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Pharmacology. Cheat sheet: briefly, the most important

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1. The subject of pharmacology, its history and tasks. Clinical pharmacology and types of pharmacotherapy

Pharmacology is 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 II 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.

At the end of the XNUMXth - beginning of the XNUMXth centuries. the first guides to pharmacology appeared, written in Russia by N. M. Maksimovich-Ambodik and A. P. Nelyubin. 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 preparations - ether and chloroform - on the organism of animals. Of great importance for the development of pharmacology were IP Pavlov's research in the physiology of the cardiovascular system and his theory of conditioned reflexes. 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.

IP 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.

Clinical pharmacology - studies the effect of drugs on the body of a sick person.

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

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

Pharmacotherapy is 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 is aimed at eliminating the cause (etiology) of the disease.

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

Symptomatic therapy eliminates or reduces individual symptoms of the disease.

Substitution therapy is used in case of insufficiency in the patient's body of biologically active substances - hormones, enzymes, etc.

Preventive therapy is carried out to prevent diseases.

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

A medicine is a substance used to treat or prevent a disease.

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

A drug is a drug in a ready-to-use form.

A dosage form 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.

A prescription 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.

The dose is expressed in mass or volume units of the decimal system and is indicated by Arabic numerals. The number of whole grams is separated by a comma (1,0). More commonly used: 0,1 - one decigram; 0,01 - one centigram; 1,001 is one milligram. The drops that make up the medicine are indicated by a Roman numeral, before which gtts is written. Biological units of action in the recipe thus indicate 500 units. Liquid substances in recipes are indicated in ml (000 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, sombre-vin, 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, indicate the required dosage form. For example, Misce ut fiat pulvis (M. f. pulvis) - "mix to make a powder."

For dosed ones, they write: "Da tales doses nu-mero 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 way the medicine is used.

3. Validity of prescriptions and dosage of medicinal substances. Solid dosage forms

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.

Solid dosage forms include tablets, dragees, powders, capsules, granules, etc.

Tablets (Tabulette, Tab.) are obtained by pressing a mixture of drug and excipient. Distinguish between simple and complex composition.

1. Rp.: Tab. Analgini 0,5 № 10 DS 1 tablet 2-3 times a day.

2. Rp.: Amidopyrini Butadioni aa 0,125 No. 20 in tab.

S. 1 tablet 3 times a day (after meals). Dragee (Dragee) is made by layering medicinal 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 D.

S. 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 powder, 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) - 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 and plates (Membranulae et Lamellae) - special solid dosage forms that contain medicinal substances on a polymer basis; glossets (Glos-setes) - small tablets intended for sub-lingual or buccal use; caramels (Caramela) are prepared in the form of sweets containing sugar and molasses.

Poultices (Cataplasmata) are used to treat diseases of the oral cavity - semi-solid preparations that have anti-inflammatory and antiseptic effects.

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

4. Liquid and soft dosage forms

Solutions (Solutiones, Sol.) are obtained by dissolving drugs in a solvent.

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

Galenic preparations 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 decoctions (Decocta, Dec.) are aqueous extracts from the dry parts of medicinal plants.

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

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

Novogalenic preparations are obtained as a result of special development with a high degree of purification of medicinal preparations (Adonisidum).

Dispersed systems are systems where the dispersion medium is a liquid (water, oil, gas, etc.), and the dispersed phase is insoluble fine particles. These are suspensions, aerosols, medicines.

Liquid dosage forms also include applications, balms, collodions, creams, soft drinks, syrups.

Applications - liquid or ointment-like preparations used for application to the skin for therapeutic purposes.

Balsams (Balsama) are liquids obtained from plants and have an aromatic smell, antiseptic and deodorizing properties.

Collodia (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.

Lemonades (Limonata) - liquids of sweet taste or acidified for ingestion.

Syrups (Sirupi) are thick, clear, sweet liquids for oral administration.

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

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

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

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

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. Plasters (Emplastra) - a dosage form in the form of a plastic mass that softens at body temperature and sticks to the skin.

5. Routes of drug administration

There are enteral and parenteral routes of drug administration. Enteral route - the introduction of the drug inside through the mouth (peros), 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.

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.

The parenteral route is the various 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 oil solutions and suspensions of medicinal substances are introduced. The therapeutic effect occurs within 10-30 minutes. The volume of the injected substance should not exceed 10 ml.

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

Inhalation. Gases (volatile anesthetics), powders (sodium cromoglycate), aerosols are administered in this way.

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.

6. The mechanism of action of drugs, doses 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.

The 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 are called 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.

The effect on the activity of enzymes is due to the fact that some medicinal substances are able to increase and inhibit the activity of specific enzymes.

The physicochemical effect on cell membranes (nerve and muscle) is associated with the flow of ions that determine the transmembrane electrical potential. Some drugs can alter ion transport (antiarrhythmics, anticonvulsants, general anesthetics).

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.

There are threshold, therapeutic and toxic doses. For each substance there is a minimum effective, or threshold, dose, below which the effect is not manifested. Doses above the threshold may be used for therapeutic purposes if they do not cause poisoning. Such doses are called therapeutic. Doses that cause poisoning are called toxic; leading to death - lethal (from lat. letum - "death"). The breadth of therapeutic action is 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 are doses used in medical practice and give a good therapeutic effect.

7. Significance of the state of the body and external conditions for the action of drugs. Absorption and distribution of drugs

Idiosyncrasy is an extremely high sensitivity to drugs. 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.

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.

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. Filtering. 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, in which particles of the medicinal substance are enclosed, 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 medicinal substances are taken orally, the rate of their absorption in different parts of the gastrointestinal tract is not the same. After passing 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 pH 1-3, which contributes to easier absorption of acids, and an increase in the small and large intestines pH to 8 - bases.

8. 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 catalyzed by enzymes of other localization (non-microsomal).

Non-synthetic reactions are oxidation, transformation and hydrolysis. Synthetic reactions are based on the conjugation of drugs with endogenous substrates (such as glycine, sulfates, water, etc.). All medicinal substances taken orally pass through the liver, where they are further converted. Biotransformation is affected by the nature of nutrition, liver disease, gender, 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. There are microsomal and non-microsomal biotransformation. Fat-soluble substances are most easily exposed to microsomal transformation. Non-microsomal biotransformation occurs mainly in the liver. There are several ways of excretion (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, while their reabsorption in the tubules of the kidneys matters. In renal failure, glomerular filtration is reduced, which leads to an increase in the concentration in the blood of various drugs, so the dose of the drug should be reduced. Medicinal substances leave the liver in the form of metabolites or, without changing, enter the bile and are excreted with feces. Under the influence of enzymes and bacterial microflora of the gastrointestinal tract, drugs can be converted into other compounds that are 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.

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.

9. Classification of anesthesia. Non-inhalation anesthesia

Depending on the depth, there are four levels of surgical anesthesia.

The first level is 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.

The second level is severe 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 blood pressure are close to normal. This anesthesia can be used for most surgical procedures.

The third level is 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.

The fourth level is an 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 bluish, 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. Inhalants include volatile liquids and gaseous substances.

Non-inhalation anesthesia occurs with the introduction of narcotic substances 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.

10. Means for inhalation and non-inhalation anesthesia

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

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

Fluorotan Phtorothanum (Halothanum, Narcotan).

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

Method 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.

Release form: in vials of 50 ml.

Nitrous oxide (Nitrogenium oxydulatum).

Does not cause deep anesthesia.

Application: anesthesia of childbirth. Minor surgical interventions. Method of application: inhalation of nitrous nitrogen is carried out using a mask or intubation in a mixture with oxygen (70-50% nitrous nitrogen and 30-50% oxygen, respectively).

Side effects: a 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.

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

Thiopental-sodium (Thiopentalum-natrium).

It has a sleeping pill, and in large doses a narcotic effect.

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

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

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

Release form: in bottles of 1 g, in a package No. 10.

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

Method 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.

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

Brietal.

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

11. 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).

Derivatives of barbituric acid facilitate falling asleep, dramatically change the structure of sleep: reduce the duration and phasing of REM sleep. After awakening, drowsiness, weakness, and impaired coordination of movements are observed.

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

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

Method 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.

Release 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.

Method of application: inside 0,1-0,2 g, for children 0,01-0,1 g, per rectum 0,2-0,3, in / in 5-10 ml of solution. V. R. D - 0,3 g, V. S. D. - 0,6 g.

Contraindications: Same as phenobarbital.

Release form: powder. List B.

Benzodiazepines.

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

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

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

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

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

Release form: tablets of 0,005 g No. 20 and 0,01 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.

Method of application: administered 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.

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

12. 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. 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 phenothiazines. Aminazin (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, dyspeptic phenomena, hepatitis.

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

Release 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 a sense of fear, anxiety, insomnia. Taken orally at 0,025-0,4 g per day; i / m 2-4 ml of a 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.

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

13. Antipsychotic drugs

Etaperazin (Aethaperazinum, Perphenazini hydroc-loridum).

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.

Method of application: taken orally in the form of tablets after meals. For taking doses - 0,004-0,01 1-2 times a day. When excited, the daily dose can 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.

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

Moditen, fluorophenazine (Moditen, Phthorphena-zinum).

It is similar in structure to etapirazine and has a strong antipsychotic effect, combined with some activating effect.

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

Method 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; i / m is administered starting from 1,25 mg (0,5 ml of a 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.

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

Moditen-depot, ftorphenazine-decanoate (Phthor-phenazinum decanoate). A strong neuroleptic 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, it is convenient for patients who find it difficult to prescribe neuroleptics in the usual form.

Dosage and administration: 12,5-25 mg intramuscularly, and sometimes 50 mg (0,5-2 ml of a 2,5% solution) are prescribed intramuscularly 1 time in 1-3 weeks.

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

Stelazine. Active antipsychotic agent.

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

Method 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.

14. Haloperedol, droperedol, chlorprothixene, propulsin

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

Release 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.

Method of application: taken orally at 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.

Release 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 (Droperidolum).

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

Application: administered intravenously for 30-60 minutes for sedation and neuroleptanalgesia (before surgery) 2,05-10 mg (1-4 ml of a 0,25% solution) together with 0,05-0,1 mg (12 ml 0,005 % 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: possible lowering of blood pressure and respiratory depression.

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

Release 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.

Chlorprothixen (Chlorprothixen).

It has antipsychotic, antidepressant and sedative effects.

Application: depression with anxiety symptoms, alcoholic delirium, sleep disturbance, somatic diseases with neurosis-like disorders, pruritus. It is taken orally at 0,025-0,05 g 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 poisoning and barbiturates, epilepsy, parkinsonism, old age, heart disease.

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

Prosulpin.

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

Application: psychosis, depression, neurotic conditions, migraine.

Method 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.

15. Leponex, tranquilizers, sibazon, xanax

It has a pronounced antipsychotic and sedative effect.

Application: schizophrenia.

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

Release 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.

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 peptic ulcer patients.

Method of application: administered orally 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.

Xanax (Xanax).

The active substance is alprazolam. Reduces anxiety, feelings of anxiety, fear, tension.

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

16. 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 (Natrii 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, irritability, insomnia, initial forms of hypertension, as well as epilepsy and chorea. Assign inside 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.

Release form: powder, from which solutions and mixtures are prepared.

Bromcamphora (Bromcamphora).

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

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

Preparations containing barbiturates 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: Dragee in a pack of 50 pieces.

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

Contraindications: pregnancy, glaucoma.

The group of sedatives also 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.

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.

17. Antidepressants

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

These are medicinal substances that eliminate the symptoms of depression in neuropsychiatric and somatic patients. In most cases, drug interaction occurs at the level of synaptic neurotransmission. Antidepressants are divided into the following groups: monoamine oxidase inhibitors, tricyclic antidepressants, tetracyclic, selective serotonin reuptake inhibitors, combined and transient antidepressants and normothymic agents.

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 conditions of various etiologies, neutrogenic enuresis in children. Assign inside 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 with severe depression, 2 ml of a 1,25% solution are injected intramuscularly, 1-3 times a day. V. R. D. inside - 0,1, V. S. D. - 0,3 g, intramuscular single - 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 first trimester of pregnancy.

Release 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: same as imizin.

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

Release form: dragee 25 mg No. 50; injection solution of 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; appoint inside 25 mg 3 times a day with a gradual increase in dose to 100-200 mg per day. With intravenous drip, the daily dose is 25-150 mg.

Side effects: same as imizin and amitriptyline.

Contraindications: same as imizin and ami-tritriptyline.

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

18. Herbal sedatives

Rhizome with roots of valerian (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.

Release 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 from motherwort herb (Herba Leonuri), passionflower herb (Herba Passiflorae) and peony tincture (Tinctura Paeoniae).

Phytopreparations of combined action are also used.

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 tension. 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.

Release form: solution of 100 ml in a vial.

This group also includes the drug fitosed 100 ml.

Application: same as Novopassit.

Corvalol (Corvalolum) is similar to the imported drug Valocardinum (Valocardinum), belongs to the group of combined drugs. Valocordin also includes hop oil, which enhances the effect.

Application: neuroses, states of excitation, functional disorders of the cardiovascular system. Assign inside 15-20 drops, with tachycardia and spasms - up to 40 drops.

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

Release form: Corvalol 15 ml; valocordin 20 and 50 ml.

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

Application: same as Corvalol.

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

Aurorix (Aurorix).

Antidepressant, reversible type A inhibitor.

Application: depressive syndromes. Take orally 150 mg 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.

Release form: 150 and 300 mg coated tablets, No. 30.

19. CNS stimulants, caffeine, piracetam

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 hydroxybutyrate, 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 (Coffeinum).

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, spasms of cerebral vessels, 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, there is a decrease in action, and with a sudden cessation of administration - increased inhibition with symptoms of fatigue, drowsiness, depression; lowering blood pressure.

Contraindications: irritability, insomnia, severe hypertension, atherosclerosis, organic diseases of the cardiovascular system, old age, glaucoma. Release form: tablets No. 10. Caffeine-sodium benzoate (Coffeinum-natrii ben-zoas).

Similar to caffeine, but more soluble in water. Release form: tablets 0,1 and 0,2 No. 5; in the form of a 10 and 20% solution in 1-2 ml ampoules. Piracetam (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.

Side effects: increased irritability, excitability, sleep disturbances, dyspepsia.

Contraindications: severe renal dysfunction, pregnancy, lactation.

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

20. Aminalon, Cerebrolysin, Pyriditol, Cordiamin

Aminolone.

Synthetic analogue - GABA (g-aminobutyric acid).

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

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

Release form: tablets of 0,25 No. 100.

Cerebrolysin (Cerebrolysin).

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

Application: CNS diseases, brain injuries, memory impairment, dementia. Enter the / m 1-2 ml every other day. The course of treatment is 30-40 injections, with intravenous administration - 10-60 ml.

Contraindications: acute renal failure, status epilepticus.

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

Pyriditol (Pyriditolum).

Synonym: Encefabol; picamilon, (Picamylon), va-zobral, (Vazobralum), instenon, (Instenon), phenibut (Phenibutum), (bilobil, (Bilobyl), tanakan, (Tanacan). Tanakan and bilobil are preparations from the gingo bi-loba plant.

Action and use: these drugs are the same as those of Cerebrolysin.

Sodium oxybutyrate (Natrii oxybutyras).

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

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

Method of application: in/in administered at the rate of 70-120 mg per 1 kg of body weight; 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 a quick on / in the introduction, motor excitation, convulsive twitching of the limbs and tongue, sometimes vomiting are possible, with an overdose - respiratory arrest.

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

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

Cordiaminum (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.

Method of application: appoint inside before meals, 30-40 drops. Parenterally: s / c, / m; in / in (slowly) administered to adults at a dose of 1-2 ml 2-3 times a day; children - depending on age. To reduce pain, novocaine is first introduced into the injection site, V. R. D. - 2 ml (60 drops), V. S. D - 6 ml (180 drops); s / c single - 2 ml, daily - 6 ml.

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

21. Camphor, Sulfocamphocaine, Ginseng Root, Rhodiola Extract, Pantocrine

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: formation of an infiltrate is possible.

Contraindications: epilepsy, tendency to convulsive reactions.

Release form: preparations for injection, use a 20% oily solution of camphor; for external use - camphor oil (10% camphor solution 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 vials 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.

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

This group also includes drugs tsitsiton (Cytitonum) and lobeline hydrochloride (Lobelinihydrochloridum). Used as respiratory analeptics.

Assign 1 tablet 5 times a day with a further dose reduction of 1-2 tablets a 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, irritability.

Release 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 Eleuthero-cocci fluidum), etc.

Application: as a tonic and tonic, CNS stimulant.

Rhodiola rosea extract is also used for symptoms of asthenia, akineto-hypotension 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 (Pantocrinum).

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.

22. 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 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 most common drug is phenobarbital.

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 (Dipheninum).

It has a pronounced anticonvulsant effect.

Application: epilepsy, mainly 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 disorders.

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

Release form: tablets of 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, in the future - 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. Release form: tablets of 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 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.

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

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

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

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

Release form: tablets of 300 mg No. 100.

23. 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 affecting 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: impaired liver and kidney function, childhood, lactation, heart disease, blood diseases, narrow-angle glaucoma, MAO inhibitors. Caution should be used in patients with bronchial asthma, emphysema, active stomach ulcers, psychosis and neuroses. Release form: capsules and tablets of 0,25 and 0,5 g No. 100.

This group also includes the combined drug Nakom (Nacom), consisting of 0,25 g of levodopa and 25 mg of carbidopa, in which the therapeutic effect is enhanced and 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.

Release 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 aid in the treatment of parkinsonism. It is taken orally at 0,05 g 3 times a day with a gradual increase in dose to 0,45 g per day, injected 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).

24. Analgesics, narcotic analgesics

Analgesics 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, administered 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.

Release 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 0,025-0,5 g per dose.

Release form: powders, tablets at ^^^ 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 for morphine.

Method of application: injected s / c 1 ml of a 1-2% solution, taken orally - 0,01-0,02 g.

Release 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. The daily dose is 400 mg. Side effects: dizziness, nausea, vomiting, weakening of attention, slow reaction. Contraindications: drug addiction, lactation.

Release form: 50 mg capsules 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.

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 narorphine, motor agitation, spasm, hypotension, sinus tachycardia.

25. Antagonists of narcotic analgesics, non-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: at high doses, nausea, drowsiness, headache, mental agitation are possible. Drug addicts go into withdrawal.

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

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 (Amido-pyrinum), antipyrine (Antipyrinum), ketazon (Cetazon) and tandedril (Tandedril). Mechanism of action: reduced energy supply to inflammation, inhibition of the activity of proteolytic enzymes, reduced capillary permeability and inhibition of inflammatory infiltration. Analgin (Analginum).

Application: pains of various origins, rheumatism, chorea. Take 0,25-0,5 g 2-3 times a day inside, with rheumatism - 0,5-1,0 g 3 times a day. In / m enter 1-2 ml of a 50% solution 2-3 times a day.

Side effects: allergic reactions and anaphylactic shock are possible.

Release 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), tem-palgin (Tempalginum), anapirin (Anapyrinum), pentalgin (Pentalginum).

Butadion (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. Release 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, and in a mixture with other drugs, these are preparations of sedalgin, citramon.

Paracetamol (Paracetamolum). Synonyms: Acetaminophen, Panadolum, Efferalganum. Antipyretic and analgesic. Application: as with other drugs, 0,2-0,4 per dose. Side effects: nephro-toxic. Contraindications: kidney disease. Release form: tablets 0,2 No. 10.

26. 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).

Pharmacological action and indications are the same as those of other analgesics, but it 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.

Release 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 indolacetic acid are represented by drugs: indomethacin (methindol); to-lectin; clinoril.

Indomethacin (Indometacin). Synonym: Metin-dolum. It blocks the synthesis of prostaglandins and the migration of leukocytes to the area of ​​inflammation.

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.

Release 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 natrium). 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. It is taken orally 25 mg 2-3 times a day after meals, then the dose is increased to 100-150 mg per day. In / m - no more than 2 ampoules during the day.

Side effects and contraindications: as indomethacin. Release form: 25 mg tablets 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.

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

27. 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.

Method 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.

Release form: capsules 250 mg No. 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: inherent in this group of drugs.

Release 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.

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

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

Release form: capsules of 10 and 20 mg No. 20. Toradol (Toradol).

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

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

Method of application: take orally 10 mg once, if necessary - every 6 hours; i / m and / in administered at 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.

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

28. 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 starting zone. It is especially sensitive to the action of chemicals.

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

Method 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.

Release form: ampoules of 1% solution of 1 ml 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 disease with dysfunction, hypotension.

Release form: tablets of 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: intestinal spasms, increased plasma prolactin levels.

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

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

29. Drugs acting primarily on peripheral neurotransmitter systems. M-cholinomimetics

In the peripheral nervous system, afferent nerves are distinguished - sensitive, carrying information to the central nervous system, and efferent nerves - centrifugal, through which the activity of internal organs is coordinated from the central nervous system. Drugs acting on the peripheral nervous system are divided into two groups: drugs that affect the efferent innervation, and drugs that affect the afferent innervation. Cholinergic synapses show different sensitivity to medicinal substances: synapses and receptors located in them and sensitive to muscarine are called muscarinic-sensitive, or m-cholinergic receptors; to nicotine - nicotine-sensitive, or n-cholinergic receptors. 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 anti-cholinesterase agents;

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

6) n-cholinolytics:

a) ganglion blocking agents (hygronium, benzo-hexonium, 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.

Method 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.

Release form: ampoules of 1 ml 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.

Method 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.

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

30. Anticholinesterase agents

There are anticholinesterase agents of reversible action (physostigmine, prozerin, oksazil, galantamine, kalimin, ubretide) and irreversible action (phosphacol, armin), the latter being more toxic.

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.

Method of application: take orally 0,015 g 2-3 times a day; injected s / c 1 ml of a 0,05% solution (1-2 ml of solution per day), in ophthalmology - 1-2 drops of a 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.

Release 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.

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

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

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

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

Ubretid.

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.

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

Armin (Armin).

Active anticholinesterase drug of irreversible action.

Application: miotic and antiglaucoma agent.

Method of application: 0,01% solution is prescribed, 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.

31. 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 the 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 bile ducts, 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-cholinergic blockers 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, vasospasm of internal organs, bronchial asthma, in ophthalmology - to dilate the pupil.

Method of application: administered orally at 0,00025-0,001 g 2-3 times a day, s / c 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.

Release 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.

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

Method of application: administered orally at 0,002-0,004 g 2-3 times a day, parenterally at 0,5-2 ml of a 0,1% solution.

Release 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.

32. 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.

Ganglion blocking 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 the impulse of the pump-motor center from the carotid glomerulus, dilate the vessels of the lower extremities and improve their blood circulation. Short-acting ganglion blockers are used for pulmonary and cerebral edema, as well as for controlled hypotension during operations 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.

Release form: 0,1 g powder in 10 ml ampoule No. 10. List B.

Long acting ganglionic blockers.

Benzoheksonium (Benzohezonium). Application: spasm of peripheral vessels, hypertension, hypertensive crises, bronchial asthma, peptic ulcer of the stomach and duodenum. Assign inside 0,1-0,2 g 2-3 times a day, s / c, / m - 1-1,5 ml of a 2,5% solution. V. R. D. - inside 0,3 g; V. S. D. - 0,9 g; s / c single - 0,075 g, daily - 0,3 g.

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

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

Release 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.

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

Pachycarpine hydroiodide (Pachycarpini hydroio-didum).

Application: for 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.

Release 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.

33. 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) - tubocu-rarin-chloride, diplacin;

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

Tubocurarine chloride (Tubocurarini-chloridum).

It is a curare-like drug with antidepolarizing action.

Application: in anesthesiology for muscle relaxation. Enter in / in 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.

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

Dithilin (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.

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

In anesthesiology practice, other drugs are also used: arduan (Arduan), pavulon (Pavulon), nor-curon (Norcuron), trakrium (Tracrium), mellictin (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.

Spasmolytin (Spasmolythinum).

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

Application: endarteritis, pylorospasm, spastic colic, peptic ulcer of the stomach and duodenum. Assign inside, after meals, 0,05-0,1 2-4 times a day, in / m - 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. Release form: powder.

34. Adrenergics

Adrenergic drugs 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 a-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 adrenoreceptors - 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 a-adrenergic receptors (a-adrenergic agonists);

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

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

a-adrenomimetics. This group includes noradrenaline, the main mediator of adrenergic synapses, secreted by the adrenal medulla and having a predominantly stimulating effect on a-adrenergic receptors, to a small extent - on b1- and less - on b2-adrenergic receptors.

Norepinephrine hydrotartate (Noradrenaiini hydrotartas). Stimulates a-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: halothane anesthesia. Caution is required in severe atherosclerosis, circulatory failure, complete atrioventricular blockade. Release form: 1 ml of 0,2% solution No. 10. List B.

Mezaton (Mesatonum). It acts mainly on a-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 norad-renaline.

Side effects and contraindications: the same. Release 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 for mezaton.

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

Naphthyzinum (Naphthyzinum). 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.

Release form: bottles of 10 ml of 0,05-0,1% solution.

35. β-agonists, α-and 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. Assign inside 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 heart.

Release 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.

Release 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.

Release form: 20 ml bottles 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.

Release form: 20 ml bottles (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.

Release form: aerosol with a dosing 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.

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

α- and β-agonists.

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 a- and b-adrenergic receptors.

Adrenaline hydrochloride (Adrenalini hydrochlo-ridum). It is used for bronchial asthma, hypoglycemia, allergic reactions 1,0 ml of a 0,1% solution, for acute cardiac arrest - intracardiac, 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.

36. Adrenoblockers, α-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, a-blockers are divided into α1 blockers, which include phentolamine, tropafen, pyrroxane and others, α2-adrenergic receptor 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, al-prenolol, 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. a-blockers and drugs block the transmission of excitation to α1- and α2-adrenergic receptors. The drugs of this group are used for diseases occurring against the background of hyperadrenalemia.

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

Dihydroergotamine (Dihydroergotamine).

It is an antiadrenergic agent, lowers vascular tone.

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

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

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

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

Release form: bottles of 10 ml of 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.

Method of application: administered 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.

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

37. 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 (Anaprillinum). 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.

Release 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.

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

Pindolol (Pindololum).

Side effects and contraindications: as in anaprilin.

Release form: 5 mg tablets No. 30; 5 ml ampoules of 0,02% solution No. 5. Nadolol (Nadololum).

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

Application: ischemic heart disease, early stages of hypertension.

Side effects: gastrointestinal dysfunction, 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 (possible tachyphylaxis), appoint 1 drop 2 times a day.

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

β1-blockers (selective action).

Cordanum (Cordanum), synonym (Talinolol).

Reduces myocardial contractility and cardiac output.

Application: cardiac ischemia, arterial hypertension, cardiac arrhythmias - 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.

Release form: dragee 50 mg No. 50.

38. 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, or-nid, 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.

Method of application: administered orally at 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.

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

Raunatin (Raunatinum), synonym: rauvazan (Rau-wasan).

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

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

Contraindications: hypotension.

Release form: tablets of 0,002 g, pills of rauvazana 0,002 each. It is prescribed 1 tablet (dragee) 3 times a day, no more than 6 tablets (dragee) per day. List B.

Oktadin (Octadinum), synonyms: Isobarin, Gaune-thidine 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. Octadine slightly increases the motility of the gastrointestinal tract.

Used to treat hypertension, rarely glaucoma.

Side effects: gastrointestinal dysfunction, bradycardia.

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

Ornid (Ornidum).

Application: arrhythmia, hypertensive crises.

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

Contraindications: atherosclerosis, myocardial infarction, cerebrovascular accident.

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

Methyldopa (Methyldopa), dopegyt (Dopegyt), Aldomet (Aldomet).

Application: hypertension. Begin treatment with 0,25-0,5 g, bringing the dose to 0,75-1 g, with insufficient effect - up to 1,5-2,0 g per day. Combine with saluretics and antihypertensive drugs.

39. Dopamine

Dopamine is a biogenic amine formed from l-tyrosine and is a precursor of noradrenaline and adrenaline and a mediator that interacts with a- and b-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 enzyme adenylate cyclase, 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.

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.

Method of application: administered in / in drip, previously 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 monitoring 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.

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

40. Histamine. Histaminomimetics

Histamine is one of the mediators involved in the regulation of vital body functions and plays an important role in the pathogenesis of a number of disease states. Normally, histamine is found in the body in a bound, inactive state. The amount of histamine increases in various pathological conditions of the body: trauma, stress, allergic reactions. Then, along with histamine, other biologically active substances are released: serotonin, bradykinin, acetylcholine, the substance of anaphylaxis, prostaglandins, etc. The amount of histamine also increases when various poisons (plant, animal, bacterial), food products (strawberries, egg protein, 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 localization in the body. With stimulation of H1 receptors, 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, regulation of blood pressure, capillary permeability, and coronary vessels is carried out. All histaminergic agents are divided into two main groups:

1) stimulants of H1 and H2 receptors - histamine mimetics;

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

Histaminomimetics.

These substances excite H1- and H2-histamine receptors and cause histamine-specific effects.

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.

Method of application: administered intravenously, s / c and / m, 0,2-0,5 ml of a 0,1% solution, for electrophoresis - a 0,1% solution.

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

Release form: ampoules of 1 ml of a 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 a high selective activity against H2- receptors.

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.

41. Antihistamines

Dimedrol (Dimedrolum). It has an antihistamine, anticholinergic and sedative effect.

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

Method of application: administered orally, intramuscularly, intravenously, topically (cutaneously, in the form of eye drops, on the nasal mucosa), rectally. Do not administer under the skin due to irritant action. Assign inside 0,025-0,05 g 1-3 times a day, i / m and / in - 1-5 ml of a 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.

Presentation: powder, tablets of 0,05 g No. 10, 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 .10 g No. XNUMX.

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.

Method of application: appoint inside 0,025 g 2-3 times a day, in / m - 1-2 ml of a 2,5% solution; PTB IV (as part of lytic mixtures) - up to 2 ml

2,5% solution. Children - according to age. V. R. D. - 0,075 g, V. S. D. - 0,5 g; i / m single - 0,05 g, daily - 0,25 g.

Side effects: dry mouth, nausea. With the / m introduction - painful infiltrates, with / in - a sharp decrease in blood pressure.

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

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

Tavegil. Synonym: Olemastinum. Long-acting antihistamine drug with a moderate sedative effect, enhances the effect of sleeping pills and alcohol.

Application: same as diprazine.

Method of application: appoint inside 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.

Release 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.

Phencarol (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.

Method of application: administered orally at 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, 1st trimester of pregnancy.

42. Histodil, ranitidine, ketotifen

H2 blockers selectively block H2 receptors, exerting an inhibitory effect on histamine-induced gastric secretion and partially eliminating histamine hypotension.

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.

Method 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.

Release 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: as in cimetidine.

How to use: take 1 tablet 2 times a day (morning and evening) regardless of the meal. 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.

Release form: 150 mg tablets No. 20, 50. Indirect antihistamines.

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.

How to use: 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, increase the daily dose to 4 mg (2 tablets 2 times a day). Children over 3 years old - 0,025 mg / kg of body weight 2 times a day.

Side effects: at the beginning of treatment - a sedative effect, sometimes dry mouth, slight dizziness. These phenomena disappear without stopping treatment.

Contraindications: pregnancy, oral antidiabetic and other drugs that cause thrombocytopenia.

Release form: capsules and tablets of 0,001 each, syrup containing 1 mg of the drug in 0,2 ml.

43. Suprastin, diazolin, cromolyn sodium

Application, side effects and contraindications: as in diphenhydramine.

Release form: tablets of 0,025 No. 20, ampoules of 1 ml of a 2% solution No. 5.

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.

Release form: tablets and dragees of 0,05 and 0,1 No. 20. List B.

Cromolyn sodium (Cromolyn Sodium).

Synonym: Intal. Prevents the release of histamine from mast cells, prevents bronchospasm.

Application: bronchial asthma.

Method 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, choosing 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.

Release form: capsules of 0,02 g No. 30 and turbohaler.

Serotonin and serotonic 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 B1-) - receptors, 5-HT2 (or B2-) - receptors, 5-HT3 (or B3-) - receptors. 5-HT2 receptors are found in the smooth muscles of the walls of blood vessels, in the 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 suggested 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. 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.

44. Serotonin adipate

Serotonin adipinate (Serotonini adipinas). hemostatic agent.

Application: pathological conditions accompanied by hemorrhagic syndrome (Werlhof's disease, thrombasthenia, etc.).

Method of application: injected intravenously (in 100-150 ml of 0,9% sodium chloride solution) or intramuscularly (in 5 ml of 0,5% novocaine solution) from 0,005 to 0,01 g in the absence of side effects, it is 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, there is pain 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 disease accompanied by anuria, stage II-III hypertension, acute thrombosis, Quincke's edema, bronchial asthma, increased blood clotting.

Release 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.

Release form: coated tablets, 0,05 g No. 50.

Imigran (Imigran).

The active substance is sumatriptan, a specific stimulator of 5HT1-serotonin receptors.

Application: for the rapid relief of migraine attacks.

Method 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.

Release form: tablets of 50 and 100 mg No. 6.

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.

Method of application: inside and parenterally 8 mg, possibly up to 32 mg.

Side effects: headache, constipation, chest pain, hypotension, bradycardia.

Release 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).

45. 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).

Anestezin (Anaesthesinum).

Application: administered orally for pain in the stomach, increased sensitivity 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).

Contraindications: individual hypersensitivity.

Release form: powder, tablets of 0,3 g No. 10. Novocain (Novocainum).

Application: all types of anesthesia, vagosympathetic and pararenal blockade for potentiation of the action of basic drugs, for general anesthesia, for relief of pain in gastric and duodenal ulcers, with anal fissures, hemorrhoids, etc.

Method of application: with infiltration anesthesia, the highest doses at the beginning of the operation are no more than 500 ml of a 0,25% solution or 150 ml of a 0,5% solution, then every hour up to 1000 ml of a 0,25% solution or 400 ml of a 0,5% solution for every hour. For conduction anesthesia, 1-2% solutions are used, epidural - 20-25 ml of a 2% solution, spinal - 2-3 ml of a 5% solution, with perirenal blockade - 50-80 ml of a 50% solution solution, vagosympathetic blockade - 30-100 ml of a 0,25% solution.

Side effects: dizziness, weakness, hypotension, allergies.

Contraindications: individual intolerance.

Release 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.

Lidocaine (Lidocaine).

Application: local anesthesia. Ventricular extrasystole and tachycardia, especially in the acute stage of myocardial infarction and due to intoxication with digitalis preparations.

Method 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.

Release form: 10% solution in 2 ml ampoules No. 10 and 2% solution in 2 and 10 ml ampoules.

46. ​​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 (Taninum).

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), alkaloid poisoning, heavy metal salts (0,5% aqueous solution for gastric lavage).

Release 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).

Release form: tablets No. 6.

St. John's wort (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 water).

Release form: chopped grass, 100,0 g each, 75 g briquettes, 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 medical practice, infusions and decoctions of plants such as: serpentine rhizome (Rhizoma Bistortae), rhizome and burnet root (Rhizoma cum radicibus Sanguisorbae), alder seedlings (Fructus Alni), sage leaves (Folium Salviae), the preparation from it - salvin (Salvinum), chamomile flowers (Flores Chamomillae), chamomile preparation; romazulan (Roma-sulon), blueberries (Baccae Murtilli), bird cherry fruits (Baccae Pruniracemosae), cinquefoil rhizome (Rhizoma Tormentillae), string 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 for 15-30 minutes before meals.

Side effects: with prolonged use in large doses, methemoglobinemia is possible.

Release form: powder, which is part of 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%). It is part of the balsamic liniment (Vishnevsky ointment).

47. 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 is 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.

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.

Release 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.

Release form: powder.

Smecta (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.

Application: acute and chronic diarrhea, especially in children, symptomatic pain associated with diseases of the esophagus, stomach, duodenum.

Method of application: to obtain a homogeneous suspension, the contents of the sachet are poured into 0,5 cups of water and mixed. For children, the powder can be dissolved in porridge, puree, compote, in a 50 ml baby bottle (based on: up to a year - 1 sachet per day, from 1 year to 2 years - 2 sachets per day, over 2 years old - 2-3 sachet per day). Adults - 3 sachets per day.

Release form: powder for the preparation of a suspension of 3 g of active substance No. 30.

48. 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).

Essential mustard oil (Oleum Sinapis aethereum) is obtained from its defatted seeds.

Mustard plasters (Oharta 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.

The fruit of the capsicum (Fructus Capsici).

Contains capsaicin.

Preparations from it: tincture of capsicum (Tinctura Capsici), pepper camphor liniment

(Linimentum Capsici camphoratum), pepper plaster (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.

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 grass (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 oaustici).

Application: as an ambulance to excite breathing and remove patients from fainting, sometimes used orally as an emetic (5-10 drops per 100 ml of water). For insect bites - externally in the form of lotions.

Contraindications: dermatitis, eczema.

Release form: bottles of 40 ml and ampoules of 1 ml No. 10.

49. 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 (secreto-motor);

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.

Preparations of reflex action (drugs 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 with a 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 released (after ingestion) by the mucous membrane of the respiratory tract, stimulate the bronchial glands and cause direct sputum liquefaction; to a certain extent, they also stimulate the motor function of the ciliated epithelium and bronchioles, 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: chronic bronchitis. The infusion is prepared at the rate of 0,6-1,0 g per 180-200 ml of water.

1 st. l. take 2-4 times a day; dry extract of 0,01-0,05 g, cough tablets - 1 tablet per dose. Children - according to age.

Release 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.

50. Marshmallow root, mukaltin, breast elixir, liquiriton, glycyram

Contains up to 35% plant mucus.

It is used in the form of a 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.

Release form: marshmallow root dry extract in a jar; alteyny syrup, 100,0 ml; dry cough syrup for children (Mixtura sicca contra tussim pro in-fatibus), 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).

Mukaltin (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.

Breast 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, children - 1 drop per year of life.

Likviriton (Liquiritonum).

Contains a sum of flavonoids from licorice roots and rhizomes.

Application: as an anti-inflammatory, antispasmodic and antisecretory agent.

Take orally 0,1-0,2 g 3-4 times a day, course

treatment - 20-30 days.

Release form: tablets 0,1 No. 25. 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. May be used to reduce the dosage of glucocorticoids. Assign inside 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 with organic heart disease and impaired liver and kidney function.

Release form: tablets 0,05 No. 50. List B.

This group also includes rhizome with cyanosis roots (Rhizoma cum radicibus Polemonii), elecampane rhizome and roots (Rhizoma cum radicibus Inulae hele-nii), large plantain leaves (Folium Plantaginis majoris) and a preparation from it plantaglucid (Plantagluci-dum), which take 0,5-1,0 g 2-3 times a day; coltsfoot leaves (Folium Farfarae), thyme herb (Herba Serpulli) and Pertusin preparation, which is taken from 1-2 tsp. up to 1 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).

51. Classification of laxatives, senna leaves, ramnil, bisacodyl

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 the feces. These are sodium and magnesium sulfate, citrate, magnesium hydroxide, Karlovy Vary salt, non-absorbable polysaccharide lactulose (duphalac), acting at the level of the large intestine. The onset of a laxative effect is 8-12 hours. Lactulose is not split 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 the peristalsis of the large intestine, the stool softens, and their volume also increases.

Third group. Bulk laxatives, or bulking agents, such as bran, agar, methylcellulose, seaweed.

Fourth group. Laxative oils (detergents) that help soften hard feces and facilitate their sliding - vaseline, almond, fennel oils, liquid paraffin. Classification according to the localization of the action. Medicines that act primarily in the small intestine (vegetable oils, liquid paraffin, saline laxatives). Drugs acting primarily in the large intestine (synthetic agents, bisacodyl, guttalax. Agents acting throughout the intestine (saline laxatives, castor oil and hydrophilic colloids). Senna leaves (Folium Sennae). Usage: as 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, 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, 0,2 g per night.

Release form: tablets 0,05 No. 30. Bisacodyl (Bisacodyl).

Application: chronic constipation of various etiologies.

Method of application: appoint per os and per rectum. Adults 1-3 tablets at night or 1-2 suppositories rectally. Children - depending on age.

Side effects: spasms of the gastrointestinal tract are possible.

Contraindications: acute inflammatory diseases and varicose veins of the rectum.

Release form: dragee 0,005 No. 30, candles 0,01 No. 12.

52. 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 drugs are 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, dobut-rex) 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 (Digitalispurpurea 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, 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;

2) diastole becomes longer;

3) slowing down the conduction of impulses.

53. Classification of cardiac glycosides. 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. Glycosides of medium duration of action, with the introduction of which the maximum effect appears after 5-6 hours and lasts for 2-3 days. With intravenous administration, the effect occurs after 15-30 minutes, the maximum after 2-3 hours. This group includes woolly foxglove glycosides (digoxin, celagid, etc.), which have moderate cumulation. This property is possessed by glycosides of digitalis rusty and adonis.

3. Glycosides of fast and short action - emergency drugs. Enter only intravenously, the effect occurs after 7-10 minutes. The maximum effect appears after 1-1,5 hours and lasts up to 12-24 hours. This group includes strophanthus and lily of the valley glycosides, which practically do not have cumulative properties. Treatment with cardiac glycosides begins with large doses prescribed for 3-6 days (saturation phase), until a clear therapeutic effect is obtained - reducing congestion, eliminating edema, shortness of breath, and improving the general condition. Then the dose is reduced and maintenance doses (maintenance phase) are prescribed, providing effective and safe therapy, taking into account the individual characteristics of the patient. In case of an 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.

Method 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.

Release form: tablets 0,0001 g No. 10, rectal suppositories 0,00015 g No. 10.

Cordigitum (Cordigitum).

Extract from dried leaves of digitalis purpurea containing a complex of glycosides.

Side effects: with an overdose of bradycardia - nausea, extrasystole.

Contraindications: acute endocarditis, used cautiously with fresh myocardial infarction, rhythm disturbances.

Release form: tablets of 0,8 mg No. 10, suppositories of 0,0012 No. 10.

54. Intermediate-acting glycosides

Lantoside (Lantosidum).

Application: chronic failure stage I-III, accompanied by tachycardia, tachyarrhythmia and atrial fibrillation.

Method of application: appoint inside 15-20 drops 2-3 times a day, with dyspeptic symptoms - microclysters, 20-30 drops, in 20 ml of 0,9% sodium chloride solution. V. R. D. inside - 25 drops, V. S. D. - 75 drops.

Release form: in dropper bottles of 15 ml.

Celanid (Celanidum).

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.

Method 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.

Release 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 for other drugs in this group.

Side effects: nausea, vomiting, loss of appetite, tachycardia, bigeminia.

Release 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. It 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 brady-systolic atrial fibrillation.

Method of application: the average single dose - 250 mcg 2-3 times a day, if necessary - up to 1 mg per day.

Side effects: bradycardia, AV blockade, heart rhythm disturbance, 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.

Release form: tablets of 250 mcg No. 30.

55. Glycosides of short and fast action. Non-steroidal and synthetic cardiotonic drugs

Glycosides of short and fast action.

Strofantin K (Strophantinum 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.

Release 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 that of strophanthin.

Release 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. They start with a slow intravenous administration of a loading dose of 50 μg / kg of body weight, then switch to a maintenance dose of 0,375-0,75 μg / kg per 1 minute. The maximum daily dose is 1,13 mcg/kg of body weight.

Side effects: heart rhythm disturbance, angina pectoris, hypotension, headache, allergic reactions.

Release form: solution for injections, 10 ml in ampoules No. 10 (in 1 ml, 1 g of corotrope). 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. A single dose is 50-200 mg, the frequency of administration is 2-3 times a day, 1 hour before meals.

Side effects: on the part of the gastrointestinal tract, sometimes nausea, heartburn, gastralgia, tachycardia is possible.

Contraindications: ventricular arrhythmias, pheochromocytoma, pregnancy, lactation.

Release form: tablets of 50 and 100 mg No. 30.

56. Classification of antiarrhythmic drugs

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) b-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 IS - local anesthetics (lidocaine, tri-mecaine, pyromecaine), as well as mexiletine and difenin;

3) subgroup 1C - aimalin, etatsizin, allapinin.

Group I antiarrhythmic drugs.

Quinidine sulfate (Chinidini sulfas).

Application: paroxysmal tachycardia, paroxysm of atrial fibrillation, extrasystoles, persistent atrial fibrillation. Inside take 0,1 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.

Release form: powder, tablets 0,1 No. 20.

Novocainamide (Novocainamidum).

It lowers the excitability of the heart muscles, suppresses ectopic foci of excitation, and has a locally-nesthetic property.

Application: cardiac arrhythmias.

Method of application: inside designate 0,5-1 g 3-4 times a day; in / m - 5-10 ml of a 10% solution, in / in (drip) for the 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.

Release form: tablets of 0,25 g No. 20, ampoules of 5 ml of a 10% solution No. 10.

Author: Malevannaya V.N.

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