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Opioid pain reliever without side effects

07.03.2017

Opioid drugs act as a powerful pain reliever, but have a number of side effects and can be addictive. But now this problem has been solved: German scientists have created a drug that effectively copes with pain and does not have a negative effect on the patient at all.

Opiate-based drugs have many disadvantages. They often bring the patient both minor discomfort, such as intestinal obstruction, and serious life-threatening, such as respiratory distress syndrome. But modern medicine cannot refuse opiates: they cope with pain extremely effectively. Unfortunately, until now, scientists have not been able to make opioid drugs bring only one benefit.

But that problem is in the past. Researchers have developed a new type of opioid that selectively targets only inflamed tissues. Theoretically, such a drug will not only relieve pain, but also will not cause side effects and addiction. The invention has already been tested on rats, and the result was purely positive, so that in the near future a new drug can become a real panacea for various types of pain.

Opioids act on special receptors located throughout the human body. The molecules of the substance are compatible with them like a key with a lock, and when they interact, dopamine is released into the blood, which suppresses pain. This is great for inflamed areas, but for healthy tissue, the benefit is highly questionable. When opioids attach to receptors in the brain, they can interact with the nerves that control a person's breathing rate, slowing them down to dangerously low levels. In the gastrointestinal tract, opioids can also negatively affect the nervous system, causing intestinal obstruction (in other words, constipation). In addition to all of the above, the release of doraphin causes euphoria and relaxation, which in the future can, with a high probability, provoke dependence on drugs.

But what if we create a painkiller that selectively interacts with opioid receptors only in damaged tissues? To find out, the research team first looked at what distinguishes inflamed tissue from healthy tissue in terms of acidity. It turned out that the acidity of damaged areas is much higher than that of healthy ones, which means that the matter was small: opioids were obtained in the laboratory that bind to receptors only under conditions of increased acidity.

Christoph Stein, professor at the Department of Anesthesiology and Intensive Care at the Free University of Berlin and co-author of the article, says that such measures eliminate the risk of side effects and addiction - opioids simply do not bind to receptors either in the gastrointestinal tract or in the brain. The results of his team's study were published today in the journal Science. The new drug is called NFEPP, and it was tested in rats with a positive result: rodents stopped feeling pain without any respiratory or stomach discomfort. Even after several rats were kept on opioids for a long time, after the dose was abruptly stopped, they did not react to this fact, although usually opioid dependence develops in rats in much the same way as in humans. As for effectiveness, the new drug and the old, long-proven in practice remedy "fentanyl" turned out to be equally effective.

The next step, according to Stein, will be testing the drug in humans. Unfortunately, bureaucratic red tape comes into play here, so scientists will be lucky if they receive all the necessary permits within at least the next few months. If their work is successful, it could be a real revolution in the field of pain medication.

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