intravenous administration - 10-60 ml.

Contraindications: acute renal failure, status epilepticus.

Product form: in ampoules of 1 ml No. 10 and 5 ml No. 5.

Pyriditol (Pyriditolum).

Synonym: Encefabol; picamilon, (Picamylon), vasobral, (Vazobralum), instenon, (Instenon), phenibut (Phenibutum), (bilobil, (Bilobyl), tanakan, (Tanacan). Tanakan and bilobil are preparations from the gingo biloba plant.

Action and application: of these drugs is the same as that of cerebrolysin.

Sodium oxybutyrate (Sodium oxybutyras).

In structure and action, it is close to GABA, enhances the effect of narcotic and analgesic substances.

Application: as a non-inhalation narcotic for single-component anesthesia, for induction and basic anesthesia in the elderly, to reduce neurotic reactions and improve sleep.

Mode of application: administered intravenously at the rate of 70-120 mg per 1 kg of body weight; for weakened patients - 50-70 mg/kg.

Dissolve in 20 ml of 5% (sometimes 40%) glucose solution.

Enter slowly (1-2 ml per minute); i / m is administered at a dose of 120-150 mg / kg or at a dose of 100 mg / kg in combination with barbiturates.

Side effects: with rapid intravenous administration, motor agitation, convulsive twitching of the limbs and tongue, and sometimes vomiting are possible; in case of overdose, respiratory arrest occurs.

With prolonged use - hypokalemia.

Contraindications: hypokalemia, myasthenia gravis, pregnancy toxicosis, neuroses, glaucoma.

Product form: ampoules of 10 ml of a 20% solution. List B.

3. Analeptics

Cordiamin (Cordiaminum).

Stimulates the central nervous system, excites the respiratory and vasomotor centers.

Application: acute and chronic circulatory disorders, reduced vascular tone, weakening of breathing, acute collapse and asphyxia, shock.

Mode of application: Prescribe 30-40 drops orally before meals. Parenteral: subcutaneously, intramuscularly; administered intravenously (slowly) to adults at a dose of 1-2 ml 2-3 times a day; for children - depending on age. To reduce pain, novocaine is first injected into the injection site, V.R.D. - 2 ml (60 drops), V.S.D - 6 ml (180 drops); SC single - 2 ml, daily - 6 ml.

Product form: in ampoules of 1 ml and 2 ml for injection; in a bottle of 15 ml. List B.

Camphor (Camphora).

It has a direct effect on the cardiac system, enhances metabolic processes in it, increases its sensitivity to the influence of sympathetic nerves, tones the respiratory center, stimulates the vasomotor center, improves microcirculation.

Application: acute and chronic heart failure, collapse, respiratory depression, poisoning with sleeping pills and narcotic drugs.

Side effects: possible formation of an infiltrate.

Contraindications: epilepsy, a tendency to convulsive reactions.

Product form: preparations for injection, use a 20% oil solution of camphor; for external use - camphor oil (10% solution of camphor in sunflower oil) (Sol. Camphorae oleosae ad usum externum); camphor ointment (Ung. Camphoratum) is used for muscle pain and rheumatism. Camphor alcohol (Spiritus Camphorae) in 40 ml bottles is used for rubbing.

Sulfocamphocaine (Sulfocamphocainum 10% pro injectionibus).

This is a complex compound of sulfacamphoric acid and novocaine. By action it is close to camphor, but does not cause the formation of infiltrates. It is used mainly for acute heart and respiratory failure, with cardiogenic shock. Contraindicated in idiosyncrasy to novocaine, with hypotension.

Product form: in 2 ml ampoules of 10% solution No. 10.

This group also includes the drugs Cytitonum and lobeline hydrochloride (Lobelini hydrochloridum). Used as respiratory analeptics. The drug Tabex is used to facilitate smoking cessation. Prescribe 1 tablet 5 times a day with a further dose reduction of 1-2 tablets per day. The course of treatment is 20-25 days. List B.

Various drugs that have an exciting effect on the central nervous system.

Ginseng root (Radix Ginseng).

Tonic.

Application: hypotension, fatigue, fatigue, neurasthenia. Take 15-20 drops 2 times a day in the morning.

Contraindications: insomnia, increased irritability.

Product form: tincture on 70% alcohol, 50 ml.

This group also includes: lemongrass tincture (Tinctura Schzandrae), liquid rhodiola extract (Extractum Rhodiolae fluidum), lure tincture (Tinctura Echinopanacis), aralia tincture (Tinctura Araliae), eleutherococcus extract (Extractum Eleutherococci fluidum), etc.

Application: as a tonic and tonic, CNS stimulant.

Rhodiola extract pink is also used for symptoms of asthenia, akineto-hypotonic syndrome; at first 10 drops 2-3 times a day, then up to 30-40 drops. The course of treatment is 1-2 months.

Pantocrine (Pantocrine).

Liquid extract from the antlers of deer, red deer and sika deer. It is used as a central nervous system stimulant, 30-40 drops per day, s / c 1-2 times a day. The course of treatment is 2-3 weeks.

Contraindications: severe atherosclerosis, organic heart disease, angina pectoris, increased blood clotting, severe forms of nephritis, diarrhea. List B.

LECTURE No. 8. Anticonvulsants

1. Anticonvulsants (antiepileptic) drugs

These are drugs that prevent or stop the development of seizures of various origins and varying degrees of severity. The group of anticonvulsants also includes antiepileptic drugs. The action of the latter is based on the suppression of the excitability of the neurons of the epileptic focus or on the inhibition of the irradiation of pathological impulses from the epileptogenic focus to other parts of the brain. Antiepileptic drugs reduce the frequency and strength of seizures, slow down the process of degradation of the psyche. The abolition of these drugs should be made gradually. The most common drug is phenobarbital, which has a strong anticonvulsant activity and at the same time a strong sedative effect.

Remedies for major convulsive seizures.

Phenobarbital (Phenobarbitalum).

It is prescribed in sub-sleeping doses. We considered this remedy earlier in the group of sleeping pills.

Difenin (Diphenin).

It has a pronounced anticonvulsant effect.

Application: epilepsy, mostly grand mal seizures. Assign inside after eating 0,1-0,3 g 1-3 times a day.

Side effects: ataxia, tremor, dysarthria, nystagmus, eye pain, irritability, skin rashes, gastrointestinal disturbances.

Contraindications: diseases of the liver, kidneys, decompensation of the cardiovascular system.

Product form: tablets 0,117 No. 10.

Tegretol (Tegretol).

Synonyms: Carbamazepinum, Finlepsin. Antiepileptic drug.

Application: epilepsy with grand mal seizures. The average dose at the beginning of treatment is 200 mg 1-2 times a day, subsequently up to 400 mg 2-3 times a day.

Side effects: loss of appetite, dry mouth, nausea, diarrhea, constipation, drowsiness, ataxia, blurred vision.

Contraindications: hypersensitivity to the drug, atrioventricular heart block.

Product form: tablets 200 and 400 mg No. 30.

This group of the drug also includes hexamedine (Hexamedinum), benzonal (Benzonalum), chloracone (Chloraconum), clonazepam (Clonazepanum). Synonym: Antelepsin.

Remedies for small seizures of epilepsy.

Suxilep (Suxilep) is an anticonvulsant.

Application: small forms of epilepsy, myoclonic seizures. Take orally 0,25 g 4-6 times a day.

Side effects: dyspepsia, headache, dizziness, leukopenia.

Product form: capsules of 0,25 No. 100.

Depakin (Depacine). Synonyms: valproic acid, sodium valproate (Acidum valpricum, Natrium valproicum). Anticonvulsant drug.

Application: petit epileptic seizures. 20-30 mg/kg per day; if necessary - up to 200 mg per day, every 3-4 days. M.S.D. - 50 mg/kg per day.

Side effects: nausea, vomiting, diarrhea, liver and pancreas dysfunction, anemia, leukopenia, ataxia, tremor, allergic reactions.

Product form: tablets 300 mg No. 100.

2. Remedies for the treatment of parkinsonism

The drugs of this group weaken or eliminate the symptoms of Parkinson's disease and other diseases associated with a predominant lesion of the subcortical nodes of the brain. The treatment of this disease is based on restoring the disturbed balance between dopaminergic and cholinergic processes in the extramid system. According to the clinical impact, the following agents are distinguished:

1) drugs that affect the dopaminergic systems of the brain;

2) antiparkinsonian anticholinergic drugs;

3) means for the treatment of spasticity.

Drugs that affect the dopaminergic systems of the brain.

Levodopa (Levodopa).

Formed in the body from the amino acid tyrosine, and is a precursor of the adrenergic mediators dopamine, norepinephrine and adrenaline, eliminates or reduces akinesia and rigidity.

Application: Parkinson's disease, parkinsonism. It is taken orally after meals starting from 0,25 g, increasing the dose to 4-6 g in 3-4 doses. B. S. D. - 8 g. During treatment, vitamin B6 should not be taken.

Side effects: nausea, vomiting, loss of appetite, hypotension, arrhythmia, irritability, depression, tremor.

Contraindications: liver and kidney dysfunction, childhood, lactation, heart disease, blood diseases, narrow-angle glaucoma, MAO inhibitors.

Caution should be used in patients with bronchial asthma, emphysema, with an active stomach ulcer, with psychosis and neurosis, in patients who have had a myocardial infarction in the past.

Product form: capsules and tablets of 0,25 and 0,5 g No. 100.

This group also includes the combined drug on whom (Nacom), consisting of 0,25 g of levodopa and 25 mg of carbidopa, in which the therapeutic effect is enhanced and the side effects are reduced.

Antiparkinsonian anticholinergic drugs.

Cyclodol (Cyclodolum).

Cholinoblokator with pronounced central (n-cholinergic receptors) and peripheral (m-cholinergic receptors) anticholinergic properties.

Application: parkinsonism of various etiologies. Inside, 0,001-0,002 g per day; it is possible to increase up to 0,002-0,004 g per day.

Side effects: dry mouth, visual disturbances, tachycardia, dizziness, mental and motor agitation.

Contraindications: pregnancy, glaucoma, prostate adenoma.

Product form: tablets 0,002 No. 50. List A.

Means for the treatment of spasticity.

Mydocalm (Mydocalm).

Suppresses polysynaptic spinal reflexes and lowers the increased tone of skeletal muscles.

Application: diseases accompanied by increased muscle tone, paralysis, paresis, contractures, extrapyramidal disorders, as an adjuvant in the treatment of parkinsonism. Take 0,05 g orally 3 times a day with a gradual increase in dose to 0,45 g per day, administer intramuscularly - 1 ml of a 10% solution 2 times a day, intravenously - 1 ml per day .

Side effects: headache, irritability, sleep disturbance.

Contraindications: myasthenia gravis, children's age (up to 3 months).

Product form: tablets of 0,05 No. 30, ampoules of 1 ml of a 10% solution No. 5.

LECTURE No. 9. Analgesics and non-steroidal anti-inflammatory drugs. Oksinamy and preparations of gold

1. Analgesics. Narcotic analgesics

Analgesics - These are drugs that selectively eliminate pain sensitivity or reduce the feeling of pain. Analgesics are divided into two main groups:

1) narcotic analgesics;

2) non-narcotic analgesics.

Narcotic analgesics. These are preparations of morphine and its synthetic substitutes. The main mechanism of action: communication with opiate receptors of the central nervous system and peripheral tissues, leading to stimulation of the analgesic system and impaired neural transmission of pain impulses; providing a specific effect on the human central nervous system, expressed in the development of euphoria, and then syndromes of mental, physical dependence and addiction.

Morphine hydrochloride (Morphini hydrochloridum).

Active analgesic.

Application: pain of various etiologies. It is taken orally at 0,01-0,02 g, injected s / c, 1 ml of a 1% solution. V. R. D. - 0,02, V. S. D. - 0,05 g.

Side effects: nausea, vomiting, constipation, oppressed breathing.

Contraindications: respiratory failure, the possibility of developing drug addiction.

Product form: 1 ml ampoules of 1% solution No. 10. List A.

Promedol (Promedolum).

A synthetic drug similar to morphine, but less depresses the respiratory center and excites the center of the vagus nerve, the vomiting center.

Application: pain of various etiologies. Enter s / c 1 ml of a 1-2% solution; take orally 0,025-0,05 g per reception.

Product form: powders, tablets of 0,025, ampoules and syringe-tubes of 1 ml of a 1-2% solution.

Omnopon (Omnoponum) - a mixture of opium alkaloids, including 50% morphine.

Action, use, side effects, contraindications: the same as morphine.

Mode of application: 1 ml of 1-2% solution is administered subcutaneously, 0,01-0,02 g is taken orally.

Product form: 1 ml ampoules of 1-2% solution No. 10. List B.

Valoron (Valoron).

Synonym: Tilidine. Synthetic centrally acting morphine substitute.

Application: severe pain syndrome of various origins. Take 50-100 mg 4 times a day. Daily dose - 400 mg.

Side effects: dizziness, nausea, vomiting, weakening of attention, slow reaction.

Contraindications: drug addiction, lactation.

Product form: capsules 50 mg No. 10 and 20.

This group also includes the following drugs: codeine (Codeinum), codeine phosphate (Codeini Phosphas) ​​(both drugs are used to calm cough), ethylmorphine hydrochloride (Aethylmorphini hydrochloridum) - mainly in ophthalmology in the form of eye drops and ointment.

2. Fentanyl. Antagonists of narcotic analgesics

Fentanyl (Phentanylum).

It has a strong, fast, but short analgesic effect.

Application: for neuroleptanalgesia in combination with neuroleptics; to relieve acute pain in myocardial infarction, angina pectoris, renal and hepatic colic.

Enter in / m or / in 0,5-1 ml of a 0,005% solution. If necessary, repeat every 20-40 minutes.

Side effects: possible respiratory depression, eliminated by the / in the introduction of nalorfin, motor excitation, spasm, hypotension, sinus tachycardia.

Contraindications: caesarean section operation; severe hypertension, depression of the respiratory center.

Product form: 2 ml ampoules of 0,005% solution. List A.

Antagonists of narcotic analgesics.

Nalorphine hydrochloride (Nalorphini hydrochloridum).

Antagonist to morphine and other opiates, but retains some of the properties of morphine.

Application: as an antidote for severe respiratory depression and other violations of body functions caused by acute poisoning with an overdose of narcotic analgesics. Enter in / in, in / m or s / c. Adults: 0,005-0,01 g (1-2 ml of 0,5% solution).

Side effects: with large doses, nausea, drowsiness, headache, and mental agitation are possible. Drug addicts experience an attack of withdrawal.

Product form: powder; 0,5% solution in ampoules of 1 ml (for adults) and 0,05% solution for newborns.

Naloxone (Naloxone).

Application: the same as nalorphine hydrochloride. Enter s / c, / m, / in 0,4 mg, with insufficient effect, re-introduce at the same dose after 2-3 minutes.

Side effects: tachycardia, nausea, vomiting, hypotension.

Product form: solution for injection: 1 ml - 0,4 mg of naloxone.

3. Non-narcotic analgesics. Derivatives of pyrozolone and para-aminophenol

Non-narcotic analgesics are drugs of various chemical structures that have analgesic, antipyretic and anti-inflammatory effects. The mechanism of the analgesic effect: inhibition of the synthesis of the main factors of the inflammatory reaction (prostaglandins, prostacyclins and thromboxane), impaired conduction of afferent pain impulses to the cerebral cortex.

Pyrosolone derivatives.

Among the drugs of this group are butadion (Butadinum), analgin (Analginum), amidopyrine (Amidopyrinum), antipyrine (Antipyrinum), ketazon (Cetazon) and tandedril (Tandedril). Mechanism of action: reduced energy supply of inflammation, inhibition of the activity of proteolytic enzymes, reduced capillary permeability and inhibition of inflammatory infiltration.

Analgin (analginum).

It has antipyretic, analgesic and anti-inflammatory action.

Application: pain of various origins, rheumatism, chorea. Take 0,25-0,5 g 2-3 times a day orally, for rheumatism - 0,5-1,0 g 3 times a day. 1-2 ml of a 50% solution is administered intramuscularly 2-3 times a day.

Side effects: allergic reactions and anaphylactic shock are possible.

Product form: tablets of 0,5 g No. 10, powder, ampoules of 1 and 2 ml of a 50% solution.

Analgin is part of some combined preparations: benalgin (Benalginum), bellalgin (Bellalginum), tempalgin (Tempalginum), anapyrin (Anapyrinum), pentalgin (Pentalginum).

Butadione (Butadionum).

Application: like analgin. Take orally 0,15 g 4-6 times a day after meals. The ointment is applied in a thin layer, without rubbing, on the surface of the skin 2-3 times a day.

Side effects: nausea, pain in the stomach, liver and kidney disease, arrhythmia, circulatory failure.

Product form: tablets 0,05 No. 10; ointment - 20 g in a tube.

Para-aminophenol derivatives.

These include the drugs phenacetin (Phenacetinum) and paracetamol (Paracetamolum).

Paracetamol is widely used. Phenacetin in its pure form is practically not used, but in a mixture with other drugs these are the drugs sedalgin, citramon.

Paracetamol (Paracetamolum).

Synonyms: Acetaminophen, Panadolum, Efferalganum. Antipyretic and analgesic.

Application: as with other drugs, 0,2-0,4 per dose.

Side effects: nephrotoxic.

Contraindications: kidney disease.

Product form: tablets 0,2 No. 10.

4. Non-steroidal anti-inflammatory drugs

Mechanism of action: they have a normalizing effect on increased capillary permeability and on microcirculation processes, thus reducing the energy supply of biochemical processes that play a role in inflammation.

This group includes salicylamide, acetylsalicylic acid (aspirin) - Acidum acetylsalicylicum (Aspyrinum).

pharmachologic effect и testimony the same as other analgesics, but still has an antiaggregatory effect, therefore it is also used for the prevention of thrombosis and embolism.

Application: Take 0,5-1,0 3-4 times a day after meals, for the prevention of thrombosis - 125-300 mg per day.

Side effects: nausea, loss of appetite, pain in the stomach, anemia, ulcerogenic effect.

Contraindications: peptic ulcer of the stomach and duodenum, kidney disease, bleeding tendency, pregnancy.

Product form: tablets of 100, 300 and 500 mg No. 10 and 100.

Combined preparations with aspirin: Alka-Prim, Alka-Seltzer, Upsa aspirin with vitamin C, Askofen, Citramon, Sedalgin.

Derivatives of indoleacetic acid represented by drugs: indomethacin (methindol); tolectin; clinoril.

Indomethacin (Indometacin).

Synonym: Metindolum. It blocks the synthesis of prostaglandins and the migration of leukocytes to the area of ​​inflammation. It has antipyretic, analgesic and anti-inflammatory action.

Application: rheumatic diseases of the joints, injuries of the musculoskeletal system, neuralgia. Take orally after meals 25 g 2-3 times a day.

The ointment is applied to the areas 2 times a day.

Side effects: headache, dizziness, dyspepsia, anemia, pain in the stomach.

Contraindications: peptic ulcer of the stomach and duodenum, impaired hematopoiesis, lactation, pregnancy, age up to 14 years.

Product form: capsules 0,25 No. 30; ointment 10% in tubes of 40 g; rectal suppositories 50 and 100 mg No. 10.

Derivatives of phenylacetic acid.

Diclofenac sodium (Diclofenac sodium).

It has a strong anti-inflammatory, analgesic and antipyretic effect, inhibits platelet aggregation.

Application: rheumatic diseases and other inflammatory and degenerative diseases of the joints.

Take 25 mg orally 2-3 times a day after meals, then increase the dose to 100-150 mg per day. IM - no more than 2 ampoules per day.

Side effects and contraindications: like indomethacin.

Product form: tablets 25 mg No. 30 and 10; solution for injection - 3 ml in ampoules No. 5 (1 ml contains 25 mg of the active substance).

Non-steroidal drugs - derivatives of propionic acid.

Propionic acid derivatives include: ibuprofen (Ibuprofenum), ketoprofen (Cetoprofen), fenoprofen (Phenoprofen), naproxen (Naproxen).

Ibuprofen (Ibuprofenum).

Pharmacological action, indications for use, side effects and contraindications: the same as indomethacin.

Product form: coated tablets, 0,2 No. 100.

5. Anthranilic acid derivatives

Main representatives: flufenamic acid (arleor) and its aluminum salt (opyrine); mefenamic acid (ponstan, ponstil); niflumic acid (donalgin). Mechanism of action: uncoupling of oxidative phosphorylation and inhibition of the activity of lysosomal enzymes.

Donalgin (Donalgin).

Non-steroidal anti-inflammatory drug. The active substance is niflumic acid.

Application: rheumatism, diseases of the musculoskeletal system, pain syndromes in fractures, inflammatory diseases of the ENT organs.

Mode of application: taken orally after meals, 250 mg 3 times a day, if necessary, the dose is increased to 1 g per day, the maintenance dose is 250-500 mg per day.

Side effects and contraindications: the same as indomethacin.

Product form: capsules 250 mg № 30.

Mefenamic acid (Acidum mefenamicum).

In terms of analgesic activity, it is equivalent to butadione and surpasses salicylates, and in antipyretic action it is equal to these drugs.

Indications, side effects and contraindications: characteristic of this group of drugs.

Product form: tablets of 0,25 and 0,5 g No. 50.

Oksinamy and drugs with a pronounced analgesic effect.

Oksinamy is a new class of non-specific anti-inflammatory drugs with a pronounced anti-inflammatory effect.

These include lornoxicam (xefocam) (Lornoxycam) (Xenofocam), meloxicam (Meloxycam) (Movalis) (Movalis), piroxicam (Piroxicam) (Hotemin, Toldin, Erazon, Roxicam, Felden), tenoxicam (Tabital, tenoctyl).

Piroxicam (Piroxicam).

A non-specific anti-inflammatory agent with a pronounced analgesic effect, it also has antipyretic properties.

Application, side effects and contraindications: the same as other nonsteroidal drugs, in addition, it also causes depression and drowsiness.

Product form: capsules of 10 and 20 mg No. 20.

Thoradol (Toradol).

Synonym: Ketanov. Its analgesic properties are similar to those of opioids.

Indications: Short-term relief of severe pain requiring anesthesia is similar in intensity to the use of drugs from the morphine group and its substitutes.

Mode of application: take 10 mg orally once, if necessary, every 6 hours; IM and IV are administered in a dose of 10-30 mg once. With repeated use - no more than 5 days.

Side effects: abdominal pain, dyspepsia, blurred vision, dizziness, sleep disturbance, bradycardia, hypertension, blood changes.

Contraindications: peptic ulcer of the stomach and duodenum; pregnancy, conditions with a high risk of bleeding.

Product form: tablets 10 mg No. 10; ampoules (in 1 ml 30 mg) No. 5.

6. Preparations of gold

The mechanism of the anti-inflammatory action of gold preparations is due to their immunomodulatory properties. These include: krizanol (Chrysanolum), auronofin (Auronofin), tauredon (Tauredon).

Crizanol (Krizanolum).

Contains from 33,5 to 35% gold.

Indications: rheumatoid arthritis.

Mode of application: administered intramuscularly once a week. A single dose is 1 ml of a 1% suspension (this is 5 mg of gold). The course of treatment is 17-58 injections.

Side effects: dermatitis, diarrhea, decreased hemoglobin levels, albuminuria, hematuria, leukopenia.

Contraindications: diseases of the liver and kidneys; systemic lupus erythematosus, fever, articular-visceral and septic forms of rheumatoid arthritis.

Product form: 2 ml ampoules of 5% suspension No. 25.

Auronofin (Auronofin).

A preparation containing gold for oral administration. It has anti-inflammatory and desensitizing effect.

Indications: rheumatoid arthritis.

Mode of application: prescribed orally for adults, 6 mg per day in 1 or 2 doses. Dose for children: 150 mcg/kg body weight per day. M.S.D. for children - 6 mg.

Side effects: diarrhea, stomach pain, rash, itching, stomatitis, conjunctivitis.

Contraindications: hypersensitivity to the drug, severe liver and kidney disease. Hematopoietic disorders, pregnancy, lactation.

Product form: tablets of 3 mg of auronofin No. 30.

tauredon (Turedon).

The gold content is about 46%. The active substance is sodium aurothiomalate. It causes inhibition of the antigen-initiated stimulation of lymphocytes, inhibition of monocytic granulocytic phagocytosis, stabilization of lysosomal membranes, strengthening of collagen fibers with the occupation of immunologically active sites that can provoke an autoimmune process.

Indications: rheumatoid arthritis, juvenile rheumatoid arthritis, psoriatic arthritis.

Mode of application: At the beginning of treatment, adults are prescribed 2 injections per week. From 1 to 3 injections, 10 mg is administered, from 4 to 6 injections - 20 mg. The total dose is 1600 mg (maximum 2000 mg). The maintenance dose is 100 mg per injection once a month or 1 mg once every 50 weeks.

Side effects: tachycardia, arrhythmia, nausea, abdominal pain, allergic reactions.

Contraindications: kidney and liver diseases, pregnancy, lactation, allergic reactions to the drug.

Product form: solution for injection: 0,5 ml in ampoules No. 10. 1 ampoule contains 10, 20, and 50 mg of the active substance.

LECTURE No. 10. Non-narcotic antitussive drugs. Vomiting and antiemetic drugs

1. Non-narcotic antitussives

This group includes drugs that are devoid of the side effects inherent in opioids.

There are drugs with a central action, acting on the cough center, and drugs with a peripheral action, when the sensitive receptors of the mucous membrane of the respiratory tract are inhibited.

Drugs with central action.

Tusuprex (Tusuprex).

It has a central antitussive effect, does not depress breathing, does not cause addiction and addiction.

Indications: acute cough of any etiology, whooping cough, to suppress cough during bronchoscopy.

Mode of application: prescribed orally for adults 20 mg 3-4 times a day, children under one year old - 5 mg 3-4 times a day, children over one year old - 5-10 mg 3-4 times a day.

Side effects: dyspepsia.

Contraindications: bronchial asthma, bronchospasm, bronchoctasia, bronchitis with sputum difficult to separate.

Product form: coated tablets of 0,01 and 0,02 g No. 30.

Glaucin (Glaucini hudrochloridum).

Works and applies in the same way as tusuprex.

Side effects: moderate hypotensive effect.

Contraindications: low blood pressure and myocardial infarction.

Product form: coated tablets, 0,05 g No. 20. List B.

Drugs with peripheral action.

Libeksin (Libexin).

It has a local anesthetic effect on the mucous membrane of the respiratory tract, causes some bronchodilator effect.

Indications: Acute and chronic bronchitis, bronchopneumonia, bronchial asthma, emphysema.

Mode of application: prescribed orally for adults 0,1 3-4 times a day, in severe cases - 0,2 3-4 times a day, for children - depending on age, 0,025-0,05 g 3-4 times a day.

Side effects: dry mouth, nausea, diarrhea, allergic reactions.

Contraindications: conditions after inhalation anesthesia, abundant secretion in the airways.

Product form: tablets of 0,1 g No. 20.

2. Emetics and antiemetics

Vomiting is most often a protective act aimed at freeing the stomach from irritating and toxic substances that have fallen into it.

Sometimes vomiting is a concomitant process that worsens the condition of the body and is caused by various factors. Often vomiting occurs as a result of overexcitation of the labyrinth apparatus. It is controlled by special structures of the medulla oblongata - the vomiting center and the so-called trigger zone.

Vomiting develops when the vomiting center is excited: with direct exposure to toxic or medicinal substances; with reflex excitation of centripetal pathways, as well as with the receipt of impulses from the chemoreceptors of the trigger zone. It is especially sensitive to the action of chemicals.

And the emetic, as well as antiemetic, effect of many medicinal substances is realized through primary stimulation or inhibition of this zone. Emetics are medications that cause vomiting when used. There are centrally acting emetics (apomorphine, Apomorphini hydrochloridum) and peripherally acting emetics (copper sulfate, Cuprum sulfatis), zinc sulfate.

Apomorphine (Apomorphini hydrochloridum).

A centrally acting emetic that stimulates the chemoreceptors of the trigger zone.

Indications: as an emetic, in chronic alcoholism to develop a reaction of aversion to alcohol.

Mode of application: injected s / c at 0,2-0,5 ml of a 1% solution.

Side effects: vascular collapse, tremor, convulsions, depression of the respiratory center.

Contraindications: severe cardiovascular disease, lung disease, peptic ulcer.

Product form: 1 ml ampoules of 1% solution No. 10. List A.

Antiemetic drugs.

Drugs from different pharmacological groups that act on the vomiting center, trigger zone, and also have a central and peripheral effect. These include m-anticholinergics, antihistamines, antipsychotics of the phenothiazine and butyrophenone groups, etc.

Dimetpramide (Dimetpramidum).

An antiemetic that blocks chemoreceptors in the trigger zone. Does not have a cumulative effect.

Indications. Vomiting of various origins.

Side effects: lowering blood pressure, drowsiness.

Contraindications: liver and kidney diseases with dysfunction, hypotension.

Product form: tablets 0,02 No. 50.

Motilium (Mottilium).

Antiemetic drug. Antagonist of peripheral and central dopamine receptors. Strengthens the peristalsis of the stomach, accelerates its emptying.

Application: nausea and vomiting of various origins. It is taken orally for 15-20 minutes, 20 mg 3-4 times during the day and at bedtime.

Side effects: spasms of the intestines, an increase in the level of prolactin in the blood plasma.

Contraindications: gastrointestinal bleeding, obstruction of the stomach or intestines, perforation of the stomach.

Product form: tablets 10 mg No. 30 and 10.

Cerucal (Cerucalum).

Antiemetic. Dopalien receptor antagonist. It has a regulating effect on the motor function of the gastrointestinal tract.

Application: nausea and vomiting of various origins, impaired motor function, atony and hypotension (after gastric resection) of the gastrointestinal tract. Take orally before meals 1-2 tablets 2-3 times a day, injected intramuscularly or intramuscularly 2-6 ml per day.

Side effects: drowsiness, fatigue, dizziness, spasm of the facial muscles, a tendency to depression.

Contraindications: bleeding from the gastrointestinal tract, perforation of the stomach and intestines, pyloric stenosis, intestinal obstruction, pheochromocytoma.

Product form: tablets of 10 mg No. 50, ampoules of 2 ml (in 1 ml of 0,005 g of the drug) No. 10.

LECTURE No. 11. Drugs acting on peripheral neurotransmitter systems. Means acting on peripheral cholinergic processes

1. Drugs acting primarily on peripheral neurotransmitter systems

In the peripheral nervous system, a distinction is made between afferent nerves - sensitive, carrying information to the central nervous system, and efferent nerves - centrifugal, through which coordination of the activities of internal organs is carried out from the central nervous system. Drugs acting on the peripheral nervous system are divided into two groups: drugs that affect efferent innervation and drugs that affect afferent innervation. Efferent, or centrifugal, nerves in the body are represented by:

1) somatic (motor), innervating skeletal muscles;

2) vegetative, innervating internal organs, glands, blood vessels.

Autonomic nerve fibers are interrupted on their way in special formations - ganglia, and the part of the fiber going before the ganglion is called preganglionic, and after the ganglion - postganglionic. All autonomic nerves are divided into sympathetic and parasympathetic, which perform different physiological roles in the body and are physiological antagonists. The transmission of excitation in synapses is carried out with the help of neurotransmitters, which can be adrenaline, norepinephrine, acetylcholine, dopamine, etc. In the transmission of excitation in the endings of peripheral nerves, the main neurotransmitter role is played by acetylcholine and norepinephrine. There are cholinergic (transmitter acetylcholine), adrenergic (transmitter adrenaline or norepinephrine) and dopaminergic (transmitter dopamine) synapses. Synapses have different sensitivity to drugs, and therefore all drugs are divided into two groups: drugs acting in the area of ​​cholinergic synapses, and drugs acting in the area of ​​adrenergic synapses. All these drugs can activate the process of synaptic transmission or, by stimulating the corresponding receptors, reproduce the effect of a natural transmitter. Such drugs are called mimetics (stimulants) - cholinomimetics and adrenergic agonists. If they inhibit the process of synaptic transmission or block receptors, they are called lytics (blockers) - anticholinergics and adrenolytics.

2. Means acting on peripheral cholinergic processes. M-cholinomimetics

Cholinergic synapses exhibit different sensitivity to drugs: synapses and receptors located in them and sensitive to muscarine are called muscarine-sensitive, or m-cholinergic receptors; to nicotine - nicotine-sensitive, or n-cholinergic receptors.

Acetylcholine, as a mediator for all cholinergic receptors, is a substrate for the action of the enzyme acetylcholinesterase, which catalyzes the hydrolysis of acetylcholine.

Cholinergics are divided into the following groups:

1) m-cholinomimetics (aceclidin, pilocarpine);

2) n-cholinomimetics (nicotine, cytiton, lobelin);

3) m-n-cholinomimetics of direct action (acetylcholine, carbachol);

4) m-n-cholinomimetics of indirect action, or anticholinesterase agents;

5) m-anticholinergics (atropine, scopolamine, platifillin, metacin);

6) n-cholinolytics:

a) ganglioblocking agents (hygronium, benzohexonium, pyrilene);

b) curare-like drugs (tubocurarine, ditilin);

7) Mr. anticholinergics (cyclodol).

M-cholinomimetics. With the introduction of these substances, the effects of excitation of the parasympathetic nervous system, bradycardia, lowering blood pressure (short-term hypotension), bronchospasm, increased intestinal motility, sweating, salivation, pupil constriction (miosis), decrease in intraocular pressure, spasm of accommodation are observed.

Aceclidine (Aceclidinum).

Active m-cholinomimetic agent with a strong miotic effect.

Indications: postoperative atony of the gastrointestinal tract and bladder, in ophthalmology - to narrow the pupil and lower intraocular pressure in glaucoma.

Mode of application: injected s / c 1-2 ml of a 0,2% solution. V. R. D. - 0,004 g, V. S. D. - 0,012. In ophthalmology, a 3-5% eye ointment is used.

Side effects: salivation, sweating, diarrhea.

Contraindications: angina pectoris, atherosclerosis, bronchial asthma, epilepsy, hyperkinesis, pregnancy, gastric bleeding.

Product form: 1 ml ampoules of 0,2% solution No. 10, ointment 3-5% in tubes of 20 g.

Pilocarpine hydrochloride (Pilocarpini hydrochloridum).

Lowers intraocular pressure in glaucoma. Stimulates peripheral m-cholinergic systems.

Indications: open-angle glaucoma, optic nerve atrophy, retinal vascular obstruction.

Mode of application: 1-2 drops of a 1% solution are injected into the conjunctival sac 3 times a day, if necessary - a 2% solution.

Side effects: persistent spasm of the ciliary muscle.

Contraindications: iritis, iridocyclitis, other eye diseases where miosis is undesirable.

Product form: eye drops 1-2% in bottles of 1, 5, 10 ml, in a tube-dropper of 1,5 ml No. 2.

3. N-cholinomimetics

N-cholinomimetics excite n-cholinergic receptors of the carotid glomerulus and partly of the chromaffin tissue of the adrenal glands, which leads to a reflex increase in the tone of the respiratory and vasomotor centers, and an increase in the release of adrenaline. A typical representative that excites both peripheral n-cholinergic receptors and n-cholinergic receptors of the central nervous system is nicotine. The action of nicotine is two-phase: small doses excite, large ones inhibit n-cholinergic receptors. Nicotine is very toxic, therefore, it is not used in medical practice, but only lobelin and cytiton are used.

Lobeline hydrochloride (Lobelini hydrochloridum).

Respiratory analeptic.

Indications: weakening or reflex respiratory arrest, asphyxia of newborns.

Mode of application: 0,3-1 ml of a 1% solution is administered intramuscularly and intravenously; for children, depending on age, 0,1-0,3 ml of a 1% solution.

Side effects: in case of overdose, excitation of the vomiting center, cardiac arrest, respiratory depression, convulsions.

Contraindications: severe damage to the cardiovascular system, respiratory arrest when the respiratory center is depleted.

Product form: 1 ml ampoules of 1% solution No. 10.

Cititon (Cytitonum).

Cytisine alkaloid acts like lobelin. Increases blood pressure by stimulating n-cholinergic receptors of sympathetic ganglia and adrenal glands.

Indications: asphyxia, shock, collapse, respiratory and circulatory depression in infectious diseases.

Mode of application: injected in/in and/m 0,5-1 ml. V. R. D. - 1 ml, V. S. D. - 3 ml.

Side effects: nausea, vomiting, slow heart rate.

Contraindications: hypertension, atherosclerosis, pulmonary edema, bleeding.

Product form: in ampoules of a 5% solution of 1 ml No. 10. This group includes combined preparations, which include n-cholinomimetics and are used to stop smoking.

Tabex (Tabex).

One tablet contains 0,0015 cytisine, 100 tablets per pack.

Lobesil (Lobesyl).

One tablet contains 0,002 lobeline hydrochloride, 50 tablets per pack.

Anabasine hydrochloride (Anabazini hydrochloridum).

Available in tablets of 0,003 in the form of chewing gum. All drugs are stored according to the list B.

4. Anticholinesterase agents

There are anticholinesterase agents of reversible action (physostigmine, prozerin, oksazil, galantamine, kalimin, ubretide) and irreversible action (phosphacol, armine), the latter being more toxic. This group includes some insecticides (chlorophos, karbofos) and chemical warfare agents (tabun, sarin, soman).

Prozerin (Prozerinum).

It has a pronounced anticholinesterase activity.

Indications: myasthenia gravis, paresis, paralysis, glaucoma, atony of the intestines, stomach, bladder, as an antagonist of muscle relaxants.

Mode of application: take 0,015 g orally 2-3 times a day; 1 ml of 0,05% solution is administered subcutaneously (1-2 ml of solution per day), in ophthalmology - 1-2 drops of 0,5% solution 1-4 times a day.

Side effects: bradycardia, hypotension, weakness, hypersalivation, bronchorrhea, nausea, vomiting, increased skeletal muscle tone.

Contraindications: epilepsy, bronchial asthma, organic heart disease.

Product form: tablets of 0,015 g No. 20, ampoules of 1 ml of a 0,05% solution No. 10.

Kalimin (Kalymin).

Less active than prozerin, but longer acting.

Application: myasthenia gravis, motor activity disorders after trauma, paralysis, encephalitis, poliomyelitis.

Mode of application: prescribed orally 0,06 g 1-3 times a day, administered intramuscularly - 1-2 ml of 0,5% solution.

Side effects: hypersalivation, miosis, dyspepsia, increased urination, increased tone of skeletal muscles.

Contraindications: epilepsy, hyperkinesis, bronchial asthma, organic heart disease.

Product form: dragee 0,06 g No. 100, 0,5% solution in 1 ml ampoules No. 10.

Ubretide (Ubritid).

Long-acting anticholinesterase drug.

Application: atony and paralytic ileus of the intestines, bladder, atonic constipation, peripheral paralysis of skeletal muscles.

Side effects: nausea, diarrhea, abdominal pain, salivation, bradycardia.

Contraindications: hypertonicity of the gastrointestinal tract and urinary tract, enteritis, peptic ulcer of the stomach and duodenum, diseases of the cardiovascular system, bronchial asthma.

Product form: 5 mg tablets No. 5, injection solution in ampoules (1 ml contains 1 mg of ubretide) No. 5.

Armin (Arminum).

Active anticholinesterase drug of irreversible action.

Application: miotic and antiglaucoma agent.

Mode of application: prescribe a 0,01% solution of 1-2 drops in the eye 2-3 times a day.

Side effects: pain in the eye, hyperemia of the mucous membrane of the eye, headaches.

Product form: in a bottle of 10 ml of 0,01% solution. In case of overdose and poisoning, the following symptoms are observed: bronchospasm, a sharp drop in blood pressure, a slowdown in cardiac activity, vomiting, sweating, convulsions, a sharp constriction of the pupil and a spasm of accommodation. Death can occur from respiratory arrest. Help in case of poisoning: gastric lavage, artificial respiration, administration of drugs that normalize the function of the cardiovascular system, etc. In addition, anticholinergics (atropine, etc.), as well as cholinesterase reactivators, drugs - dipyroxime or isonitrozine are prescribed.

dipyroxime (Dipyroxym).

Used for poisoning with anticholinesterase drugs, especially phosphorus-containing ones. Can be prescribed together with m-anticholinergics. Administer once (s.c. or i.v.), in severe cases - several times a day. Available in ampoules in the form of a 15% solution of 1 ml.

Isonitrosin (Izonitrosyn) - similar in action to dipyroxime. Available in ampoules of 3 ml of 40% solution. Administer 3 ml intramuscularly (in severe cases - intravenous), repeat if necessary.

5. M-cholinolytics

The drugs of this group block the transmission of excitation in m-cholinergic receptors, making them insensitive to the mediator acetylcholine, resulting in effects opposite to the action of parasympathetic innervation and m-cholinomimetics.

M-anticholinergics (drugs of the atropine group) suppress the secretion of salivary, sweat, bronchial, gastric and intestinal glands. The secretion of gastric juice decreases, but the production of hydrochloric acid, the secretion of bile and pancreatic enzymes decrease slightly. They dilate the bronchi, reduce the tone and peristalsis of the intestines, relax the biliary tract, reduce the tone and cause relaxation of the ureters, especially with their spasm. Under the action of m-anticholinergics on the cardiovascular system, tachycardia, increased heart rate, increased cardiac output, improved conduction and automatism, and a slight increase in blood pressure occur. When introduced into the cavity, the conjunctiva causes pupil dilation (mydriasis), an increase in intraocular pressure, accommodation paralysis and dryness of the cornea. According to the chemical structure, m-anticholinergics are divided into tertiary and quaternary ammonium compounds. Quaternary amines (matatsin, chlorosil, propanteline bromide, furomegane, ipratropium bromide, troventol) penetrate poorly through the blood-brain barrier and exhibit only a peripheral anticholinergic effect.

Atropine sulfate (Atropini sulfas).

It has m-anticholinergic activity. It blocks the m-cholinergic systems of the body.

Application: peptic ulcer of the stomach and duodenum, spasms of blood vessels in internal organs, bronchial asthma, in ophthalmology - to dilate the pupil.

Mode of application: prescribed orally at 0,00025-0,001 g 2-3 times a day, subcutaneously at 0,25-1 ml of a 0,1% solution, in ophthalmology - 1-2 drops of a 1% solution. V.R.D. - 0,001, V.S.D. - 0,003.

Side effects: dry mouth, tachycardia, blurred vision, intestinal atony, difficulty urinating.

Contraindications: glaucoma.

Product form: ampoules of 1 ml of 0,1% solution No. 10, eye drops (1% solution) of 5 ml, powder. List A.

Metacin (Methacinum).

Synthetic m-anticholinergic, superior in activity to atropine.

Application, side effects, contraindications: the same as for atropine.

Mode of application: appoint inside at 0,002-0,004 g 2-3 times a day, parenterally at 0,5-2 ml of a 0,1% solution.

Product form: tablets of 0,002 No. 10, ampoules of 1 ml of a 0,1% solution No. 10. Combined preparations containing m-cholinolytics: bellataminal, bellaspon, belloid, besalol, bellalgin. Assign 1 tablet 2-3 times a day for intestinal cramps, increased acidity of gastric juice and others; suppositories (betiol and anuzol) are used for hemorrhoids and rectal fissures.

6. N-cholinolytics

A group of drugs that selectively block n-cholinergic receptors of the autonomic ganglia, the carotid sinus zone and the adrenal medulla is called ganglion blockers, and a group that blocks n-cholinergic receptors of neuromuscular synapses is called muscle relaxants, or curare-like drugs.

Ganglioblocking agents, blocking the n-cholinergic receptors of the autonomic ganglia, cause a number of characteristic changes:

1) dilate blood vessels and reduce blood pressure, reduce the release of adrenaline, reduce impulses to the vasomotor center from the carotid glomerulus, dilate the vessels of the lower extremities and improve their blood circulation. Short-acting ganglioblockers are used for pulmonary and cerebral edema, as well as for controlled hypotension during operations in order to reduce blood loss;

2) reduce the tone of the smooth muscles of the internal organs and reduce the secretion of glands;

3) have a stimulating effect on the muscles of the uterus, such as pahikarpin.

Ganglioblockers of short action.

Hygronium (Hygronium).

Application: in anesthesiology to create artificial hypotension. Enter in/in (drip) 0,01% solution in isotonic sodium chloride solution or 5% glucose solution.

Side effects: severe hypotension.

Product form: powder of 0,1 g in an ampoule with a capacity of 10 ml No. 10. List B.

Long acting ganglionic blockers.

Benzohexonium (Benzohezonium).

Application: spasm of peripheral vessels, hypertension, hypertensive crises, bronchial asthma, peptic ulcer of the stomach and duodenum. Prescribed orally 0,1-0,2 g 2-3 times a day, subcutaneously, intramuscularly - 1-1,5 ml of a 2,5% solution. V.R.D. - orally 0,3 g; V.S.D. - 0,9 g; SC single - 0,075 g, daily - 0,3 g.

Side effects: general weakness, dizziness, palpitations, orthostatic collapse, dry mouth, bladder atony.

Contraindications: hypotension, severe damage to the liver and kidneys, thrombophlebitis, severe changes in the central nervous system.

Product form: tablets of 0,1 g No. 20, ampoules of 1 ml of a 2,5% solution No. 10.

Pentamine (Pentaminum).

Indications for use, side effects and contraindications: similar to benzohexonium.

Product form: in ampoules of 1 and 2 ml of a 5% solution.

Pachycarpine hydroiodide (Pachycarpini hydroiodidum).

Application: with spasms of peripheral vessels and to stimulate labor, to reduce bleeding in the postpartum period. Assign inside, p / c, in / m.

Contraindications: pregnancy, severe hypotension, liver and kidney disease.

Product form: available in tablets of 0,1 g, ampoules of 2 ml of a 3% solution. Released only by prescription. List B. The same group includes pyrilene (Pirilenum) and temechin (Temechinum) tablets of 0,005 g each.

7. Curariform drugs

Curare-like substances block n-cholinergic receptors of skeletal muscles and cause relaxation of skeletal muscles (muscle relaxants). According to the mechanism of action, they are divided into substances:

1) antidepolarizing (competitive) type of action (tubocurarine, diplacin, meliktin);

2) depolarizing type of action (ditilin);

3) mixed type of action (dioxonium).

According to the duration of action, muscle relaxants are divided into three groups:

1) short-acting (5-10 min) - ditilin;

2) medium duration (20-40 min) - tubocurarine chloride, diplacin;

3) long-acting (60 minutes or more) - anatruxonium.

tubocurarine chloride (Tubocurarinini-chloridum).

It is a curare-like drug with antidepolarizing action.

Application: in anesthesiology to relax muscles. Administered intravenously at 0,4-0,5 mg/kg. During surgery, the dose is up to 45 mg.

Side effects: possible respiratory arrest. To weaken the effect of the drug, prozerin is administered.

Contraindications: myasthenia gravis, pronounced disorders of the kidneys and liver, senile age.

Product form: in 1,5 ml ampoules containing 15 mg of preparation No. 25.

Ditilin (Dithylinum) listenone (Lysthenon).

Synthetic depolarizing short-acting muscle relaxants.

Application: tracheal intubation, surgical interventions, reduction of dislocations. It is administered intravenously at the rate of 1-1,7 mg/kg of the patient's body weight.

Side effects: possible respiratory depression.

Contraindications: glaucoma. Ditilin solutions should not be mixed with barbiturates and donated blood.

Product form: 5 ml ampoules of 2% solution No. 10.

In anesthesiology practice, other drugs are also used: arduan (Arduan), pavulon (Pavulon), norcuron (Norcuron), trakrium (Tracrium), melliktin (Mellictin). M-, n-anticholinergics have a blocking effect on m- and n-cholinergic receptors. Among them are substances that block predominantly peripheral m- and n-cholinergic receptors (peripheral m-, n-anticholinergics, or antispasmodics) and have an antispasmodic effect. These are spasmolitin, tifen, etc. There are also drugs that penetrate the blood-brain barrier and block m- and n-cholinergic receptors of the central nervous system, used to treat mainly Parkinson's disease (cyclodol, dinezin). In addition, there are drugs that have a central and peripheral m- and n-anticholinergic effect, such as aprofen.

Spasmolitin (Spasmolythin).

Peripheral m-, n-anticholinergic, which has an antispasmodic effect.

Application: endarteritis, pylorospasm, spastic colic, peptic ulcer of the stomach and duodenum. Prescribed orally, after meals, 0,05-0,1 2-4 times a day, intramuscularly - 5-10 ml of a 1% solution.

Side effects: dry mouth, headache, dizziness, epigastric pain, local anesthesia.

Contraindications: glaucoma, work that requires a quick mental and physical reaction.

Product form: powder.

LECTURE No. 12. Means acting on peripheral adrenergic processes

1. Adrenergics

Adrenergic agents are medicinal substances that affect adrenergic synapses located in the area of ​​​​the end of the sympathetic nerves. Since adrenoreceptors are divided into several types (α- and β-) and α-adrenergic receptors are postsynaptic α1, presynaptic and postsynaptic α2, and among β-adrenergic receptors similar β1- and β2-adrenergic receptors are distinguished, all means that affect the transmission of excitation to adrenergic synapses are divided into three main groups:

1) excitatory adrenergic receptors - adrenomimetics;

2) blocking adrenergic receptors - adrenoblockers (adrenolytics);

3) affecting the metabolism, deposition and release of the mediator (sympatholytics).

Adrenomimetics are agents that stimulate adrenoceptors. According to the action on a certain type of adrenergic receptors, adrenomimetics are divided into three groups:

1) predominantly stimulating α-adrenergic receptors (α-adrenergic agonists);

2) predominantly stimulating β-adrenergic receptors (β-agonists);

3) stimulating α- and β-adrenergic receptors (α-, β-agonists).

α- adrenomimetics.

This group includes norepinephrine, the main mediator of adrenergic synapses, secreted by the adrenal medulla and having a predominantly stimulating effect on α-adrenergic receptors, to a small extent on β1-adrenergic receptors and less on β2-adrenergic receptors.

Norepinephrine hydrotartate (Noradrenaiini hydrotartas).

Stimulates α-adrenergic receptors, has a strong vasopressor effect, stimulates heart contraction, has a weak bronchodilator effect.

Application: acute decrease in blood pressure in trauma, surgery, poisoning, cardiogenic shock. Introduce / in (drip) 2-4 mg of the drug (1-2 ml of a 0,2% solution) in 500 ml of a 5% glucose solution.

Side effects: headache, chills, palpitations, if it gets under the skin, necrosis is possible.

Contraindications: fluorotan anesthesia. Caution is required in severe atherosclerosis, circulatory failure, complete atrioventricular blockade.

Product form: 1 ml of 0,2% solution No. 10. List B.

Mesatone (Mesatonum).

It acts predominantly on α-adrenergic receptors, it is more stable than norepinephrine, and is effective when administered orally, intravenously, intramuscularly, s / c and topically. It is used in the same way as norepinephrine.

Side effects and contraindications: the same.

Product form: powder and ampoules of 1 ml of 1% solution. List B.

Fetanol (Phetanolum).

Increases blood pressure compared to mezaton for a longer period.

Application, side effects and contraindications: the same as the mezaton.

Product form: powder, tablets of 0,005 g, in ampoules of 1 ml of a 1% solution.

Naftizin (Napthyzinum).

Synonym: Sanorine.

Application: acute rhinitis, sinusitis, allergic conjunctiva. The vasoconstrictor effect is longer than that of norepinephrine and mezaton, and the sanorin emulsion acts longer than an aqueous solution of naphthyzinum.

Product form: vials of 10 ml of a 0,05-0,1% solution.

Galazolin (Halazolinum).

Close to naphthyzinum in action and application.

2. β-agonists

The drugs of this group have a direct excitatory effect on β1- or β1- and β2-adrenergic receptors. Stimulation of β2-adrenergic receptors, has a rapid and pronounced bronchodilator effect, reduces swelling of the bronchial mucosa. Increases the functional activity of β1-receptors in the myocardium, enhances cardiac activity.

Isadrin (Isadrinum).

Application: emphysema, bronchial asthma, pneumosclerosis. Prescribed orally 1-2 tablets 3-4 times a day sublingually, in the form of inhalations - 0,5-1 ml of a 0,5-1% solution 2-4 times a day.

Side effects: tachycardia, arrhythmia, nausea.

Contraindications: severe atherosclerosis, arrhythmia, pain in the region of the heart.

Product form: tablets of 0,005 g No. 20; in ampoules of 1 ml of a 0,5% solution No. 5, an aerosol of 25 g each. List B.

Alupent (Alupent).

Close to izadrinu, but with bronchial asthma acts longer.

Product form: 1 ml ampoules of a 0,05% solution and 20 ml vials of a 2% solution for an aerosol containing 400 single doses, tablets of 0,02 g.

Synonym: Astmopent.

Product form: vials of 20 ml of a 1,5% solution for an aerosol containing 200 and 400 single doses.

Dobutamine (Dobutaminum).

Increases coronary blood flow, improves blood circulation.

Side effects: Tachycardia, arrhythmia, increased blood pressure, pain in the heart, nausea.

Contraindications: subaortic stenosis.

Product form: vials of 20 ml (250 mg dobutamine). Enter in / in, previously dissolved in a 0,9% sodium chloride solution.

Fenoterol (Fenoterolum).

Synonyms: Berotek. Close to Asthmopent, but longer acting. Better tolerated.

Application: bronchial asthma.

Product form: aerosol with a metering valve, one press - 0,2 mg of the drug; 1 breath 2-3 times a day. Under the name partusisten (partusisten) is used as a means of relaxing the muscles of the uterus.

Salbutamol (Salbutamolum).

Synonym: Ventolin. Gives a pronounced bronchodilator effect. Reception: inside and inhalation with bronchial asthma.

Product form: aerosol cans and tablets of 0,002 g.

α- And β- adrenomimetics.

These drugs improve the conduction of the nerve impulse in the postganglionic synapses of sympathetic nerve fibers. The main effects are associated with a direct or indirect stimulating effect on both α- and β-adrenergic receptors.

Adrenaline hydrochloride (Adrenalini hydrochloridum).

Used for bronchial asthma, hypoglycemia, allergic reactions 1,0 ml of 0,1% solution, for acute cardiac arrest - intracardiacly, for glaucoma - 1-2% solution in drops.

Side effects: tachycardia, increased cardiac output, increased blood pressure, deterioration in myocardial oxygen supply.

Contraindications: arterial hypertension, severe atherosclerosis, diabetes mellitus, thyrotoxicosis, pregnancy, angle-closure glaucoma.

Ephedrine hydrochloride (Ephedrini hydrochloridum).

Works weaker, but longer.

Application: bronchial asthma, allergic diseases, poisoning with sleeping pills, drugs, hypotension, enuresis, trauma, blood loss, infectious diseases, myasthenia gravis. Locally as a vasoconstrictor, to dilate the pupil for diagnostic purposes. Assign inside of 0,025 g 2-4 times a day.

Enter parenterally (0,5-1,0 ml of a 5% solution) and drip (2 ml of a 5% solution in 500 ml of a 5% glucose solution or 0,9% sodium chloride solution). Do not take at the end of the day or before bed.

Side effects: palpitations, nausea, sweating, insomnia, nervous excitement, urinary retention, rash, trembling of the limbs.

Contraindications: hypertension, atherosclerosis, severe organic heart disease, hyperthyroidism, insomnia.

Product form: tablets of 0,025 No. 10, ampoules of 2, 3 and 5% solution of 1 ml. List A.

Ephedrine is part of the tablets "Teofedrin" (Teophedrinum) and the drug "Solutan" (Solutan).

3. Antiadrenergic drugs. Adrenoblockers

Blocking the transmission of nervous excitation in the area of ​​​​adrenergic receptors can be carried out in different ways:

1) blocking adrenoreceptors (pharmacological substances with such properties are called adrenoblockers, or adrenolytics);

2) a violation of the accumulation and release of the neurotransmitter by nerve endings. This effect is carried out by sympatholytic substances or sympatholytics;

3) violation of the mediator formation process.

Unlike ganglionic blockers, antiadrenergic substances interrupt the conduction of efferent nerve excitation by acting on postganglionic synapses without affecting the transmission of excitation in the ganglia. Adrenoblocking substances, depending on the predominance of their effect on α- or β-adrenergic receptors, are divided into two groups:

1) α-blockers;

2) β-blockers.

In turn, α-blockers are divided into α1 blockers, which include phentolamine, tropafen, pyrroxane and others, α2-adrenergic blockers (yohimbine).

β-blockers are divided depending on the presence of their so-called sympathomimetic activity into:

1) β-blockers without internal sympathomimetic activity (propranolol, atenolol, timolol, etc.), which significantly reduce cardiac output and heart rate;

2) β-blockers with moderate internal sympathomimetic activity (oxeprenolol, alprenolol, acebutalol), slightly reducing cardiac output and heart rate;

3) β-blockers with pronounced internal sympathomimetic activity (pindolol or visken), which have little effect on cardiac output and heart rate. α- and β-adrenergic receptor blockers - labetolol. β-adrenergic receptor blockers: anaprilin, (obzidan), oxprenolol, talinolol (kordanum), metaprolol. In addition, in this group there are so-called cardioselective β1-blockers, which exhibit a selective effect on the heart (atenolol, metoprolol, practolol), used for tachyarrhythmia, angina, and hypertension. β2-adrenergic receptor blockers (timolol) reduce the production of intraocular fluid and are effective for glaucoma and some types of tremor; have a vasodilatory effect mediated through β2-adrenergic receptors.

4. α-blockers

These drugs block the transmission of excitation to α1- and α2-adrenergic receptors. The drugs of this group are used for diseases that occur against the background of hyperadrenalemia: pheochromocytoma, migraine, cerebrovascular accident, endarteritis, Raynaud's disease, acrocyanosis, the initial stages of atherosclerotic gangrene, trophic ulcers of the extremities, bedsores, sluggishly healing wounds, hypertension, hypertensive crises.

α1, α2-blockers (non-selective action).

Dihydroergotamine (Dihydroergotamine).

It is an antiadrenergic agent, lowers vascular tone.

Application: migraine, coronary spasm, Raynaud's disease.

Mode of application: appoint inside 10-20 drops in 0,5 cups of water 1-3 times a day.

Side effects: with increased sensitivity, dyspeptic phenomena are observed.

Contraindications: severe atherosclerosis, hypotension, organic heart disease, myocardial infarction, impaired liver and kidney function, old age.

Product form: vials of 10 ml of a 0,2% solution. List B.

Phentolamine (Phentolamin).

α-blocker, dilates peripheral vessels, slightly reduces blood pressure, has a pronounced hypotensive effect in pheochromocytoma.

Application: endarteritis, Raynaud's disease, hypertensive crises, diagnosis and surgical removal of pheochromocytoma.

Mode of application: prescribed orally after meals, 0,05 g 3-4 times a day, possibly up to 0,1 g 3-5 times a day.

Side effects: tachycardia, dizziness, nausea, vomiting, diarrhea, swelling of the nasal mucosa, skin itching.

Contraindications: severe organic lesions of the cardiovascular system.

Product form: tablets of 0,025, ampoules containing 0,005 g of the drug.

α1-blockers (selective action).

Prazosin (Prazosin).

It inhibits the enzyme phospholinesterase, which helps to relax vascular smooth muscles.

Application: arterial hypertension, congestive heart failure.

Mode of application: prescribed orally 0,5 mg 1 time a day (before bedtime), up to 1 mg 3-4 times a day. For congestive heart failure - up to 3-20 mg per day in 3-4 doses.

Side effects: collapse, dizziness, insomnia, depression, weakness, dry mouth.

Contraindications: pregnancy, kidney disease, age up to 12 years.

Product form: tablets of 0,001, 0,002, 0,005 g No. 50.

5. β-blockers

They inhibit the conduction of a nerve impulse due to the inhibition of β1- and β2-adrenergic receptors. β1-, β2-blockers (non-selective action).

Anaprilin (Anaprillin).

Synonyms: Obsidan, Inderal, Propranolol.

It inhibits β1- and β2-adrenergic receptors, has antianginal, antiarrhythmic and hypotensive effects.

Application: arterial hypertension, angina pectoris, sinus arrhythmia, tachycardia, thyrotoxic crisis. Assign inside 10 mg 3 times a day, gradually increasing the dose to 20-40 mg 3-4 times a day (sometimes up to 200 mg per day).

Side effects: weakness, bradycardia, hypotension, bronchospasm, nausea, diarrhea, sleep disturbance, agitation, depression.

Contraindications: myocardial infarction, hypotension, bronchial asthma, conduction disorders, Raynaud's disease and other obliterating vascular diseases.

Product form: tablets of 0,01 and 0,04 g No. 50, ampoules of 5 ml of a 0,25% solution No. 10.

Oxprenolol (Oxprenololum), synonyms: Trasicor, Coretal.

Close to anaprilin, but has a less pronounced effect on the strength and frequency of heart contractions.

Application: angina pectoris, arrhythmia, hypertension.

Product form: tablets of 0,02. Take 1 tablet 2-3 times a day (you can take up to 2-3 tablets 2-3 times a day).

Pindolol (Pindololum).

Synonym: Visken. Non-cardioselective β-blocker. Has internal sympathomimetic activity. Close to oxprenolol, but somewhat inferior to propranolol. It has antianginal, antiarrhythmic and hypotensive effects. Ingestion of 0,005 g 3 times a day 30 minutes after meals, parenterally administered in / in for 5 minutes 0,4 mg (2 ml of a 0,02% solution).

Side effects and contraindications: like anaprilin.

Product form: tablets 5 mg No. 30; 5 ml ampoules of 0,02% solution No. 5.

Nadolol (Nadololum).

Synonym: Corgard. β-blocker of non-selective action.

Application: ischemic heart disease, early stages of hypertension.

Side effects: dysfunction of the gastrointestinal tract, bradycardia, insomnia.

Contraindications: bronchial asthma, blockade and heart defects, diseases of the liver, kidneys, pregnancy. Produced in tablets of 0,04 and 0,08 g, it is prescribed 2 tablets 1 time per day.

Timolol (Timololum).

Close to anaprilin.

Application: glaucoma (tachyphylaxis is possible), appoint 1 drop 2 times a day.

Product form: bottles of 3 and 5 ml of a 0,5% solution.

β1-blockers (selective action).

Kordanum (Cordanum), synonymous with (Talinolol).

Reduces myocardial contractility and cardiac output.

Application: cardiac ischemia, arterial hypertension, cardiac arrhythmia - 50 mg 3 times a day, up to 300 mg per day.

Side effects: headache, nausea, dizziness.

Contraindications: heart failure, cardiogenic shock, impaired conduction of the heart and peripheral circulation, diseases of the bronchi and lungs.

Product form: dragee 50 mg № 50.

This group includes drugs with a duration of action of up to 6 hours (metoprolol - Metopolol) and up to 24 hours (atenolol - Atenolol, acebutanol - Acebutanol).

6. Sympatholytics

Sympatholytic drugs disrupt the deposition of norepinephrine, as well as its release from the endings of sympathetic nerve fibers. Sympatholytics include reserpine, raunatin, isobarine, ornid, dopegyt, methyldopa.

Reserpine (Reserpinum), synonyms: Rausedil, Serpasil.

It has a hypotensive and sedative effect.

Application: hypertension, mental illness of vascular etiology, psychosis against the background of high blood pressure.

Mode of application: appoint orally 0,1-0,25 mg per dose up to 1 mg per day, V. R. D. - 1 mg, V. S. D. - 2 mg. It is recommended to alternate with other antihypertensive drugs.

Side effects: hyperemia of the mucous membranes of the eyes, dyspepsia, bradycardia, depression, dizziness.

Contraindications: peptic ulcer of the stomach and duodenum, kidney disease with impaired function, organic diseases of the cardiovascular system.

Product form: tablets of 0,1 mg, 0,25 mg No. 50. Rausedil - ampoules of 1 ml of a 0,1-0,25% solution. Included in the combined preparations: Adelfan, Trirezide, Christepin (Brinerdine), Adelfan-Esidrexa, Adelfan-Esidrexa-K.

Raunatin (Raunatinum), synonym: Rauwasan (Rauwasan).

Contains the sum of alkaloids of rauwolfia serpentine roots. It has a hypotensive, antiarrhythmic, sedative effect. Similar in action to reserpine.

Application: hypertonic disease.

Side effects: sweating, weakness, pain in the heart.

Contraindications: hypotension.

Product form: tablets of 0,002 g, pills of rauvazana 0,002 each. It is prescribed 1 tablet (pellets) 3 times a day, not more than 6 tablets (pellets) per day. List B.

Oktadin (Octadinum), synonyms: Isobarin, Gaunethidine Sulfate, Ismelin.

It has a pronounced hypotensive effect, which is preceded by a small (from several minutes to an hour) hypertensive reaction when administered parenterally. The effect of oktadin on the eye is manifested in the narrowing of the pupil and a decrease in intraocular pressure. Oktadin slightly increases the motility of the gastrointestinal tract.

Apply for the treatment of hypertension, rarely glaucoma.

Side effects: dysfunction of the gastrointestinal tract, bradycardia.

Product form: tablets and dragees of 0,025 g. It is prescribed 1 tablet 3 times a day with blood pressure control.

Ornid (Ornidum).

Synonym: Bretylii tosilas. It blocks the presynaptic membrane and disrupts the release of norepinephrine, and also inhibits the reuptake of norepinephrine. The duration of action is 6-8 hours, it has a hypotensive and antiarrhythmic effect.

Application: arrhythmia, hypertensive crises.

Side effects: nausea, dizziness, blurred vision, addiction is possible.

Contraindications: atherosclerosis, myocardial infarction, cerebrovascular accident.

Product form: ampoules of 1 ml of a 5% solution. It is prescribed in / m at 0,1-05 ml 2-3 times a day. List B.

Methyldopa (Methyldopa) dopegit (Dopegyt) aldomet (Aldomet).

Violates the formation of the norepinephrine mediator, acts on enzyme systems, promotes the formation of a less active biological compound, has a hypotensive and slight sedative effect.

Application: hypertonic disease. Treatment is started with 0,25-0,5 g, increasing the dose to 0,75-1 g, and if the effect is insufficient - to 1,5-2,0 g per day. Combined with saluretics and antihypertensive drugs.

Side effects: headache, nausea, vomiting, leukopenia.

Contraindications: diseases of the liver, hematopoietic organs, pheochromocytoma, pregnancy.

Product form: tablets of 0,25.

LECTURE 13. Dopamine and dopaminergic drugs

1. Dopamine

Dopamine - a biogenic amine formed from l-tyrosine and which is a precursor of norepinephrine and adrenaline and a mediator that interacts with α- and β-adrenergic receptors, as well as with specific receptors, called dopamine receptors and located in various areas of the body. Many dopamine receptors in various areas of the CNS. They can be divided into presynaptic and postsynaptic. In addition, postsynaptic dopamine receptors can be divided into d1, associated with the action of dopamine on the activity of the adenylate cyclase enzyme, and d2, not associated with this action. Depending on the degree of dopamine stimulation or blocking of these receptors by antipsychotics, they are divided into four types: d1-d4. Substances that stimulate dopamine receptors are called dopaminomimetics, or dopamine receptor agonists, and substances that block dopamine receptors are called dopamine lytics, or dopamine receptor antagonists.

Dopaminomimetics.

These substances are divided into two groups:

1) indirect action, affecting presynaptic dopamine receptors that regulate the synthesis and release of dopamine and norepinephrine;

2) direct action, affecting postsynaptic dopamine receptors.

The first group of indirect action from domestic drugs includes levodopa, midantan and others that stimulate the synthesis of dopamine and presumably delay its destruction, promote the release of dopamine from the granules of presynaptic endings, used to treat Parkinson's disease.

The second group - psychostimulants with dopaminergic properties (phenamine (amphetamine)), facilitating the release of dopamine and norepinephrine from the granules of presynaptic nerve endings and inhibiting the activity of MAO and the reverse neuronal uptake of dopamine. Meridil (methylphenidate) is a psychostimulant that has the ability to release dopamine from the granules of presynaptic nerve endings. The psychostimulant centedrin and other drugs are similar in action.

Dophanomimetics of direct action and dofanominolytics.

Dopamine (Dofaminum).

Stimulant of direct action on dopamine receptors. It increases the strength of heart contractions and the level of blood pressure, increases cardiac output, reduces the resistance of the renal vessels, increasing blood flow in them, as well as diuresis.

Application: shock of various etiologies, acute cardiovascular and renal failure, cardiac surgery.

Mode of application: administered intravenously, pre-dissolved in a 5% glucose solution or 0,9% sodium chloride solution (1 ml should contain 500 mcg of dopamine). Infusions are carried out continuously - from 2-3 hours to 1-4 days under monitor supervision. The average daily dose is 800 mcg.

Side effects: spasm of peripheral vessels, tachycardia, ventricular extrasystole, respiratory failure, headache, agitation.

Contraindications: pheochromoacytoma, monoamine oxidase inhibitors, anesthetics.

Product form: 5 ml ampoules of 0,5% solution No. 10. List B.

2. Dopaminergic drugs

Parlodel (Parlodelum).

Synonym: Bromocriptinum. Activates dopamine receptors, inhibits the secretion of the hormone of the anterior pituitary gland prolactin, without affecting other pituitary hormones. Reduces the content of growth hormone in the blood, reduces the secretion of ACTH, suppresses physiological lactation. It is used for amenorrhea and infertility associated with an increased content of prolactin, to suppress lactation, with Itsenko-Cushing's disease and Parkinson's disease.

Mode of application: taken with meals for galactorrhea, prolactin-dependent amenorrhea, infertility from 1/2 tablet 2-3 times a day to 1 tablet 2-3 times a day. Treatment is continued until milk secretion completely stops and the menstrual cycle normalizes. For acromegaly: from 1 tablet per day (1-2 weeks) to 4-8 tablets per day in equal doses every 6 hours. For Parkinson's disease, the effect occurs at doses of 10-15 mg per day. In combination with levodopa - lower doses. The initial dose is 2,5 mg 2 times a day with a gradual increase in the dose to 5 mg, while simultaneously reducing the dose of levodopa or discontinuing it. For Itsenko-Cushing's disease - 3 tablets per day, then up to 1-2 tablets. After 2-3 weeks - maintenance therapy: 1 tablet 1 time per day. The course of treatment is 6-8 weeks.

Side effects: in the first days of treatment: nausea, vomiting, dizziness, rarely - hypotensive effect.

Contraindications: hypotension, gastrointestinal diseases, oral contraceptives, monoamine oxidase inhibitors.

Product form: tablets 0,0025 No. 30 and 100.

Dopaminolitics.

Antipsychotic drugs blocking postsynaptic dopamine receptors with simultaneous blocking of presynaptic dopamine receptors. It is believed that the suppression of dopaminergic transmission of nerve impulses in different areas of the CNS causes differences in the spectrum of psychotropic activity and the nature of the side effects of drugs in this group. According to the action of antipsychotics through presynaptic dopamine receptors, it is possible to select such drugs from this group that have antipsychotic activity, but are devoid of side extrapyramidal effects. Selective D2 receptor antagonists are drugs sulpiride (Sulpirid), metoclopramide (Metoclopramidum).

LECTURE No. 14. Histamine and antihistamines

1. Histamine. Histaminomimetics

Histamine is one of the mediators involved in the regulation of vital functions of the body and plays an important role in the pathogenesis of a number of painful conditions. Usually histamine is in the body in a bound, inactive state. The amount of histamine increases in various pathological conditions of the body: injuries, stress, allergic reactions. Then, along with histamine, other biologically active substances are released: serotonin, bradykinin, acetylcholine, substance of anaphylaxis, prostaglandins, etc. The amount of histamine also increases when various poisons (plant, animal, bacterial), food products (strawberries, egg whites, etc.), as well as some medicinal substances - anticholinergics, novocaine, antibiotics, etc. In the body there are specific receptors called histamine, or H-receptors, the mediator of which is histamine. Histamine receptors (H1 and H2) have different localizations in the body. When H1 receptors are stimulated, the tone of the smooth muscles of the intestines, bronchi, and bladder increases; stimulation of H2 receptors increases the secretion of the gastric glands, regulates the functioning of the salivary glands, and relaxes the smooth muscles of the uterus. Through H1 and H2 receptors, the level of blood pressure, capillary permeability, and coronary vessels are regulated. All histaminergic drugs are divided into two main groups:

1) H1- and H2-receptor stimulants - histaminomimetics;

2) H1- and H2-receptor blockers - antihistamines.

Histaminomimetics.

These substances excite H1- and H2-histamine receptors and cause the effects characteristic of histamine. As a drug, histamine has limited use. It is obtained from histidine by bacterial cleavage or synthetically.

Histamine (Histaminum).

In medical practice, histamine dihydrochloride is used. It causes spasm of smooth muscles, dilation of capillaries and a decrease in blood pressure, increased heart rate, increased secretion of gastric juice.

Application: polyarthritis, rheumatism, pain caused by damage to peripheral nerves, allergic diseases, for diagnostics and instrumental studies.

Mode of application: 0,2-0,5 ml of 0,1% solution is administered intravenously, subcutaneously and intramuscularly; for electrophoresis - 0,1% solution.

Side effects: in case of overdose - collapse, shock.

Product form: ampoules of 1 ml of 0,1% solution No. 10. As diagnostic tools for determining the secretory function of the stomach, a histalog (Gystalog), betazol (Betazol), tidazine (Tytazin), which exhibit high selective activity against H2 receptors, are used.

Antihistamines.

They are divided into two groups:

1) substances of direct action;

2) substances of indirect action, the effect of which is realized through a mediator, the synthesis or release of which changes with the introduction of these substances.

Direct acting antihistamines.

Among this group of drugs, substances that block H1 receptors (H1 blockers) and H2 receptors (H2 blockers) can be distinguished.

2. Antihistamines

Dimedrol (Dimedrolum).

It has antihistamine, anticholinergic and sedative effects.

Application: allergic diseases (urticaria, hay fever, allergic conjunctivitis, angioedema, etc.), parkinsonism, chorea, Meniere's disease, as a sedative and hypnotic.

Mode of application: administered orally, intramuscularly, intravenously, topically (cutaneously, in the form of eye drops, on the nasal mucosa), rectally.

Do not inject under the skin due to irritation. Prescribed orally 0,025-0,05 g 1-3 times a day, intramuscularly and intravenously - 1-5 ml of 1% solution, in the form of eye drops (0,2-0,5% solution). V.R.D. - 0,1 g, V.S.D. - 0,25 g, IM - 0,05 and 0,15 g, respectively.

Side effects: dizziness, headache, dry mouth, nausea, drowsiness, general weakness.

Contraindications: persons whose profession requires a quick response.

Product form: powder, tablets of 0,05 g No. 10, of 0,02 No. 6 for children, ampoules of 1 ml of 1% solution No. 10, rectal suppositories of 0,01 g No. 10 for children, sticks of 0,05 g No. 10.

Diprazine (Diprazinum).

Synonym: Pipolphen. It has a strong antihistamine activity, more active than diphenhydramine. Has a sedative effect.

Application: allergic diseases, rheumatism with a pronounced allergic component, allergic complications caused by drugs, itchy dermatosis, Meniere's disease, etc.

Mode of application: prescribed orally 0,025 g 2-3 times a day, intramuscularly - 1-2 ml of a 2,5% solution; IV (as part of lytic mixtures) - up to 2 ml of a 2,5% solution. For children - according to age. V.R.D. - 0,075 g, V.S.D. - 0,5 g; IM single - 0,05 g, daily - 0,25 g.

Side effects: dry mouth, nausea. With intramuscular injection - painful infiltrates, with intravenous administration - a sharp decrease in blood pressure.

Contraindications: alcohol intoxication, to persons whose work requires a quick response.

Product form: coated tablets, 0,025 and 0,005 No. 10, 2 ml ampoules of 2,5% solution No. 10.

Tavegil (Tavegil).

Synonym: Clemastinum. Antihistamine of prolonged action with a moderate sedative effect, enhances the effect of sleeping pills and alcohol.

Application: the same as diprazine.

Mode of application: prescribed orally at 0,001 g 2 times a day, if necessary - up to 0,004 g. Children from 6 to 12 years old - 0,0005-0,001 g 2 times a day.

Side effects: headache, constipation, dry mouth.

Contraindications: persons whose work requires intense physical and mental activity.

Product form: tablets of 0,001 g No. 20, 2,5 mg No. 20, ampoules of 2 ml of a 0,1% solution (2 mg) No. 5.

Suprastin (Suprastin).

Application, side effects and contraindications: like diphenhydramine.

Product form: tablets of 0,025 No. 20, ampoules of 1 ml of a 2% solution No. 5.

Fenkarol (Phencarolum).

Unlike diphenhydramine and diprazine, it does not have a sedative and hypnotic effect.

Application: as with other drugs in this group, it can be prescribed to persons whose work requires a quick response.

Mode of application: appoint orally 0,025-0,05 g 3-4 times a day, but with caution in patients with severe diseases of the cardiovascular system, liver and peptic ulcer, i-th trimester of pregnancy.

Product form: tablets of 0,025 and 0,01 g No. 20. List B.

This group also includes Diazolin (Diazolinum), which does not have a sedative and hypnotic effect, but due to irritation of the gastric mucosa, it is better to use it after eating in a dragee.

Product form: tablets and dragees 0,05 and 0,1 No. 20. List B.

3. Other drugs of the antihistamine group

H2 blockers selectively block H2 receptors, exerting an inhibitory effect on histamine-induced gastric secretion and partially eliminating histamine hypotension. They find use in the treatment of stomach ulcers.

Histodil (Histodil).

Synonym: Cimetidine. H2 receptor blocker. Antihistamine, reduces the secretion of hydrochloric acid in the stomach.

Application: for the treatment of benign tumors of the stomach and duodenum, reflux esophagitis, Zollinger-Ellison syndrome, inactive phase of erosive gastric hemorrhages.

Mode of application: administered orally 200 mg 3 times a day with meals and 400 mg at bedtime (1 g per day). It can also be administered intramuscularly or intravenously slowly at a dose of 200 mg, if necessary, repeat after 4-6 hours.

Side effects: dizziness, fatigue, rash, rarely nephritis or acute pancreatitis, which disappears when the drug is discontinued.

Contraindications: with caution during pregnancy, lactation, diseases of the liver, kidneys, circulatory systems.

Product form: tablets of 200 mg No. 50, ampoules of 2 ml of 10% solution No. 10.

Ranitidine (Ranitidinum).

Synonym: ranisan. A powerful blocker of H2-histamine receptors.

Indications for use, side effects, contraindications: like cimetidine.

Mode of application: take 1 tablet 2 times a day (morning and evening) regardless of meals. The course of treatment is 4-6 weeks.

For prevention - 1 tablet in the evening before bedtime for 12 months, every 4 months - endoscopy. With Zollinger-Ellison syndrome - 1 tablet 3 times a day, if necessary - up to 4-6 tablets a day. Patients with limited renal function (serum creatine level exceeds 3,3 mg (100 ml)) - daily 1/2 tablet 2 times a day.

Product form: tablets 150 mg No. 20, 50.

Antihistamines of indirect action.

These drugs act indirectly by disrupting the synthesis of histamine and reducing the amount of free histamine.

Ketotifen (Ketotifenum).

Synonym: Zaditen. An antiallergic agent that inhibits the release of histamine in the body, thereby preventing the occurrence of anaphylaxis, swelling of the mucous membranes, bronchospasm and other manifestations of an allergic reaction.

Application: prevention and treatment of bronchial asthma of allergic origin. allergic rhinitis.

Mode of application: Take 1 tablet in the morning and evening with meals. Patients sensitive to the sedative effect of the drug are initially prescribed 1/2 tablet per day, gradually increasing the dose to 2 mg per day. If necessary, the daily dose can be increased to 4 mg (2 tablets 2 times a day). Children over 3 years old - 0,025 mg/kg body weight 2 times a day.

Side effects: at the beginning of treatment - sedation, sometimes dry mouth, slight dizziness. These phenomena disappear without stopping treatment.

Contraindications: pregnancy, oral antidiabetic and other drugs that cause thrombocytopenia.

Product form: capsules and tablets of 0,001 each, syrup containing 1 mg of the drug in 0,2 ml. List B.

Cromolyn sodium (Cromolyn Sodium).

Synonym: Intal. Prevents the release of histamine from mast cells, prevents bronchospasm.

Application: bronchial asthma.

Mode of application: for inhalation (1 capsule 3-4 times a day) using a turbohaler. Can be used in combination with bronchodilators and corticosteroids. Inhalations are carried out daily. Start with 4 capsules per day (at intervals of 6 hours). In severe cases - up to 8 capsules per day (every 3 hours, 1 capsule). After the condition improves, the number of inhalations is gradually reduced, selecting an effective maintenance dose.

Side effects: in some cases, irritation of the larynx and throat, especially during respiratory diseases, sometimes cough and short-term bronchospasm. Cough is soothed by taking a glass of water immediately after inhalation, and in case of repeated bronchospasm, a preliminary inhalation of a bronchodilator is done.

Contraindications: pregnancy, age up to 5 years, with caution in patients with liver and kidney damage.

Product form: capsules of 0,02 g No. 30 and turbohaler.

Serotonin and serotonin and antiserotonin drugs.

Serotonin, or 5-hydroxytryptamine, is a biogenic amine formed in the body as a result of the transformation of the amino acid l-tryptophan. It accumulates in synaptic vesicles and is released under the influence of nerve impulses, interacting with specific receptors, referred to as serotonin (serotonergic). There are 5-HT1 (or S1-) - receptors, 5-HT2 (or S2-) - receptors, 5-HT3 (or S3-) - receptors. 5-HT2 receptors are found in the smooth muscles of the walls of blood vessels, bronchi and platelets. 5HT1 and 5HT3 receptors are found in the smooth muscles and mucosa of the gastrointestinal tract. 5HT3 receptors are found in peripheral tissues and in the central nervous system. Serotonin plays the role of a mediator in the CNS. Serotonin plays an important role in the pathogenesis of depression and the mechanism of action of antidepressants. It is assumed that the development of nausea and vomiting may be due to stimulation of serotonin 5HT3 receptors localized in the region of the vomiting center. The peripheral action of serotonin is characterized by contraction of the smooth muscles of the uterus, intestines, bronchi and other smooth muscle organs, constriction of blood vessels. Serotonin is one of the mediators of inflammation. When applied topically, it has a pronounced edematous effect, has the ability to shorten bleeding time, increase platelet aggregation, which releases serotonin. In medical practice, serotonin and its derivatives, as well as some of its antagonists, are used.

4. Serotonin and serotonergic and antiserotonin drugs

Serotonin adipate (Serotonini adipinas).

hemostatic agent.

Application: pathological conditions accompanied by hemorrhagic syndrome (Verlhof's disease, thrombasthenia, etc.).

Mode of application: administered intravenously (in 100-150 ml of 0,9% sodium chloride solution) or intramuscularly (in 5 ml of 0,5% novocaine solution) starting from 0,005 and up to 0,01 g in the absence of side effects phenomena, administered intramuscularly 2 times a day with an interval of at least 4 hours. The daily dose for adults is 0,015-0,02 g. The course of treatment is up to 10 days.

Side effects: with rapid injection into a vein, pain occurs along the vein and in the abdomen, discomfort in the heart area, increased blood pressure, heaviness in the head, difficulty breathing, nausea, vomiting, decreased diuresis, pain at the injection site when injected intramuscularly.

Contraindications: glomerulonephritis, kidney diseases accompanied by anuria, stage II-III hypertension, acute thrombosis, Quincke's edema, bronchial asthma, increased blood clotting.

Product form: 1 ml ampoules of 1% solution No. 10. List B.

Mexamine (Mexaminum).

Close to serotonin. Causes contraction of smooth muscles, constriction of blood vessels, has a sedative effect, enhances the effect of hypnotics and analgesics. It has radioprotective activity.

Application: prevention of general radiation reaction during radiation therapy. Assign inside from 0,05 to 0,1 g 30-40 minutes before each session.

Side effects: mild nausea, pain in the epigastric region, rarely vomiting.

Contraindications: severe sclerosis of the vessels of the heart and brain, cardiovascular insufficiency, bronchial asthma, pregnancy, kidney disease with impaired function.

Product form: coated tablets, 0,05 g No. 50.

Imigran (Imigran).

The active substance is sumatriptan, a specific stimulator of 5HT1-serotonin receptors.

Application: for quick relief of migraine attacks.

Mode of application: only after the onset of a migraine attack, 50 mg, possibly up to 100 mg.

Side effects: dizziness, drowsiness, nausea and vomiting, arterial hypertension, bradycardia, allergic reactions.

Contraindications: organic diseases of the cardiovascular system, monoamine oxidase inhibitors, ergotamine and its derivatives.

Product form: tablets 50 and 100 mg No. 6.

Zofran (Zofran).

The active substance ondansetron, a selective serotonin 5HT3 receptor antagonist, prevents or eliminates nausea and vomiting caused by chemotherapy or radiation therapy, as well as after surgery.

Application: nausea and vomiting after surgery, chemotherapy or radiation therapy.

Mode of application: inside and parenterally 8 mg, possibly up to 32 mg.

Side effects: headache, constipation, chest pain, hypotension, bradycardia.

Product form: tablets of 4 and 8 mg No. 10, ampoules for injections of 2 and 4 ml (2 mg per 1 ml of the active substance).

Cyproheptane (Cyproheptanum).

Synonym: Peritol. It has antihistamine activity, but also a strong antiserotonin agent. It has anticholinergic and antiallergic activity, especially in itching dermatoses.

Application: allergic diseases, serum sickness, migraine. 4 mg 3-4 times a day, for children - depending on age. Daily doses for adults are not higher than 32 mg, for children 2-6 years old - 8 mg, 6-14 years old - 12 mg.

Side effects: dry mouth, ataxia, nausea, skin rash.

Contraindications: pregnancy, glaucoma, urinary retention, persons whose work requires a quick reaction, incompatible with alcohol.

Product form: 4 mg tablets No. 20, syrup for children, 100 ml each (in 1 ml 0,4 mg of the drug). List B.

LECTURE No. 15. Means acting in the field of sensitive nerve endings. Drugs that reduce the sensitivity of nerve endings

1. Local anesthetics

The drugs of this group selectively block the process of excitation transmission in the efferent nerves and their endings, causing a loss of pain sensitivity at the site of their injection.

There are different types of local anesthesia:

1) surface (terminal) anesthesia (application of anesthetics to the surface of the skin, mucous membranes of the eyes, nose, etc.);

2) conduction anesthesia (injection of an anesthetic into or near a nerve);

3) spinal anesthesia (anesthetic solution is injected directly into the spinal canal);

4) infiltration anesthesia (the tissues of any part of the body are impregnated with an anesthetic in layers).

Preparations.

Anestezin (Anaesthesinum).

Local anesthetic.

Application: appoint inside with pain in the stomach, hypersensitivity of the esophagus, 0,3 g 3-4 times a day; externally in the form of a 5-10% ointment and powders for urticaria and skin diseases accompanied by itching, for pain relief of ulcerative and wound surfaces; in suppositories of 0,05-0,1 g for diseases of the rectum (with a crack, itching, hemorrhoids); in the form of a 5-20% oily solution for anesthesia of the mucous membranes.

Contraindications: individual hypersensitivity.

Product form: powder, tablets of 0,3 g No. 10.

Novocaine (Novocaine).

Local anesthetic.

Application: all types of anesthesia, vagosympathetic and pararenal blockade to potentiate the action of basic narcotic drugs, in general anesthesia, to relieve pain in gastric and duodenal ulcers, with anal fissures, hemorrhoids, etc.

Mode of application: for infiltration anesthesia, the highest dose at the beginning of the operation is no more than 500 ml of a 0,25% solution or 150 ml of a 0,5% solution, then for every hour up to 1000 ml of a 0,25% solution or 400 ml 0,5, 1% solution every hour. For conduction anesthesia, 2-20% solutions are used, for epidural anesthesia - 25-2 ml of a 2% solution, for spinal anesthesia - 3-5 ml of a 50% solution, for perirenal block - 80-50 ml of a 30% solution, vagosympathetic blockade - 100-0,25 ml of 0,1% solution, as a local anesthetic and antispasmodic agent in suppositories - XNUMX g each.

Side effects: dizziness, weakness, hypotension, allergies.

Contraindications: individual intolerance.

Product form: powder; 2 ml ampoules of 0,5, 1- and 2% solution No. 10, 5 ml ampoules of 0,5- and 2% solution No. 10; 10 ml ampoules of 0,5, 1 and 2% solution No. 10, 1 ml ampoules of 2% solution No. 10, 400 ml of 0,25 and 0,5% solution, rectal suppositories containing 0,1 , 10 g of novocaine, No. XNUMX. List B.

2. Other local anesthetics

Lidocaine (Lidocinum).

Synonym: Xycain. Local anesthetic and antiarrhythmic agent.

Application: local anesthesia. Ventricular extrasystole and tachycardia, especially in the acute stage of myocardial infarction and due to intoxication with digitalis preparations.

Mode of application: appoint only in / m, the total dose is not more than 300 mg.

Contraindications: severe functional disorders of the liver.

Side effects: headache, dizziness, drowsiness.

Product form: 10% solution in 2 ml ampoules No. 10 and 2% solution in 2 and 10 ml ampoules.

Ultracaine (Ultracaine).

It has a fast and strong anesthetic effect, good general and local tolerance.

Application: local and infiltration anesthesia in surgical interventions, labor pain relief, treatment of pain syndromes, lumbar anesthesia, conduction anesthesia in dentistry.

Mode of application.

1. For local anesthesia, a 2% solution of ultracaine is used in an amount of 2-5 ml (for example, when removing atheroma) and up to 100 ml (for example, when removing a hernia). Local conduction anesthesia for blockade of peripheral nerve endings or nerve plexuses is performed using 15-30 ml, the effect lasts about 2-3 hours.

2. Ultracaine 2% A. Doses and method of use are the same as for ultracaine 2%. For paracervical blockade, 6-8 ml is mainly used, for epidural and epidural anesthesia - 15-20 ml.

3. Ultracain 5%. The full onset of analgesia with the lumbar injection of 1,5-2 ml of a hypertonic solution of ultracaine 5% in 2-10 minutes and usually lasts 2-3 hours.

4. Ultracain-DS. When removing teeth of the upper jaw without signs of inflammation, 2 ml is administered per tooth as a vestibular depot. If it is necessary to make an incision or suture the palate, use 0,1 ml for each suture.

Side effects: depends on the dose used. There may be fainting, collapse, respiratory disorders, nausea, vomiting, involuntary muscle movements, contractions and spasms caused by the action of adrenaline, which is contained in ultracaine.

Contraindications: paroxysmal tachycardia, atrial fibrillation and glaucoma. The preservative substance ultracaine (methyl ester of parahydroxybenzoic acid) has a hydroxyl group in its composition in the para position. Patients suffering from allergies to this group, the introduction of ultracaine is contraindicated.

Product form: in ampoules of ultracaine 2%, 10 ml No. 5, ultracaine 2% A - 10 ml No. 5, ultracaine 5% - 2 ml No. 5, ultracaine DS - 2 ml No. 50.

Other local anesthetics are also used in medical practice. In ophthalmology they use a 0,5% solution of dicaine (Dicainum), a 0,5% solution of pyromecainum (bumecaine - Bymecainum), in ophthalmology and otorhinology 0,5, 1 and 2% solutions. In addition, there are dosage forms containing local anesthetics: Anestezol suppositories, Pavetesin tablets, Olazol aerosol.

3. ​​Astringents

Astringents, when applied to mucous membranes, cause coagulation of proteins, the resulting film protects the mucous membrane from irritating factors, pain decreases and inflammation is weakened.

This effect is exerted by many substances of plant origin, as well as weak solutions of salts of certain metals.

Tannin (Ta ninum).

gallodubic acid. It has astringent and anti-inflammatory action.

Application: stomatitis, gingivitis, pharyngitis (1-2% solution for rinsing (3-5 times a day), externally for burns, ulcers, cracks, bedsores (3-10% solutions and ointments), poisoning with alkaloids, heavy salts metals (0,5% aqueous solution for gastric lavage).

Product form: powder.

Tansal (Tansal).

Composition: tanalbine - 0,3 g, phenyl salicylate - 0,3 g. Astringent and disinfectant.

Application: acute and subacute enteritis and colitis (1 tablet 3-4 times a day).

Product form: tablets number 6.

Hypericum grass (Herba Hyperici).

Contains tannins such as catechins, hyperoside, azulene, essential oil and other substances.

Application: as an astringent and antiseptic for colitis in the form of a decoction (10,0-200,0 g) 0,3 cups 3 times a day 30 minutes before meals, for rinsing the mouth in the form of a tincture (30-40 drops per glass of water) .

Product form: chopped grass 100,0 g each, briquettes 75 g each, tincture (Tinctura Hyperici) in 25 ml bottles.

Oak bark (Cortex Quecus).

Application: as an astringent in the form of an aqueous decoction (1:10) for rinsing with gingivitis, stomatitis and other inflammatory processes of the oral cavity, pharynx, larynx, externally for the treatment of burns (20% solution).

In medicinal practice, infusions and decoctions of such plants as: rhizome of serpentine (Rhizoma Bistortae), rhizome and root of burnet (Rhizoma cum radicibus Sanguisorbae), alder fruit (Fructus Alni), sage leaves (Folium Salviae), a preparation from it - salvin are also used. (Salvinum), chamomile flowers (Flores Chamomillae), chamomile preparation; Romasulan (Romasulon), blueberries (Baccae Murtilli), bird cherry fruits (Baccae Pruni racemosae), cinquefoil rhizome (Rhizoma Tormentillae), succession grass (Herba Bidentis).

Metal salts. Bismuth preparations.

Bismuth nitrate basic (Bismuthi subnitras).

Application: as an astringent, weak antiseptic, fixing agent for gastrointestinal diseases, it is prescribed orally at 0,25-1 g (for children, 0,1-0,5 g) per reception 4-6 times a day 15-30 minutes before meals.

Side effects: with prolonged use in high doses, methemoglobinemia is possible.

Product form: powder, which is part of the Vikair tablets, used for gastric and duodenal ulcers, and Neo-Anuzol suppositories, which are used for hemorrhoids.

Xeroform (Xeroformium).

Applied externally as an astringent, drying and antiseptic agent in powders, powders, ointments (3-10%). Included in the balsamic liniment (Vishnevsky ointment)

Dermatol (Dermatolum).

Synonym: Bismuthi subgallas. Applied as an astringent, antiseptic and drying agent externally for inflammatory diseases of the skin, mucous membranes in the form of powders, ointments, suppositories.

Product form: powder.

Lead preparations: lead acetate (Plumbi acetas) - lead lotion - 0,25% solution.

Aluminum preparations: Alum (Alumen). Used as an astringent and hemostatic agent (0,5-1% solution).

Alum burnt (Alumen ustum).

As an astringent and drying agent in the form of a powder included in the powder.

4. Coating agents and absorbent agents

Enveloping agents.

Enveloping agents form colloidal solutions in water - mucus that covers the mucous membranes and protects them from the action of irritating substances.

They are used to treat inflammatory diseases of the gastrointestinal tract, as well as to reduce the irritating effect of certain drugs. As enveloping agents, starch mucus, mucus from flax seed, some organic and inorganic substances capable of forming colloidal solutions are used.

Almagel (Almagel).

Combined preparation, 5 ml of which contains 4,75 gel of aluminum hydroxide, 0,1 g of magnesium oxide with the addition of D-sorbitol.

Application: peptic ulcer of the stomach and duodenum, hyperacid gastritis and other diseases of the stomach. Almagel A also includes 0,1 g of anesthesin, it is used in the presence of concomitant pain. Assign 1-2 tsp. 4 times a day 30 minutes before meals.

Flax seed (semen).

It is prescribed externally for poultices, internally as an enveloping and emollient in the form of mucus (Mucilago seminis Lini), which is prepared from 1 part whole flaxseed and 30 parts ex tempore hot water.

adsorbents.

They have the ability to protect mucous membranes from irritation, slow down the absorption of various substances from the gastrointestinal tract in case of poisoning. The most commonly used are activated carbon, white clay powder, smectite, etc.

Carbolene (Carbolenum).

Activated carbon (Tabulettae Carbonis activi) is able to adsorb gases, alkaloids, salts of heavy metals, toxins, etc.

Application: as an adsorbent for dyspepsia, flatulence, taken orally 1-3 tablets 2-4 times a day.

Product form: tablets of 0,25 g No. 10.

clay white (Bolus alba).

Application: as an enveloping and adsorbing agent, it is taken orally (10-100 g) for gastrointestinal diseases (colitis, enteritis), externally in the form of powders, ointments, pastes for skin diseases.

Product form: powder.

Smectite (Smecta).

Antidiarrheal agent. The suspension has significant sorption properties and enveloping ability, protecting the mucous membrane of the digestive tract from the negative effects of H ions, intestinal microorganisms, their toxins and other irritants, prevents water and electrolyte losses, increases the amount of mucus and improves its quality.

Application: acute and chronic diarrhea, especially in children, symptomatic pain associated with diseases of the esophagus, stomach, duodenum, is compatible with oral rehydrants (does not change physiological peristalsis).

Mode of application: To obtain a homogeneous suspension, pour the contents of the sachet into 0,5 cups of water and mix. For children, the powder can be dissolved in porridge, puree, compote, in a 50 ml baby bottle (at the rate of: up to one year - 1 sachet per day, from 1 to 2 years - 2 sachets per day, over 2 years - 2-3 sachet per day). Adults - 3 sachets per day.

Product form: powder for the preparation of a suspension of 3 g of active substance No. 30.

LECTURE No. 16. Means whose action is associated mainly with irritation of the nerve endings of the mucous membranes and skin

1. Preparations containing essential oils. Preparations containing menthol

These drugs excite receptors located in the skin and mucous membranes, the impulses from which enter the central nervous system. This causes a reaction on the part of organs that have conjugated innervation in the central nervous system with areas exposed to irritating substances, as a result of which the blood supply to the organ and its trophism improve, which favorably affects various inflammatory processes. The effect of irritants is also enhanced by the local reaction that they cause and which is associated with the release of biologically active substances.

They are divided into several groups: products containing essential oils; bitterness; products containing ammonia.

menthol (Mentholum).

Applied externally as an analgesic (distracting) agent, inside as a sedative (validol). Included in many combination drugs.

Application: inflammatory diseases of the upper respiratory tract in the form of nasal drops and inhalations.

For young children, the use of menthol-containing drugs is contraindicated.

Validol (Validolum).

A 25-30% solution of menthol in isovaleric acid methyl ester has a calming effect on the central nervous system. It is prescribed for mild forms of angina pectoris, neurosis (4-5 drops per piece of sugar or bread).

Product form: tablets number 6 and 10.

Oil menthol 1 or 2% (Oleum Mentholi), 10 ml vials.

Ointment boromenthol (Boromentholum).

With itching, neuralgia, rhinitis.

Tablets "Pectusin" (Tabuletta pectusinum).

Contain menthol - 0,004 g, eucalyptus oil 0,0005 g and other fillers.

Application: inflammatory diseases of the upper respiratory tract.

Menovazine (Menovasinum).

Contains menthol - 2,5 g, novocaine and anesthesin - 1 g each and 70% alcohol - up to 100 ml, used for neuralgia, myalgia and as an antipruritic agent.

Ointment "Gevkamen" (Unguentum Geucamenum).

Contains menthol - 18 g or mint oil - 22,5 g, eucalyptus oil and camphor - 10 g each, clove oil - 1 g, paraffin and petroleum jelly - up to 100 g.

Application: neuralgia, myalgia.

Aerosol "Camphomen" (Aerosolum "Camphomenum").

It is used mainly for the treatment of acute rhinitis and pharyngitis. Not recommended for children under 5 years of age.

Mixture for inhalation (Mixtio pro inhalationibus).

Contains menthol, eucalyptus tincture and glycerin.

Ingacamph (Inhacamf).

Pocket inhaler with camphor, menthol, methyl ester, salicylic acid and eucalyptus oil.

Ointment "Evcamon" (Unguentum "Efcamonum").

It consists of camphor, clove and mustard essential oils, eucalyptus, menthol, methyl salicylate, capsicum tincture, thymol and chloral hydrate, cinnamon alcohol, paraffin, petroleum jelly and spermaceti.

Application: arthritis, myositis, neuralgia.

Contraindications: damage to the skin.

Tooth dropscontaining menthol, thymol, phenyl salicylate, glycerin and alcohol.

2. Products containing essential oils. bitterness. Products containing ammonia

Products containing essential oils.

eucalyptus leaf (Folium Eucalypti).

Application: decoction and infusion of eucalyptus as an antiseptic for rinsing and inhalation in ENT diseases, as well as for the treatment of fresh and infected wounds, inflammatory diseases of the female genital organs.

Eucalyptus tincture (Tinctura Eucalypti).

Application: 15-30 drops per reception, for rinsing - 10-15 drops per glass of water.

Eucalyptus oil (Oleum Eucalypti).

Application: 15-20 drops per glass of water.

mustard seed (Semen Sinapis).

From its defatted seeds, essential mustard oil (Oleum Sinapis aethereum).

The mustard (Charta Sinapis).

When wetted with warm water, there is a strong smell of essential mustard oil. Used as an anti-inflammatory agent. When moistened, apply to the skin for 5-15 minutes until pronounced redness appears. Do not apply to broken skin.

Capsicum fruit (Fructus Capsici).

Contains capsaicin.

Preparations from it: capsicum tincture (Tinctura Capsici), pepper camphor liniment (Linimentum Capsici camphoratum), patch pepper (Emplastrum Capsici).

Application: as a distraction for neuralgia, myositis, etc. Before applying the patch, the skin is degreased with alcohol or cologne and wiped dry.

Purified turpentine oil (purified turpentine)

(Oleum Terebinthinae rectificatum).

Application: as a distraction for neuralgia, myositis, rheumatism.

Contraindications: damage to the liver and kidneys.

Turpentine ointment (Unguentum Terebinthinae).

Application: the same as that of terpine oil.

Formic alcohol (Spiritus Acid formici).

Application: externally for rubbing with myositis, neuralgia.

bitterness.

Bitterness (amara) - herbal preparations containing substances with a strong bitter taste. By irritating the taste buds of the mucous membranes of the oral cavity and tongue, they cause by reflex an increase in the secretion of gastric juice, an increase in appetite, and an improvement in digestion. It is prescribed for hypacid and chronic atrophic gastritis, with anorexia due to nervous diseases, after undergoing surgical interventions. Take 2-4 times a day 15-20 minutes before meals with a little water.

Contraindications: increased gastric secretion, peptic ulcer of the stomach and duodenum, reflux esophagitis. This group includes centaury grass (Herba Gentaurii), wormwood herb (Herba Absinti), water shamrock leaf (Folium menyanthidis), dandelion root (Radix Taraxaci), calamus rhizome (Rhizoma Calami).

Used in the form of infusions and decoctions.

Products containing ammonia.

Ammonia solution 10% (Solutio Ammonii caustici).

Application: as an emergency medicine to stimulate breathing and bring patients out of fainting, sometimes used internally as an emetic (5-10 drops per 100 ml of water). For insect bites - externally in the form of lotions.

Contraindications: dermatitis, eczema.

Product form: bottles of 40 ml and ampoules of 1 ml No. 10.

LECTURE No. 17. Expectorants

1. Means that stimulate expectoration

They cause increased secretion and thinning of bronchial mucus (sputum), which facilitates its separation when coughing. They are divided into two groups:

1) drugs that stimulate expectoration (secretory);

2) mucolytic agents (bronchosecretolytic).

Secretomotor drugs enhance the physiological activity of the ciliated epithelium and the peristaltic movements of the bronchioles, promoting the promotion of sputum from the lower sections to the upper sections of the respiratory tract and its removal. The effect is usually combined with an increase in the secretion of the bronchial glands and a slight decrease in the viscosity of sputum. Conventionally, the drugs of this group are divided into two subgroups: reflex and resorptive action.

Reflex action drugs (preparations of thermopsis, istoda, marshmallow and other medicinal plants, sodium benzoate, terpinhydrate, etc.). When taken orally, they have a moderate irritating effect on the receptors of the gastric mucosa and reflexively affect the bronchi and bronchial glands. The effect of some drugs (thermopsis, etc.) is also associated with a stimulating effect on the vomiting and respiratory centers.

The means of reflex action also include drugs with predominant emetic activity (apomorphine, lycorine), which have an expectorant effect in small doses. A number of preparations of reflex action partially have a resorptive effect: the essential oils and other substances contained in them are excreted through the respiratory tract and cause increased secretion and liquefaction of sputum.

Resorptive drugs (sodium and potassium iodide, ammonium chloride, partially sodium bicarbonate, etc.) have an effect mainly when they are secreted (after ingestion) by the mucous membrane of the respiratory tract, stimulate the bronchial glands and cause direct dilution of sputum; to a certain extent, they also stimulate the motor function of the ciliated epithelium and bronchioles. Iodine preparations have a particularly active effect on the viscosity of sputum. Mucolytic (both enzymatic and synthetic) increase the volume of sputum, thin the mucus and enhance the drainage function of the bronchi, and as a result - a pronounced anti-inflammatory effect.

Thermopsis herb, mouse herb (Herba Thermopsidis).

Contains alkaloids (the main of which is thermopsin), saponins, essential oil, tannins, ascorbic acid. The action of all these substances on the body is complex, but generally expectorant, in large doses - emetic.

Application: Chronical bronchitis. The infusion is prepared at the rate of 0,6-1,0 g per 180-200 ml of water.

1 tbsp. l. take 2-4 times a day; dry extract 0,01-0,05 g, cough tablets - 1 tablet per dose. For children - according to age.

Product form: dry thermopsis extract (Extractum Thermopsidis siccum) in jars; cough tablets (Tabulettae contra tussim) containing 0,01 g of thermopsis grass in fine powder, sodium bicarbonate 0,25 No. 10, dry cough mixture for adults. List B.

Althea root (Radix Althae).

Contains up to 35% plant mucus.

Apply in the form of powder, infusion, syrup as an expectorant and anti-inflammatory agent for respiratory diseases.

Included in the chest collection No. 1, 3. 1 tbsp. l. collection is poured with a glass of boiling water, insisted for 20 minutes, filtered and taken 0,5 cups 2-3 times a day.

Product form: marshmallow root extract dry in a jar; alteyny syrup, 100,0 ml; dry cough syrup for children (Mixtura sicca contra tussim pro infatibus), which also includes sodium benzoate and sodium bicarbonate, ammonium chloride, anise oil; breast fees No. 1 (marshmallow root, coltsfoot leaves, oregano herb) and No. 3 (marshmallow root, licorice root, sage leaves, anise fruits and pine buds).

Mukulin (Mucaltinum).

A preparation containing a mixture of polysaccharides and marshmallow herbs. Assign 1-2 tablets per dose before meals for acute and chronic respiratory diseases.

Liquorice root (Radix Glycyrrhizae).

Contains glycyrrhizic acid, flavonoids and other active substances. It has anti-inflammatory properties, antispasmodic effect, accelerates the healing of stomach ulcers.

Preparations: chopped licorice root - 100 g; chest elixir (Elixir pectoralis) - 25 ml. Ingredients: thick licorice root extract, anise oil, aqueous ammonia, ethyl alcohol. Take as an expectorant, 20-40 drops 3-4 times a day, for children - 1 drop per year of life.

Liquiriton (Liquiritonum).

Contains a sum of flavonoids from licorice roots and rhizomes.

Application: as an anti-inflammatory, antispasmodic and antisecretory agent. Take 0,1-0,2 g orally 3-4 times a day, the course of treatment is 20-30 days.

Product form: tablets 0,1 No. 25.

Breast Collection #2 (Species pectorals).

Ingredients: crushed licorice root and plantain leaves, crushed coltsfoot leaves.

Application: 1 st. l. collection on a glass of boiling water insist 20 minutes, filter; 0,5 cups of infusion at the reception, after eating.

Glycyram (Glycyrramum).

Monosubstituted ammonium salt of glycyrrhizic acid, isolated from licorice roots, has an anti-inflammatory effect associated with a moderately stimulating effect on the adrenal cortex.

Application: bronchial asthma, allergic dermatitis, eczema. Can be used to reduce the dosage of glucocorticoids. Prescribed orally 0,05-0,1 g 2-4 times a day (up to 3-6 times), 30 minutes before meals. The course of treatment is from 2 to 6 weeks. Do not take if you have organic heart disease or impaired liver or kidney function.

Product form: tablets 0,05 No. 50. List B.

This group also includes a rhizome with roots of cyanosis (Rhizoma cum radicibus Polemonii), a rhizome and roots of elecampane (Rhizoma cum radicibus Inulae helenii), large plantain leaves (Folium Plantaginis majoris) and a preparation from it plantaglucid (Plantaglucidum), which is taken at 0,5, 1,0-2 g 3-1 times a day; coltsfoot leaves (Folium Farfarae), thyme herb (Herba Serpulli) and Pertusin preparation, which is taken from 2-1 tsp. up to XNUMX dec. l. (Pertussinum), anise fruit (Fructus Anisi vulgaris), wild rosemary herb (Herba Ledi Palustris), oregano herb (Herba Origani vulgaris), pine buds (Turiones Pini), tricolor violet herb (Herba Violae tricolori).

2. Mucolytic drugs

Acetylcysteine (Acetylcestein).

One of the most active mucolytic drugs.

Application: respiratory tract diseases.

Mode of application: inhalations of 2-5 ml of a 20% solution 3-4 times a day for 15-20 minutes.

Side effects: possible nausea.

Contraindications: bronchial asthma. Mixing solutions of acetylcysteine ​​with solutions of antibiotics and proteolytic enzymes is undesirable in order to avoid drug inactivation. If necessary, you can add bronchodilators. It is possible to use a solution from opened ampoules for inhalation for no more than 48 hours.

Product form: 20% solution of 5 ml, 5% solution of 10 ml No. 10. List B.

Bromhexine (Bromhexin).

The drug has a mucolytic, expectorant effect and a weak antitussive.

Application: acute and chronic bronchitis, pneumonia, sanitation of the bronchial tree in the preoperative period, to prevent the accumulation of thick viscous sputum in the bronchus after surgery, to accelerate the release of a contrast agent after bronchography.

Mode of application: taken orally 0,004-0,008 g 2-3 times a day. For children - depending on age.

Product form: dragee 0,004 g No. 50, 0,008 g No. 20. List B.

Trypsin (Trypsin).

Proteolytic enzyme, facilitates the removal of viscous secrets, exudates. Assign for diseases of the respiratory tract inhalation or intramuscularly. It has an anti-inflammatory effect.

Contraindicated with pulmonary tuberculosis, emphysema, diseases of the liver, kidneys, pancreas. Do not administer intravenously! Produced in ampoules containing 0,01 and 0,005 g of crystalline trypsin. Used for inhalation.

Potassium iodide (Kalii iodidum).

Application: respiratory and thyroid diseases. As a mucolytic agent, it is used in the form of a 1-3% solution, 1 tbsp. l. 3-5 times a day.

sodium benzoate (Natri benzoas).

Application: as an expectorant for diseases of the respiratory tract in powders, solutions and mixtures of 0,2-0,5 g 3-4 times a day.

Product form: powder.

LECTURE No. 18. Laxatives

1. General characteristics of laxatives

There are several classifications of laxatives. The general classification includes two groups:

1) inorganic substances - saline laxatives, magnesium and sodium sulfate, Karlovy Vary salt;

2) organic substances consist of three subgroups, such as:

a) vegetable oils - castor and almond;

b) preparations containing anthraglycosides (buckthorn extract, rhubarb tablets), senna preparations (senna leaves, cofiol, regulax cubes, senade, glaxena);

c) preparations containing synthetic agents (bisacodyl, guttalax, forlax, fortans), synthetic disaccharides (lactulose), vaseline oil.

The modern classification of laxatives according to the mechanism of action includes 4 groups of drugs.

First group. Chemical agents that cause a laxative effect by chemical irritation of the receptor apparatus of the colon and thus stimulate its peristalsis. These drugs act at the level of the colon, usually causing a single bowel movement 6-10 hours after ingestion. These include anthraquine derivatives (drugs of rhubarb root, buckthorn bark, joster fruits, hay leaves), diphenylmethane (phenolphthalein, bisacodyl, guttalax, dulcolax), castor oil.

Second group. Osmotic agents that have the ability to retain water in the intestinal lumen, which leads to an increase in volume and softening of stool. These are sodium and magnesium sulfate, citrate, magnesium hydroxide, Carlsbad salt, non-adsorbable polysaccharide lactulose (Duphalac), acting at the level of the colon. The onset of the laxative effect is 8-12 hours. Lactulose is not broken down in the small intestine and enters the large intestine unchanged. In the colon it is broken down by the intestinal flora. The breakdown products of lactulose have a stimulating effect on colon peristalsis, stool softens, and in addition, its volume increases.

Third group. Bulk laxatives, or bulking agents, such as bran, agar, methylcellulose, seaweed.

Fourth group. Laxative oils (detergents) that help soften hard stool and make it easier to slide - petroleum jelly, almond, fennel oil, liquid paraffin. Classification by localization of action. Medicines that primarily act in the small intestine (vegetable oils, petroleum jelly, saline laxatives). Medicines that act primarily in the colon (synthetic drugs, bisacodyl, guttalax. Medicines that act throughout the intestine (salt laxatives, castor oil and hydrophilic colloids).

2. Laxatives

Chemical laxatives.

senna leaves (Folium Sennae).

Application:: in the form of an infusion of 1 tbsp. l. or 1 tsp. 1-3 times a day.

Product form: whole and cut leaves 50 g each, dry extract in tablets 0,03 No. 25 each, briquettes 75 g each. Finished preparations: senade No. 10 in tablets, glaxena No. 10 in tablets.

Ramnil (Rhamnilum).

Dry standardized preparation of buckthorn bark.

Application: taken as a laxative at 0,2 g per night.

Product form: tablets 0,05 No. 30.

Bisacodyl (Bisacodyl).

Synonym: Dutcolach. Mechanism of action: irritates intestinal receptors, and also enhances mucus secretion and liquefaction of intestinal contents.

Application: chronic constipation of various etiologies.

Mode of application: prescribed per os and per rectum. Adults: 1-3 tablets at night or 1-2 suppositories rectally. For children - depending on age.

Side effects: spasms of the gastrointestinal tract are possible.

Contraindications: acute inflammatory diseases and varicose veins of the rectum.

Product form: dragee 0,005 No. 30, candles 0,01 No. 12.

Guttalax (Guttalax).

It has a fast and strong laxative effect by direct stimulation of the colon. The stomach passes without changes, it is excreted with a stool, it is not addictive.

Application: all kinds of constipation, hemorrhoids, anal fissures, in the postoperative period.

Mode of application: adults: 5 to 10 drops, up to 15 drops possible. Children from 2 to 12 years old - from 2 to 5 drops. Take either in the morning or before bed. The effect occurs after 6-10 hours.

Contraindications: acute abdomen, pregnancy.

Product form: vials of 10 ml of the drug.

Castor oil (Oleum Ricini).

Application: take as a laxative - 15-30 g each, children - 5-10 g each.

Contraindications: poisoning with male fern extract and fat-soluble substances (phosphorus, benzene), externally used to treat burns, ulcers.

Product form: bottles of 25 g. Capsules of 1,0 No. 15.

Osmotic laxatives.

Carlsbad salt artificial (Sal carolinum fastitium).

Application: As a laxative, take 1 tbsp in the morning on an empty stomach. l. (children 2-6 years old - 1 tsp) per 0,5 cup of water; as a choleretic 1 tsp. in a glass of warm water 30-45 minutes before meals 2-3 times a day.

Product form: in a package of 125 g. Carlsbad geyser natural salt is also on sale, 100 g in a package.

Dufalac (Dufalac).

Synonym: Lactyloza.

Product form: powder for oral administration in sachets of 10 g No. 10, syrup of 200, 500 and 1000 ml (100 ml - 67 g of lactulose). Adults for the treatment of constipation - 10-30 g per day in the first 2 days; maintenance dose - 10-20 g per day. For children 7-14 years old, the initial dose is 10 g per day, maintenance dose is 7-10 g per day; from 1 g to 6 years, the initial and maintenance doses are the same - 3-7 g per day; children under 1 year - 3 g per day. This drug is contraindicated in case of intestinal obstruction. With caution - for patients with diabetes mellitus. The drug may interfere with the release of the active substance from enteric drugs.

LECTURE No. 19. Means acting on the cardiovascular system

1. Classification of funds acting on the cardiovascular system

Means acting on the cardiovascular system can be divided into several groups:

1) cardiotonic means;

2) antiarrhythmic drugs;

3) means that improve the blood supply to organs and tissues, cerebral circulation;

4) antihypertensive and hypertensive drugs;

5) angioprotectors and hypolipodemic agents;

6) agents that inhibit and stimulate blood coagulation.

Cardiotonic means widely used to treat heart failure. Along with drugs that stimulate the contractile activity of the myocardium (cardiac glycosides), agents are used that reduce the load on the myocardium and facilitate the work of the heart, reduce the energy costs of the heart muscle and improve its function with more economical activity. Such means of complex therapy are primarily peripheral vasodilators that reduce pre- and afterload on the myocardium by reducing peripheral vascular resistance and expanding the peripheral vascular bed, as well as diuretics that reduce the load on the myocardium, providing a hypovolemic effect, i.e., reducing the volume of circulating plasma blood. To a certain extent, cardiotonic properties are possessed by agents that have a general positive effect on the metabolic processes of the body, including myocardial metabolism (anabolic hormones, riboxin, etc.). In the treatment of acute heart failure, in addition to pressor amines, modern adrenomimetic drugs (dopamine, dobutrex) and cardiotonic corotrotrop (malrinone) are used.

cardiac glycosides.

This group includes drugs that increase myocardial contractility. Plants containing cardiac glycosides include different types of foxglove (Digitalis purpurea L.) Adonis (Adonis vernalis L.), lily of the valley (Convallaria majalis L.), different types of jaundice (Erysimum canescens Roth.), strophanthus (Strophanthus gratus, Strophanthus Kombe ), oleander (Nerium oleander), hellebore (Helleborus purpurascens W. et K.), etc. The mechanism of action of cardiac glycosides is associated with the activity of the enzyme adenosine triphosphatase, which ensures the transport of potassium, sodium, and calcium ions. They normalize the energy and electrolyte metabolism disturbed in the heart muscle, promote the absorption of creatine phosphate, the use of ATP by the heart, and increase the glycogen content in the heart muscle. The therapeutic effect of cardiac glycosides is expressed in the following changes in the work of the heart:

1) the strength of heart contractions increases, the systole becomes more energetic and short in time, the stroke volume of blood increases;

2) diastole becomes longer. More blood enters the chambers of the heart, the heartbeat slows down;

3) the slowdown in the conduction of impulses is manifested in relation to the atrioventricular node and bundle. Diuresis increases under the influence of cardiac glycosides. Symptoms of poisoning with cardiac glycosides: bradycardia, and increased excitability of the heart contributes to the appearance of tachycardia, extrasystoles. In violation of atrioventricular conduction, ventricular flutter, cardiac arrest may occur.

2. Long acting glycosides

Cardiac glycosides are divided into three groups.

1. Long acting glycosides, with the introduction of which the maximum effect when taken orally develops after 8-12 hours and lasts up to 10 days or more. With intravenous administration, the effect occurs after 30-90 minutes, the maximum effect is manifested after 4-8 hours. This group includes digitalis purpurea glycosides (digitoxin, etc.), which have a pronounced cumulation.

2. Intermediate-acting glycosides, when administered, the maximum effect appears after 5-6 hours and lasts for 2-3 days. When administered intravenously, the effect occurs after 15-30 minutes, the maximum effect occurs after 2-3 hours. This group includes glycosides of foxglove woolly (digoxin, celagid, etc.), which have moderate accumulation. This property is possessed by glycosides of foxglove and adonis.

3. Fast and short acting glycosides - emergency medications. Administered only intravenously, the effect occurs within 7-10 minutes. The maximum effect appears after 1-1,5 hours and lasts up to 12-24 hours. This group includes glycosides of strophanthus and lily of the valley, which have practically no cumulative properties. Treatment with cardiac glycosides begins with large doses prescribed for 3-6 days (saturation phase), until a clear therapeutic effect is obtained - reduction of congestion, elimination of edema, shortness of breath, improvement of general condition. Then the dose is reduced and maintenance doses are prescribed (maintenance phase), providing effective and safe therapy, taking into account the individual characteristics of the patient. In case of overdose of cardiac glycosides, potassium preparations are prescribed - panangin, asparkam.

long acting glycosides.

Digitoxin (Digitoxin).

Glycoside obtained from various types of foxglove (Digitalis purpurea L., Digitalis Lanata Ehrh., etc.). It has a strong cardiotonic effect, increases the force of contraction of the heart muscle, reduces the heart rate, has pronounced cumulative properties, is rapidly absorbed from the gastrointestinal tract.

Application: chronic heart failure with circulatory disorders stage II and III.

Mode of application: appoint inside 0,1 mg and per pectum 0,15 mg 1-2 times a day. V. R. D. - 0,5 mg, V. S. D. - 1 mg.

Side effects and contraindications: the same as for other digitalis preparations.

Product form: tablets 0,0001 g No. 10, rectal suppositories 0,00015 g No. 10.

Cordigite (Cordigitum).

Extract from dried leaves of digitalis purpurea containing a complex of glycosides.

Used for heart failure, 0,4-0,8 mg 2-4 times a day.

Side effects: with an overdose of bradycardia - nausea, extrasystole.

Contraindications: acute endocarditis, apply carefully with fresh myocardial infarction, rhythm disturbances.

Product form: tablets of 0,8 mg No. 10, suppositories of 0,0012 No. 10.

3. Intermediate-acting glycosides

Lantoside (Lantosidum).

Novogalenic drug obtained from the leaves of woolly foxglove (Digitalis lanata). It is similar to alcoholic solutions of the digitalis glycoside complex, but is absorbed faster and has a lower cumulative property.

Application: chronic failure stage I-III, accompanied by tachycardia, tachyarrhythmia and atrial fibrillation.

Mode of application: prescribed orally 15-20 drops 2-3 times a day, for dyspeptic symptoms - microenemas, 20-30 drops, in 20 ml of 0,9% sodium chloride solution. V.R.D. inside - 25 drops, V.S.D. - 75 drops.

Product form: in dropper bottles of 15 ml.

Celanide (Celalidum).

Synonym: isolanide. A glycoside obtained from the leaves of woolly foxglove (Digitalis lanata Eheh.). It acts on the heart like other digitalis glycosides, gives a quick effect and cumulates little.

Application: acute and chronic circulatory failure, tachyarrhythmic form of atrial fibrillation, paroxysmal tachycardia.

Mode of application: take orally 1 tablet (0,25 mg) 2-3 times a day; in / in 1-2 ml of a 0,02% solution 1-2 times a day.

Side effects and contraindications: the same as for other digitalis glycosides.

Product form: tablets of 0,25 mg No. 30, ampoules of 1 ml of a 0,02% solution No. 10, vials of 10 ml of a 0,05% solution.

Digoxin (Digoxinum).

Cardiac glycoside contained in the leaves of woolly foxglove.

Application, contraindications: the same as the rest of the drugs in this group.

Side effects: nausea, vomiting, loss of appetite, tachycardia, bigeminia.

Product form: tablets of 0,00025-0,0001 No. 50, ampoules of 1 ml of 0,025% solution No. 10. List B.

Meproscillarin (Meproscillarin).

Cardiac glycoside from squill. Increases the strength and speed of heart contractions, slightly slows down the heart rate (HR), AV conduction, causes an indirect vasodilating effect in chronic heart failure, reduces venous pressure, increases diuresis, reduces shortness of breath, and edema.

Application: chronic heart failure, including in the presence of normo- or bradysystolic atrial fibrillation.

Mode of application: the average single dose is 250 mcg 2-3 times a day, if necessary - up to 1 mg per day.

Side effects: bradycardia, av-blockade, cardiac arrhythmia, anorexia, nausea, vomiting, diarrhea, headache, fatigue, dizziness. Less common are xanthopsia, decreased visual acuity, scotomas, macro- and micropsia.

Contraindications: absolute with hypersensitivity to the drug, relative with severe bradycardia, isolated mitral stenosis, acute myocardial infarction, unstable tachycardia, extrasystole, severe liver dysfunction, pregnancy, lactation.

Product form: tablets 250 mcg No. 30.

4. Glycosides of short and fast action. Non-steroidal and synthetic cardiotonic drugs

Glycosides of short and fast action.

Strofantin K (Strophantinum K).

A mixture of cardiac glycosides isolated from the seeds of Kombe strophanthus, containing mainly strophanthin K and strophanthoside K. It has a systolic effect, has little effect on heart rate and conduction in the atrioventricular bundle.

Application: acute cardiovascular failure, paroxysmal tachycardia. Enter / in 0,5-1 ml of a 0,025% or 0,05% solution in 10-20 ml of a 40% glucose solution. V. R. D. - 1 ml of a 0,05% solution, V. S. D. - 2 ml of a 0,05% solution.

Side effects: like meproscillarin.

Contraindications: organic lesions of the heart and blood vessels, acute myocarditis, endocarditis, severe cardiosclerosis.

Product form: 1 ml ampoules of 0,025% and 0,05% solution No. 10. List B.

Korglikon (Corgliconum).

Purified preparation from the leaves of May lily of the valley. It is similar to convallatoxin and strophanthin, but gives a longer effect.

Application: chronic and acute insufficiency, paroxysmal tachycardia. Enter slowly 0,5-1 ml of a 0,05% solution in 20 ml of a 40% glucose solution. V. R. D. - in / in 1 ml, V. S. D. - 2 ml.

Side effects: the same as in strophanthin.

Product form: 1 ml ampoules of 0,06% solution No. 10. List B.

Non-steroidal and synthetic cardiotonics.

Korotrop (Korotrop).

The active substance is milrinone lactate.

Application: acute and chronic heart failure in the stage of decompensation. Start with a slow intravenous loading dose of 50 mcg/kg body weight, then switch to a maintenance dose of 0,375-0,75 mcg/kg per 1 minute. The maximum daily dose is 1,13 mcg/kg body weight.

Side effects: heart rhythm disturbance, angina pectoris, hypotension, headache, allergic reactions.

Product form: solution for injections of 10 ml in ampoules No. 10 (in 1 ml 1 g of corotrope).

Escandin (Escandin).

The active substance is ibopamine hydrochloride. It has a positive inotropic effect, causes an increase in stroke and minute volumes of the heart, improves kidney perfusion, increases diuresis, reduces the load on the myocardium, reduces the production of norepinephrine, renin and aldosterone, in therapeutic doses does not affect blood pressure and heart rate.

Application: chronic heart failure. The dose is set individually. Single dose - 50-200 mg, frequency of administration 2-3 times a day, 1 hour before meals.

Side effects: from the gastrointestinal tract sometimes nausea, heartburn, gastralgia, tachycardia is possible.

Contraindications: ventricular arrhythmias, pheochromocytoma, pregnancy, lactation.

Product form: tablets 50 and 100 mg No. 30.

Dobutrex (Dobutrex).

The active substance is dobutamine hydrochloride.

Application: acute heart failure, acute myocardial infarction, cardiogenic shock, acute decompensation of chronic heart failure.

Mode of application: individual and adjusted taking into account the patient’s reaction. The infusion rate is from 2,5 to 10 mcg/kg per 1 min. Possibly - up to 20 mcg/kg per minute, rarely - 1 mcg/kg per minute.

Side effects: cardiac arrhythmia, hypotension, angina pectoris, shortness of breath, phlebitis at the injection site.

Product form: concentrate for infusion 20 ml in a vial, 1 vial contains 250 mg of the active substance.

5. Antiarrhythmic drugs. Classification

Antiarrhythmic drugs - drugs that have a normalizing effect on the disturbed rhythm of heart contractions, belong to different classes of chemical compounds and belong to different pharmacological groups. But there are a number of drugs for which the main action is a normalizing effect on the heart rhythm in various types of arrhythmias. Drugs are divided into four groups (classes):

1) membrane stabilizing agents (quinidine-like) - class I;

2) β-blockers - class II;

3) drugs that slow down repolarization (the main representative is amiodarone, sympatholytic ornid) - class III;

4) calcium channel blockers (antagonists of calcium ions) - class IV.

Class I includes a number of drugs that are divided according to some features of the action. They are conditionally divided into three subgroups:

1) subgroup IA - quinidine, novocainamide, ethmozine, disopyramide;

2) subgroup IB - local anesthetics (lidocaine, trimecaine, pyromecaine), as well as mexiletine and difenin;

3) subgroup IC - aymalin, etatsizin, allapinin.

Group I antiarrhythmic drugs.

Quinidine sulfate (Chinidini sulfas).

Dextrorotatory isomer of quinine.

Application: paroxysmal tachycardia, paroxysmal atrial fibrillation, extrasystoles, persistent atrial fibrillation. Take 0,1 orally 4-5 times a day, if necessary - up to 0,8-1,6 g per day.

Side effects: in case of overdose - depression of cardiac activity, nausea, vomiting, diarrhea, sometimes atrial fibrillation.

Contraindications: decompensation of the cardiovascular system, pregnancy.

Product form: powder, tablets 0,1 No. 20.

Novocainamide (Novocainamidum).

It reduces the excitability of the muscles of the heart, suppresses ectopic foci of excitation, and has a local anesthetic property.

Application: cardiac arrhythmias.

Mode of application: 0,5-1 g is prescribed orally 3-4 times a day; IM - 5-10 ml of a 10% solution, IV (drip) for relief of acute attacks - 2-10 ml of a 10% solution in a 5% glucose solution or 0,9% sodium solution chloride

Side effects: collatoptoid reactions, general weakness, headache, nausea, insomnia.

Contraindications: severe heart failure, conduction disturbance.

Product form: tablets of 0,25 g No. 20, ampoules of 5 ml of a 10% solution No. 10.

Aymalin (Ajmalinum).

An alkaloid found in some types of rauwolfia.

Application: cardiac arrhythmia, arrhythmia caused by digitalis intoxication, recent myocardial infarction.

Mode of application: administered intramuscularly - 0,05-0,15 g per day, to relieve an acute attack of tachycardia intravenously - 2 ml of a 2,5% solution in 10 ml of 0,9% sodium solution. To eliminate arrhythmia, take 0,1 g orally 3-4 times a day.

Side effects: weakness, nausea, vomiting, lowering blood pressure, with a / in the introduction of a feeling of heat.

Contraindications: severe disorders of the conduction system of the heart, severe heart failure, hypotension, inflammatory changes in the myocardium.

Product form: coated tablets, 0,05 g No. 200, 2 ml ampoules of 2,5% solution No. 10.

6. Antiarrhythmic drugs I and II class

Group I also includes the following drugs.

Etmozin (Aetmozinum).

Application: rhythm disturbance, effective in overdose of cardiac glycosides.

Mode of application: initial dose - 75-200 mg per day (25-50 mg 3-4 times a day) depending on the form of arrhythmia and tolerability. Maintenance therapy - reduced dose by 1/3. The course of treatment is 7-45 days.

Side effects: slight soreness in the epigastrium, slight dizziness.

Contraindications: severe disorders of the conduction system of the heart, severe hypotension, impaired liver and kidney function, monoamine oxidase inhibitors.

Product form: coated tablets, 0,1 g No. 50, 2,5% solution in 2 ml ampoules No. 10.

Ethacizine (Aethcizinum).

It has antiarrhythmic action, local anesthetic and antispasmodic activity.

Application: arrhythmias of various etiologies.

Mode of application: prescribed orally, 1 tablet 3-4 times a day, regardless of meals; IV (administration time not less than 5 minutes) - 2 ml of a 2,5% solution in 20 ml of a 0,9% sodium chloride solution.

Side effects: dizziness, noise in the ears and head, numbness and burning sensation of the lips and the tip of the tongue, a "mesh" before the eyes, staggering when ingested, disturbance of accommodation. In such cases, the reception is stopped.

Contraindications: cardiac conduction disorders, severe heart failure, hypotension.

Product form: 2,5% solution in ampoules of 2 ml No. 10, coated tablets of 0,05 g, No. 50.

Ritmilen (Rytmilen).

It is used in the same way as etatsizin, and for surgical interventions.

Mode of application: rhythmylene is quickly and almost completely absorbed from the gastrointestinal tract, but no significant hemodynamic changes are observed; with intravenous administration, blood pressure may decrease. The initial daily dose orally is 0,2-0,3 g, then, depending on the patient’s condition, 0,3-0,8 g in 3-4 doses. With intramuscular administration - 0,001-0,002 g/kg body weight.

Side effects: difficulty urinating, urinary retention, dry mouth, headache. When canceled, the phenomena disappear.

Contraindications: complete atrioventricular block, cardiogenic shock, pregnancy, childhood.

Product form: capsules of 0,1 No. 100, 1% solution in ampoules of 5 ml No. 10, tablets of 0,1 g No. 100.

Group II antiarrhythmic drugs.

Lidocaine (Lidocinum).

Was considered in the group of local anesthetics.

Allapinin (Allapininum).

An antiarrhythmic drug that does not have a negative inotropic property, does not cause arterial hypotension, has a local anesthetic and sedative effect. It is used to treat arrhythmias.

Mode of application: 0,025 g orally, after crushing the tablets, 30 minutes before meals, washed down with warm water. If there is no effect, prescribe 0,025 g every 6 hours up to 0,05 g per dose. The course of treatment is individual. Higher doses: single - 0,15 g, daily - 0,3 g.

Side effects and contraindications: the same as for rhythmylene.

Product form: tablets of 0,025 g No. 30. This group also includes trimecaine, mexitil, difenin, propafenone, etc.

7. Class III antiarrhythmic drugs

This group includes β-blockers (anaprilin, inderal, obzidan), trazikor, aptin.

Anaprilin (Anaprillin).

Was considered in the group of β-adrenergic blockers.

Whisken (Visken).

It has antianginal, antiarrhythmic and hypotensive effects, has internal sympathomimetic activity.

Application: angina pectoris, arrhythmia, hyperkinetic syndrome, hypertension.

Mode of application: prescribed in cardiology - 1 tablet 3 times a day (sometimes 4 times a day) after meals. The maximum dose is 3 tablets 3 times a day.

Side effects: at the beginning of treatment, bradycardia, bronchospasm, headache, drowsiness, dizziness, gastrointestinal upset, nausea, passing on their own, may occur.

Contraindications: cardiac decompensation, shock, sinus bradycardia, cor pulmonale, ether anesthesia.

Product form: tablets 5 mg No. 30.

Trazikor (Trasicor).

Specific blocker of sympathetic β-adrenergic receptors; has antiarrhythmic properties.

Application: rhythm disturbances of various origins, angina pectoris.

Mode of application: prescribed orally at 0,02 g 2-3 times a day, if necessary - 0,08-0,12 g per day.

Side effects: dyspepsia, weakness, dizziness, heart failure.

Contraindications: bronchial asthma, atrioventricular blockade, bradycardia.

Product form: tablets of 0,02 and 0,08 g No. 40.

8. Class IV antiarrhythmic drugs

The drugs in this group have antiadrenergic properties and do not affect membranes.

Kordaron (Cordarone).

Decreases the heart rate. Attacks of stenocardia disappear or happen less often.

Application: chronic coronary insufficiency, arrhythmia.

Mode of application: Initially, 0,2 g is prescribed 3 times a day during or after meals. After a week - up to 0,1 g 3 times a day or 0,2 g 2 times a day. The course of treatment is 2-3 weeks, repeated after 1-2 weeks. For arrhythmia, intravenous injection is administered.

Side effects: dyspepsia, euphoria, increased irritability, with prolonged use - bradycardia.

Contraindications: bradycardia, pregnancy, bronchial asthma.

Product form: tablets of 0,2 g No. 50, ampoules of 3 ml of a 5% solution No. 5.

Finoptin (Finoptin).

Synonyms: Isoptin, Verpamil.

The action is the same as that of cordarone, but it also has natriuretic and diuretic properties.

Application: the same as that of cordarone, in addition, it is prescribed for the prevention of myocardial infarction and in the postinfarction period.

Mode of application: take 0,04-0,08 g orally 3 times a day, intravenously - 2-4 ml of a 0,25% solution 1-3 times a day.

Side effects: nausea, dizziness.

Contraindications: cardiogenic shock, atrioventricular conduction disturbances. Combination with β-blockers.

Product form: tablets of 0,04 g No. 100, 0,25% solution in ampoules of 2 ml (5 mg) No. 25.

Fenigidin (Phenihidine).

Synonyms: Corinfar, Adalar, Nifedipin. Used for cardiac ischemia with angina attacks, especially in combination with hypertension, sublingually 0,02 g 2-3 times a day. Maintenance dose - 0,01 g 3 times a day. The course of treatment is 1-2 months. After taking the drug, lie down for 30-60 minutes. For hypotension - 0,01 g 3 times a day with blood pressure monitoring.

Side effects: headache, palpitations.

Contraindications: pregnancy.

Product form: tablets 0,01 No. 40.

This group also includes ornid (Ornidum).

LECTURE No. 20. Means that improve the blood supply to organs and tissues

1. Means that improve blood supply and myocardial metabolism

The list of drugs used to eliminate disorders of the blood supply and metabolism of the myocardium includes antianginal drugs, which include organic nitrates, calcium ion antagonists, β-blockers and other drugs that affect the adrenergic innervation of the heart, antispasmodics, etc. And as antianginal ( additional) agents - drugs that increase the overall resistance of body tissues to hypoxia and improve general metabolic processes.

Antianginal drugs.

This is a group of drugs with different mechanisms of action used to treat angina pectoris. Three groups of drugs are used as highly effective: nitrates, β-adrenergic blockers and calcium antagonists.

Nitro-containing drugs.

The main drugs for the treatment of angina pectoris. The most common are nitroglycerin and its various forms, nitrosorbitol.

Nitroglycerine (Nitroglycerine).

Expands blood vessels, relaxes the smooth muscles of the gastrointestinal tract, biliary tract.

Application: prescribed for the relief of angina attacks, sometimes with biliary dyskinesia and embolism of the central retinal artery.

Mode of application: take 1/2-1 tablet (or 1-2 drops of a 0,5-1% solution) sublingually.

Side effects: tinnitus, headache, dizziness, collapse.

Contraindications: glaucoma, increased intracranial pressure, cerebrovascular accident, acute period of myocardial infarction, cerebral atherosclerosis.

Product form: tablets of 0,0005 g No. 40, vials of 10 ml of a 1% solution, capsules No. 20 with 0,0005 g of a 1% solution in oil.

Trinitrolong (Trinitrolong).

Oval-shaped polymer films containing 1 or 2 mg of nitroglycerin. It is used as a prolonged preparation of nitroglycerin. Trinitrolong plate is pressed with fingers to the oral mucosa after eating.

Product form: polymer plates No. 50, 0,001 and 0,002 g each.

Sustak (Sustac).

Long-acting dosage form of nitroglycerin. It is used only to prevent attacks of angina pectoris, 2,6 mg (Sustak-Mite) 2 times a day, if necessary - 6,4 mg (Sustak-Forte) per dose.

Side effects: like nitroglycerin.

Contraindications: acute myocardial infarction, glaucoma, cerebral hemorrhage, coronary thrombosis.

Product form: tablets Sustak-mite 2,6 mg and Sustak forte 6,4 mg No. 25.

Nitrong (Nitrong).

Similar to joint.

Product form: tablets 2,6 mg No. 50 and 100.

Nitrodur (Nitrodur).

The transdermal therapeutic system (TTS) is a long-acting nitroglycerin preparation (24 hours duration) used to prevent angina attacks.

Mode of application: the initial dose is 400 mcg / h or 10 mg per day. TTC is glued for 12-14 hours, after which it is removed, after 12 hours it is glued again on a dry, clean area of ​​\uXNUMXb\uXNUMXbthe skin.

Product form: TTS in the form of a patch with an area of ​​20 cm2 and a release rate of the active substance of 10 mg per day No. 28.

2. Other drugs that improve blood circulation and myocardial metabolism

Erinite (Erynitum).

Slower absorbed than nitroglycerin.

Application To prevent attacks in chronic coronary insufficiency, it is prescribed orally or sublingually at 0,01-0,02 g 2-3 times a day.

Side effects and contraindications: the same as for nitroglycerin.

Product form: tablets of 0,01 g No. 50.

Nitrosorbite (Nitrosorbidum).

Synonyms: Carvasin, Dinitrate, Isoket, Isosorbit. Similar to erinite, but the action is longer. It is absorbed from the gastrointestinal tract after 20-30 minutes.

Application, side effects, contraindications: the same as nitroglycerin.

Product form: tablets of 0,01 g No. 25.

Nitromaz (Nitro 2% voide-salva).

Ointment containing glyceryl nitrates is absorbed through the skin slowly, which leads to a long-term effect.

Application: angina pectoris, for adults only, individual dosage. An effective single dose of 7,5-30 mg (2-8 cm) of 2% ointment, which is applied to a special paper 10 x 6 cm in size and applied to the left upper chest. Depending on the condition of the patient, the ointment can be applied 1-3 times a day.

Side effects: redness of the face, dizziness, tachycardia, headache. In patients who have been taking nitroglycerin for a long time and abruptly finished taking it, angina pectoris may worsen.

Contraindications: pregnancy, lactation, severe anemia, pronounced narrowing of the lumen of the cerebral vessels.

Product form: in tubes of 45 g of ointment.

cardiket (Kardiket).

Reduces myocardial oxygen demand, has a direct coronary dilating effect, improves blood supply to the subendocardium.

Application: prevention of angina attacks, rehabilitation treatment after myocardial infarction, pulmonary hypertension, treatment of chronic heart failure.

Mode of application: set individually, taking into account the stage of the disease. Retard tablets are prescribed 0,02 g 2-3 times a day, or 0,04 g 2 times a day, or 0,06 g 1-2 times a day. Capsules retard appoint 0,12 g 1 time per day, preferably in the morning. Kardiket is taken after a meal, without chewing and drinking a small amount of liquid. The interval between doses is at least 8 hours.

Side effects: headache, arterial hypotension, drowsiness, tachycardia, nausea, vomiting, erythema.

Contraindications: acute phase of myocardial infarction, low left ventricular filling pressure, shock, vascular collapse, systolic pressure less than 90 mm Hg. Art.

Product form: retard tablets No. 50 and 100 (isosorbitol dinitrate 0,02, 0,04, 0,06 g each). Retard capsules in a package of 20 and 50 pieces, 1 capsule contains isosorbitol dinitrate 0,12 g.

3. Antagonists of calcium ions

Antagonists of calcium ions.

Substances that inhibit the passage of Ca2+ through calcium are called calcium ion antagonists. The main (typical) representatives of this group are verapamil, nifedipine (fenigidin), diltiazem, which are divided into three subgroups:

1) phenylalkylamines (verapamil, gallopamil);

2) dehydropyridines (nifedipine, nitrendipine, amlodipine, nicardipine);

3) benzothiazepines (diltiazem).

Calcium ion antagonists also include cinnarizine and flunarizine, but due to their non-selective action they are not classified as typical drugs in this group. The main use of calcium ion antagonists is as cardiovascular agents.

By causing vasodilation and reducing peripheral vascular resistance, they reduce blood pressure, improve coronary blood flow, and have an antianginal effect. Drugs that affect the excitability and conduction of the heart are used as antiarrhythmic drugs.

There are the following classes of selective calcium channel blockers:

1) verapamil, isoptin, coveril, finoptin - class I;

2) corinfar, nifedipine, etc. - class II;

3) cardil, diltiazem, etc. - class III;

4) calcium channel locators with effects on cerebral vessels (cinnarizine, flunarizine) - class IV;

5) prenylamine - class V;

6) posicor - VI class.

Verapamil (Verapamil).

It has antianginal, antiarrhythmic and hypotensive effects.

Application: angina pectoris, arterial hypertension, prevention of cardiac arrhythmias.

Mode of application: prescribed orally for angina pectoris 120 mg 3 times a day, for hypertension - 120 mg 2 times a day, increasing to 160 mg 2 times a day, for the prevention of cardiac arrhythmias - 40-120 mg 3 times a day.

Side effects: bradycardia, hypotension, AV blockade, nausea, vomiting, headache, dizziness.

Contraindications: severe bradycardia, AV block II-III degree, acute heart failure, chronic insufficiency II-III degree, hypotension.

Product form: tablets 40 and 80 mg No. 50.

Cardil (cardil).

The active substance is diltiazem.

Application: angina pectoris, arterial hypertension.

Mode of application: tablets 30 mg 3-4 times a day, 60 mg - 1 / 2-2 tablets 3-4 times a day (usually 1 tablet 3 times a day), 120 mg of prolonged action 1 or 1/2 tablets 1-2 times a day. The dose of cardil is selected strictly individually.

Side effects: headache, fatigue, nausea, irritation of the gastric mucosa, skin rashes.

Contraindications: acute stage of myocardial infarction, cardiac shock, atrioventricular conduction disturbances.

Product form: tablets of 30 and 60 mg No. 100. Long-acting tablets of 120 mg No. 100.

Cinnarizine (Cinnarizinum).

Synonym: stugeron (Stygeron). The drug selectively improves cerebral circulation, relaxes the smooth muscles of blood vessels, is a calcium antagonist.

Application: ischemic disorders of cerebral circulation associated with hypertension and cerebral atherosclerosis, migraine, menopausal vascular disorders, peripheral circulation disorders.

Mode of application: take orally 0,025-0,05 g 2-3 times a day as a vasodilator and antispasmodic.

Product form: tablets of 0,025 g No. 50.

Pozikor (Posicor).

Contains 50 or 100 mg of mibefradil hydrochloride No. 14, 28 or 98. Take initially 50 mg 1 time per day, possibly increasing to 100 mg per day. Used as a selective calcium channel blocker.

4. Other antianginal drugs

Other antianginal drugs.

Curantyl (Curantil).

Coronary expander.

Application: chronic coronary insufficiency.

Mode of application: take orally 0,025-0,025 g 3-6 times a day, intramuscularly or intravenously, 1-2 ml of a 0,5% solution.

Product form: tablets of 0,025 g No. 100, ampoules of 2 ml of a 0,5% solution No. 5.

Carbocromen (Carbocromenum).

Synonyms: Intensain, Intencordin. This is an antianginal agent.

Application: ischemic heart disease with angina attacks.

Mode of application: prescribed orally after meals, 150 mg 3 times a day for 0,5-1,5 months. After achieving a therapeutic effect, the patient is transferred to maintenance doses - 75 mg 3 times a day.

Side effects: headache, general weakness, dry mouth, nausea, vomiting, pruritus.

Contraindications: peptic ulcer of the stomach and duodenum, exacerbation of chronic gastritis, diseases of the liver and kidneys with impaired function.

Product form: tablets of 0,075 g No. 100.

Kordaron (Cordarone).

Antianginal and antiarrhythmic agent. Its mode of action is twofold: direct action on smooth muscles, especially vessels, and antiadrenergic action.

Indications: angina pectoris, coronary insufficiency, myocardiopathy, rhythm disturbances of various origins, conditions after myocardial infarction.

Mode of application: 1 tablet 3 times a day for 1 week. Then 1 tablet 2 times a day. After 15 days from the start of treatment, 1 tablet 1 time per day for 5 days. In case of an attack of arrhythmia - intravenous drip of 5 mg/kg body weight in 250 ml of 5% glucose solution. If necessary, infusions are repeated after 24 hours.

Side effects: nausea, heaviness in the epigastrium, bradycardia, irritability, euphoria.

Contraindications: bradycardia (pulse up to 60 beats per minute) and disorders of the conduction system of the heart, pregnancy. For bronchial asthma - with caution.

Product form: 1 tablet contains 200 mg of amiodarone chloride in package No. 60. In one ampoule (3 ml) 150 mg of amiodarone chloride, in a package - 5 ampoules.

Sidnopharm (Sydnopharm).

Contains molsidomine, a substance of the syndonimine class, capable of eliminating oxygen starvation of the heart muscle by acting on the peripheral circulatory system without affecting the myocardium.

Application: angina attacks.

Mode of application: orally 1/2-1 tablet 2-3 times a day after meals, for a quick effect - sublingually. The duration of action of the drug is 6-8 hours.

Side effects: at the beginning of treatment - a headache, a decrease in blood pressure, passing after a dose reduction.

Contraindications: hypotension, cardiogenic shock, acute myocardial infarction, pregnancy.

Product form: tablets of 0,002 g No. 30.

LECTURE No. 21. Drugs that improve cerebral circulation

1. Drugs that improve the metabolic processes of the brain

Drugs that positively affect the blood supply to the brain, increase its oxygen supply and enhance metabolic processes in it, and also simultaneously have general antispasmodic activity and cause vasodilation and improve blood circulation in various organs and tissues, belong to the group of drugs that improve cerebral circulation.

Cavinton (Cavinton).

1 tablet contains 5 mg of apovincamic acid ethyl ester, 1 ampoule (2 ml) - 10 mg of this substance. Cavinton selectively improves cerebral blood flow and oxygen supply to the brain without lowering blood pressure or having a direct effect on the heart.

Application: disorders of cerebral blood flow of various etiologies with mental and neurological disorders. Diseases of the vascular and retinal membranes of the eyes caused by atherosclerosis or angiospasm, partial thrombosis, secondary glaucoma caused by blockage of blood vessels. Age-related vascular or toxic lesions of the auditory nerve, dizziness of labyrinthine origin.

Mode of application: for acute disorders, 3 mg IV is prescribed 10 times a day, then 1-2 tablets orally 3 times a day; maintenance dose - 1 tablet 3 times a day.

Contraindication: pregnancy.

Product form: tablets of 0,005 g No. 50, ampoules of 2 ml (10 mg) No. 10.

Sermion (Sermion).

It activates metabolism, reduces the tone of cerebral and peripheral vessels, reduces cerebrovascular resistance and increases cerebral blood flow.

Application: acute and chronic cerebral and peripheral vascular-metabolic disorders, intramuscularly 4 mg are distributed into 1-2 injections per day, intravenously 4-8 mg in 100 ml of 0,9% sodium chloride solution, but methods of administration, doses and time is selected individually.

The solution ready for injection can be stored at room temperature for up to 48 hours.

Side effects: dizziness, drowsiness, insomnia.

Product form: tablets of 0,01 No. 30, 4 vials of 4 mg and 4 ampoules, with a solvent of 4 ml.

Oksibral (Oxybral).

Preparation from periwinkle minor. Action, like Cavinton.

Application: dizziness, cerebral vascular damage of various origins; weakening and memory disorder, migraine, to improve intellectual abilities in children. Orally, 1 capsule retard 2 times a day. If necessary, parenterally 2 ml 1-2 times a day.

Side effects: allergic reactions, skin rash.

Contraindications: brain tumor, pregnancy.

Product form: retard capsules 0,03 No. 10, 20, 60, injection solution 2 ml No. 5 (1 ml - 0,0075 g of active substance).

2. Other drugs in this group

Flunarizine (Flunarizin).

Calcium antagonist with a predominant effect on the vessels of the brain.

Application: stroke, migraine prevention, psychomotor syndrome in the elderly, vestibular disorders.

Mode of application: appoint inside 20 mg 1 time per day, then reducing the dose to 10 mg (5 mg in the morning and evening).

Side effects: drowsiness, nausea, dry mouth, stomach pain, skin rash. In high doses, nausea, vomiting, collapse and other reactions that occur with theophylline are possible.

Contraindications: acute myocardial infarction, heavy bleeding, hemorrhages, severe coronary and cerebral sclerosis with hypertension, pregnancy.

Product form: dragee 100 mg No. 60, 400 mg No. 20, 5 ml ampoules (100 mg) No. 5.

Tanakan (Tanakan).

Standardized herbal extract of gingo biloba. Improves cerebral circulation and supply of oxygen and glucose to the brain, normalizes metabolic processes. Used for the consequences of a stroke and traumatic brain injury.

Mode of application: prescribed orally, 1 tablet 3 times a day with meals, 10-20 drops 3 times a day. The course of treatment is 3 months.

Side effects: indigestion, headaches.

Product form: film-coated tablets, 40 mg No. 30, 30 ml solution.

Pyracetam (Pyracetamum).

Synonym: Nootropyl. It has a positive effect on the metabolic processes of the brain.

Application: chronic and acute cerebrovascular accidents, coma after injuries and intoxications of the brain, diseases of the central nervous system.

Mode of application: in severe conditions, 2-6 g per day is administered intramuscularly or intravenously. For chronic conditions - 1,02-2,04 g per day (sometimes up to 3,2 g per day or more) in 3-4 doses.

Side effects: hyperstimulation, dyspeptic phenomena, exacerbation of angina pectoris is possible in elderly patients.

Contraindications: pregnancy, acute renal failure.

Product form: capsules of 0,4 g No. 60, ampoules of a 20% solution No. 10, coated tablets of 0,2 No. 120.

Cerebrolysin (Cerebrolysinum).

Hydrolyzate of the medulla containing 18 amino acids. Helps improve metabolism in the brain tissue.

Indications: diseases accompanied by dysfunction of the central nervous system.

Mode of application: injected i / m 1-2 ml every 3 days. The course of treatment is 20-40 injections.

Product form: in ampoules of 1 ml No. 10, 5 ml of 5% solution No. 5.

3. Peripheral vasodilators and calcium antagonists

These drugs act mainly on the most distal parts of the vascular system, they determine mainly the resistance of peripheral vessels and the deposition of blood in the venous bed.

These include organic nitrates (nitroglycerin, nitrosorbitol, etc.) sodium nitroprusside, molsidomine, prarosin, apressin. They are used in the complex therapy of heart failure, acute myocardial infarction, arterial hypertension. Drugs of this group should be used with careful hemodynamic control with strict adherence to doses, as they can greatly lower systemic blood pressure, cause a collaptoid state, and worsen the blood supply to the heart.

Apressin (Apressinum).

Synonyms: Apresoline, Hydralazine. Lowers blood pressure, has an adrenolytic and sympatholytic effect.

Application: hypertension, eclampsia, renal failure. The initial dose is 0,01 g 2 times a day, administered orally after meals, up to 0,025 g 4 times a day. The course of treatment is several weeks with a gradual reduction in dose.

Side effects: tachycardia, pain in the heart area, headache, orthostatic collapse, nausea, rash, edema of various localization, sweating, fever.

Contraindications: severe atherosclerosis.

Product form: coated tablets, 0,01 and 0,025 g No. 20.

Naniprus (Naniprus).

Synonyms: Nitroprusside natrium, Nipride. Lyophilized form of sodium nitroprusside in ampoules with sodium citrate stabilizer. It has a pronounced vasodilating effect, as a result of exposure to the walls of the arteries, blood pressure decreases and the postcardiac load is reduced.

Application: hypertensive crises of any origin, malignant hypertension, acute left-sided heart failure during myocardial infarction. It is used exclusively as a drip infusion into a vein, the initial dose is 0,5-5 mg/kg body weight (usually 2-8 mg/kg per 1 min), and only a freshly prepared solution. Do not mix with solutions of other medications.

Contraindications: cerebral hemorrhage, impaired cyanide metabolism. Caution in the presence of arteriovenous anastomosis and increased intracranial pressure.

Product form: dark glass ampoules of 10 ml containing 30 mg of naniprus. In the package, an ampoule containing 5 ml of solvent is attached to the ampoule. The antianginal effect of calcium antagonists is associated with their direct effect on the myocardium and coronary vessels, which leads to an increase in blood flow in them, a decrease in peripheral resistance and systolic blood pressure. There are drugs with a relatively selective effect on the cerebral vessels of this group (nimodipine).

Nimotop (Nimotop).

The active substance is nimodipine.

Application: for the prevention of spasm of cerebral vessels and the treatment of ischemic disorders of cerebral circulation caused by subarachnoid hemorrhage, brain injury. The course in / in, introductions begin with a dose of 1 mg (5 ml of solution) per hour. Taking into account the body weight of the patient for 1 hour, about 15 μg / kg is administered. Then the dose is increased to 2 mg / h (about 30 mcg / kg in 1 hour). Tablets are taken at a dose of 60 mg 6 times a day for 7 days.

Side effects: hypotension, tachycardia, headache, insomnia, agitation, impaired renal function.

Contraindications: pregnancy, lactation, severe liver dysfunction.

Product form: tablets of 30 mg No. 30, solution for infusion - 50 ml in bottles No. 5 (1 mg of the active substance in 10 bottle).

LECTURE No. 22. Antihypertensive drugs

1. Classification of antihypertensive drugs

Antihypertensive (hypotensive) drugs are drugs of various chemical groups that reduce systemic blood pressure and are used to treat and prevent arterial hypertension, relieve hypertensive crises and other pathological conditions based on spasm of peripheral blood vessels. The mechanism of action is determined by the degree of their influence on the regulation of vascular tone. They are divided into the following groups:

1) drugs that affect the vasomotor (vasomotor) centers of the brain (clophelin, methyldopa, guanfazine);

2) agents that block the conduction of nervous excitation at the level of autonomic ganglia (benzogexonium, pentamine, etc.);

3) sympathetic agents that block the presynaptic endings of adrenergic neurons (octadin, reserten);

4) agents that inhibit α- and β-adrenergic receptors (phentolamine, tropafen, prazosin, anaprilin, atenolol and other α- and β-blockers;

5) myotropic antihypertensive drugs (papaverine, noshpa, etc.);

6) calcium channel antagonists;

7) angiotensin-converting enzyme blockers (captoproil, ramipril (tritace), quinapril (accupro), cilazapril (inhibais), perigdopril (prestarium), etc.);

8) drugs of the prostaglandin group (prostin BP);

9) aldosterone antagonists (spironolactan);

10) diuretics;

11) combined preparations.

Means that affect the vasomotor (vasomotor) centers of the brain.

Clophelin (Clophelinum).

Synonyms Haemitonum, Catapresan, Chlophaxolin. It has a pronounced hypotensive effect, lowers blood pressure, slows down the heart rate, has a sedative effect and lowers intraocular pressure.

Application: all types of arterial hypertension and for the relief of hypertensive crises, primary open-angle glaucoma. Used orally 0,000075 g 2-4 times a day, daily dose - 0,3-0,45 mg, sometimes 1,2-1,5 mg, course of treatment - up to 6-12 months. 0,5-1,5 ml of a 0,01% solution is administered intramuscularly and subcutaneously. For intravenous administration, 0,5-1,5 ml of a 0,01% solution is diluted in 10-20 ml of a 0,9% sodium chloride solution and administered slowly over 3-5 minutes. Parenterally administered only in a hospital or emergency setting. For glaucoma - in the form of instillations into the eye of 0,0125, 0,25 or 0,5% solutions 2-4 times a day without miotics or in combination with them. If the visual field condition is stable, it is used for a long time, sometimes for years; if there is no effect within 1-2 days, it is canceled.

Side effects: dry mouth, weakness, drowsiness, with large doses - constipation, orthostatic collapse. In ophthalmic practice, there may be an undesirable decrease in blood pressure and bradycardia.

Contraindications: persons whose work requires quick mental and motor reactions. In eye practice - pronounced atherosclerosis of cerebral vessels, arterial hypotension.

Product form: tablets of 0,000075 and 0,00015 g No. 50, ampoules of 1 ml of 0,01% solution No. 10, tube-droppers No. 2 of 1,5 ml of 0,125, 0,25% and 0,5% solution.

Drugs that block the conduction of nervous excitation at the level of autonomic ganglia, were considered in the topic "Ganglioblockers".

Sympatholytic drugs that block the endings of adrenergic neurons - in the topic "Sympatholytics".

means of oppression β- And α-adrenergic receptors - in the topic "Adrenoblockers".

2. Preparations of this group

papaverine hydrochloride (Papaverini hydrochloridum).

Myotropic antispasmodic drug.

Application: cerebral vascular spasms, angina pectoris, cholecystitis, pylorospasm, urinary tract spasm, bronchospasm, hypertension. Prescribed orally 0,04-0,06 g 3-5 times a day, subcutaneously - 1-2 ml of a 2% solution 2-4 times, with acute spasm of the coronary vessels and smooth muscles of the abdominal organs intravenously c (slowly) - 1 ml of 2% solution.

It is prescribed orally per se, as well as in combination with phenobarbital, etc. It is part of suppositories. V.R.D. orally - 0,4 g, V.S.D. - 0,6 g, parenteral daily dose - 0,3 g.

Side effects: atrioventricular block, ventricular extrasystole, with intravenous administration - decreased blood pressure, constipation.

Product form: powder, tablets of 0,01 g (for children) No. 10; 0,04 No. 10, ampoules of 2 ml of a 2% solution No. 10, rectal suppositories of 0,02 g No. 10.

Dibazol (Dibazolum).

Vasodilator, antispasmodic and hypotensive agent.

Application: diseases accompanied by spasms of blood vessels, residual effects of polio. Orally prescribed per se and in combination with papaverine, theobromine, phenobarbital 0,02 g 2-3 times a day, subcutaneously - 1-5 ml of a 1% solution.

Side effects: with caution in the elderly.

Product form: powder, tablets of 0,004 g with a score and 0,02 No. 10, ampoules of 1% solution No. 10 of 1 and 5 ml.

Noshpa (No-spa).

It has a pronounced antispasmodic, but weak hypotensive effect.

Application: spasms of the stomach and intestines, spasmodic constipation, attacks of cholelithiasis and urolithiasis, angina pectoris. Prescribed orally 0,04-0,08 g 2-3 times a day, intravenously (slowly) - 2-4 ml of a 2% solution, if necessary - intra-arterially (obliterating endarteritis).

Side effects: dizziness, palpitations, sweating, feeling hot, allergic dermatitis.

Product form: tablets of 0,04 g No. 100, ampoules of 2 ml containing 0,04 g of the drug, No. 50.

calcium channel antagonists discussed in the topic "Calcium ion antagonists".

Angiotensin-converting enzyme blockers.

This group of drugs is involved in the metabolism of the aldosterone-angiotensin-renin system.

From the ACE group, captopril and enap (enalapril) are widely used as medicines.

Capoten (Capoten).

Synonym: captopril. An effective remedy for heart failure and hypertension. It is recommended for patients who cannot be treated with conventional therapy to use it together with diuretics. The initial dose is 25 mg 2-3 times a day. If after 2 weeks there is no decrease in blood pressure, you can take up to 50 mg 2-3 times a day. The drug is taken under medical supervision. For heart failure - 25 mg 3 times a day. The maximum daily dose is 450 mg.

Side effects: itching, redness of the face, abdominal pain.

Product form: tablets 25 mg No. 40.

Enap (Enap).

Synonyms: enalapril, renitek. It is used as capoten: orally from 10 to 20 mg per day, up to 40 mg per day (in 2 doses). The maximum daily dose is 80 mg. When taken, hypotension and dizziness are possible. Contraindicated in severe liver and kidney damage, pregnancy, and lactation.

Product form: tablets 10 and 20 mg No. 20.

3. Preparations of the prostaglandin group

Prostin BP (Prostin VR).

Causes vasodilating, hypotensive and antiplatelet effects.

Application: congenital heart defects, arterial hypertension.

Mode of application: Continuous infusion through one of the major veins or through the umbilical arterial stream is recommended. The initial dose is 0,05-0,1 mcg per 1 minute, up to 0,4 mcg/kg per minute is possible.

Side effects: respiratory failure, bradycardia, cardiac arrhythmias.

Contraindications: acute respiratory distress syndrome.

Product form: concentrate for infusion: 0,2 ml - 100 mcg; 0,5 ml - 250 mcg, 1 ml - 500 mcg, 1-5 pieces per package.

Aldosterone antagonists.

These include spironolactone, according to the mechanism of action, it is a competitive aldosterone antagonist. It is prescribed for arterial adrenal hypertension.

Veroshpiron (Verospiro n).

Synonym: spironolactone. It has a pronounced diuretic and hypotensive effect.

Application: edema caused by cardiovascular failure, liver cirrhosis. Orally prescribed 0,075-0,3 g per day. Adults usually take 0,1-0,2 in 2-4 doses. When the condition improves - up to 0,025 g.

Side effects: dizziness, drowsiness, dermatoses, hyponatremia and hyperkalemia are possible.

Contraindications: acute renal failure.

Product form: tablets of 0,025 g No. 20.

Diuretics.

In antihypertensive therapy, the following diuretics are often used: thiazide diuretics, diuretics of the loop of Henle and potassium-sparing.

Hypothiazide (Hypothiazid).

Synonyms: dichlothiazide, Esidrex.

Active diuretic and antihypertensive agent.

Application: the same as for veroshpiron, but also for glaucoma and toxicosis of pregnant women. Take 0,025-0,05 g per day orally before meals, in severe cases - up to 0,2 g per day.

Take 3-7 days followed by a break of 3-4 days. With hypertension, 0,025-0,05 in combination with other antihypertensive drugs.

Side effects: weakness, dyspepsia, dermatitis, hypokalemia and hypochloremic alkalosis.

Contraindications: with insufficiency of kidney function.

Product form: tablets of 0,025 and 0,1 g No. 20.

Diuretics of the loop of Henle.

These include furosemide, ethacrynic acid (uregit), brinaldix.

Furosemide (Furosemidum).

Fast-acting diuretic (saluretic), which has a hypotensive effect.

Application: severe forms of arterial hypertension, hypertensive crises. Prescribed orally, intramuscularly or intravenously. For hypertension, 20-40 mg 1 time per day, when combined with heart failure - up to 80 mg, IM or IV (slow stream) - 20-60 mg 1-2 times per day, if necessary - up to 120 mg.

Side effects: nausea, diarrhea, skin flushing, itching, hypotension, reversible hearing loss, interstitial nephritis, dizziness, depression, muscle weakness, thirst. Perhaps the development of hypokalemia, hyperuricemia, uricozoria, hyperglycemia.

Contraindications: first half of pregnancy, hepatic coma, end-stage renal failure, mechanical obstruction of the urinary tract.

Product form: tablets 40 mg No. 50, 1% solution in 2 ml ampoules No. 5, 10, 25 per package.

Combined drugs.

These drugs reduce the number of tablets used.

Adelfan (Adelphane).

Composition: reserpine - 0,1 mg, hydrazine - 10 mg.

Adelfan Ezid Rex: reserpine - 0,1 mg, hydralazine - 10 mg, hydrochlorothiazide - 10 mg.

Adelfan esidrex K: reserpine - 0,1 mg, hydralazine - 10 mg, hydrochlorothiazide - 10 mg, potassium chloride - 600 mg.

Triresid K: reserpine - 0,1 mg, hydralazine - 10 mg, hydrochlorothiazide - 10 mg, potassium chloride - 350 mg.

Sinipress (Sinipress).

Composition: reserpine - 0,1 mg, hydrochlorothiazide - 10 mg, dihydroergocristine - 0,6 mg.

Brinerdin (Brinerdine).

Composition: brinaldix - 5 mg, reserpine - 0,1 mg, dihydroergocristine - 0,5 mg.

Christepin (Crystepin).

Composition: clopamide - 5 mg, reserpine - 0,1 mg, dihydroergocristine - 0,5 mg. Apply these drugs 1-4 tablets (pellets) per day.

LECTURE № 23. Angioprotectors. Hypolipodemic agents

1. Angioprotectors

Medicines that improve microcirculation, normalize vascular permeability, reduce swelling of vascular tissues and improve metabolic processes in their walls. They are widely used in the treatment of various angiopathy, vascular permeability disorders in rheumatoid diseases, trophic ulcers, atherosclerotic vascular lesions, vein diseases with congestive and inflammatory processes. The mechanism of action of angioprotectors is different. A certain role is played by the activity of hyaluronidase, inhibition of prostaglandin biosynthesis, anti-bradykinin action and other factors.

Parmidin (Parmidinum).

Synonyms: Anginin, Prodectin.

Application: atherosclerosis of the vessels of the brain, heart, limbs, diabetic retinopathy, retinal vein thrombosis, obliterating endarteritis, trophic ulcers of the leg. Orally, 0,25 g is prescribed 3-4 times a day, if necessary, up to 3 g per day. The course of treatment is 2-6 months.

Side effects: dyspepsia, headache.

Product form: tablets of 0,25 g No. 100.

doxium (Docium).

Synonym: Dobesifar. Reduces capillary fragility and increased permeability. Prescribed orally for diabetic microangiopathy and retinopathy, 2-3 tablets per day for 4-6 months, then 1-2 tablets per day. If venous vessels are affected, take 1 tablet 3 times a day for 1-3 weeks, then 1 tablet 2 times a day, taken during or after meals. In addition, it is prescribed for liver cirrhosis, hemorrhoids, venous insufficiency and increased capillary permeability.

Side effects: gastrointestinal disorders, allergic rash.

Product form: tablets 0,25 No. 100.

Etamzilat (Aethamzilatum).

Normalizes the permeability of the vascular wall, improves microcirculation, has a hemostatic effect.

Application: prevention and control of bleeding during surgical interventions, injuries. In emergency cases with intestinal and pulmonary bleeding, especially with normal indicators of the blood coagulation system. In / in, in / m is administered for prophylactic purposes 1 hour before surgery, 2-4 ml (1-2 ampoules) or inside 2-3 tablets 3 hours before surgery.

For therapeutic purposes in emergency cases - 2-4 ml IV or IM, and then every 4-6 hours - 0,25 g parenterally or 0,5 g orally. For diabetic microangiopathies - in courses of 2-3 months, 1 tablet 3 times a day or administered intramuscularly at 2 ml (1 ampoule) 2 times a day for 10-14 days.

1 ml of the solution is injected subconjunctivally and retrobulbarno. Do not use in hemorrhages caused by anticoagulants. Produced in ampoules of 2 ml of a 12,5% ​​solution No. 10 and tablets of 0,25 g No. 50.

Aescusan (Aescusan).

Increases the tone of blood vessels and reduces blood clotting.

Indications: prevention of thrombosis, venous congestion, vein dilatation. Take orally before meals 12-15 capsules 3 times a day.

Product form: a bottle of 20 ml, pills No. 100. The drug "Esflazid" (Aesflazidum) in tablets is similar.

Troxevasin (Troxevazin).

Synonym: Venoruton. Reduces permeability and fragility of capillaries.

Application: varicose veins, superficial thrombophlebitis, venous ulcers, dermatitis, hemorrhoids. Initially, the drug is prescribed in / m or / in (slowly) 1 ampoule every other day (5 injections), then orally 2-3 capsules a day with meals for 2-3 weeks.

Product form: capsules 0,3 No. 50, forte tablets 500 mg No. 30, 5 ml ampoules of 10% solution No. 5, 2% hydrophilic gel 40 g each.

2. Lipid-lowering drugs

Preparations of this group are used in the complex therapy of diseases accompanied or caused by lipid metabolism disorders. These include drugs from the following groups:

1) anion exchange resins, or bile acid sequestrants;

2) nicotinic acid and some of its derivatives;

3) fibrates (derivatives of fibproic acid);

4) probucol, enzyme inhibitors (HMG-CoA reductase).

Cholestyramine (Cholestyraminum).

When taken orally, it is not absorbed and is excreted unchanged in the feces.

Application: itching caused by bile stasis (cholelithiasis, carcinoma, etc.), hypercholesterolemia, digitalis poisoning. Inside appoint 1 tsp. 2 times a day. The daily dose can be up to 16 g (in 4 divided doses). Other drugs can be taken at least an hour later.

Side effects: nausea, vomiting, diarrhea or constipation. It is necessary to control the prothrombin index.

Product form: powder in vials of 500 g.

A nicotinic acid (Acidum nicotinicum).

Application: vascular spasm, atherosclerosis. Orally, 0,05 g is prescribed 2-3 times a day, or up to 0,1 g 2-3 times. Parenteral: 1% sodium nicotinate solution, 1 ml 1-2 times a day (10-15 days).

Side effects: redness of the face and upper half of the body with a tingling and burning sensation, dizziness, rushes of blood to the head, with prolonged use of large doses - fatty infiltration of the liver.

Product form: powder, tablets of 0,05 No. 50, ampoules of 1 ml of 1% solution No. 10.

Miscleron (Miscleron).

Synonym: Clofibrat.

Application: atherosclerosis and other diseases accompanied by hypercholesterolemia. Inside, take 2-3 capsules 3 times a day before meals.

Side effects: dyspepsia, rash, itching.

Contraindications: liver and kidney dysfunction, pregnancy.

Product form: capsules of 0,25 No. 50.

Probucol (Probucol).

Reduces the level of total cholesterol due to low density lipoproteins.

Indications: lipid metabolism disorders associated with increased levels of cholesterol and low-density lipoproteins. Orally prescribed 500 mg 2 times a day with meals. The course of treatment is 3 months.

Side effects: flatulence, diarrhea, abdominal pain, nausea.

Contraindications: myocardial infarction, cardiac arrhythmias, pregnancy, lactation.

Product form: tablets 0,25 No. 50.

Lovastatin (Lovastatin).

It lowers the content of cholesterol, triglycerides, low density lipoproteins, moderately increases the content of high density lipids, which have an antiatherogenic effect.

Application: hyperlipoproteinemia, not corrected by a special diet and physical activity. Take 10-20 mg orally once a day - in the evening after meals. The maximum dose is 1 mg.

Side effects: dyspepsia, liver disease, pregnancy, lactation.

Product form: tablets of 0,02 and 0,04 g No. 30. In addition, in the treatment of atherosclerosis, menetol, lipostabil, polysponin, peribusponin, etc. are used as additional drugs.

References

1. Belousov Yu. B., Moiseev V. S., Lepakhin V. K. Clinical pharmacology and pharmacotherapy. M.: Universum, 1993.

2. Kukes VG Clinical pharmacology. M.: Medicine, 1991.

3. Lazareva D. N. Effect of drugs in pathological conditions. M.: Medicine, 1990.

4. Lawrence D. R., Benitt P. N. Clinical pharmacology. M.: Medicine, 1991.

5. Lyakin K. N., Krylov Yu. F. Biotransformation of medicinal substances. M.: Medicine, 1981.

6. Mashkovsky M. D. Medicines. In 2 vols. T. 1, 2. Kharkov: Torsing, 1998.

7. Industry standard "Rules for the release (sale) of medicines in pharmacy organizations". Basic provisions. Ost 91500.05.0007-2003 St. Petersburg, 2003.

8. Pershin G. N., Gvozdeva E. I. Textbook of pharmacology. M.: Medicine, 1967.

Author: Malevannaya V.N.

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