Meldonium – pharmacological properties of the drug, use in sports and medicine

Meldonium in sport is one of the most discussed topics in the world and domestic media. This drug, once included in the list of substances allowed for athletes, is officially recognized as doping by the World Anti-Doping Agency (WADA). Meanwhile, the majority of domestic scientists and sports nutrition specialists do not agree with the decision of this organization and consider meldonia an innocuous medicine, not related to stimulants of physical activity.

Let’s try to figure out what meldoniy is, how the given drug works, what is the use and harm of meldonia, why it is taken by athletes and why meldonium is recognized as doping. We will also consider the history of the preparation and find out what its applications are.

Meldonium – general information, history of creation

The drug is a metabolic drug, known in medicine as “Mildronate.” The action of meldonia on the body – stimulating and protective: the substance normalizes the work of cells that have undergone hypoxia (oxygen deficiency) or nutritional deficiency.

In medicine, the drug is used quite widely: for example, it is part of complex drug therapy for coronary heart disease (ischemic disease), heart attacks and heart failure. In Russia since 2012, the drug is included in the list of vital drugs. In Russian pharmacies the cost of mildronate in tablets is in the range of 150-270 rubles.

Meldonium was obtained in the 1970s in the Latvian SSR at the Institute of Organic Synthesis. Initially, the remedy was patented as a stimulant for the growth of domestic animals and birds and was used in agriculture and industry. The creator of the drug Professor Ivars Kalvinsh argues that the idea of ​​using meldonia in medicine arose after his long use in other industries.

In 1984, the drug was patented in the United States, but a few years later it was banned from use. Mildronate analogs exist in the USA, but it is almost impossible to get them in ordinary pharmacies, although in medicine the effectiveness of meldonia is not in doubt among doctors and pharmacists.

Application in medicine – indications, forms of release, pharmacological action

Meldonium is a white powder with a pronounced crystalline structure. Preparations are produced in tablet form (capsules with a soluble coating) and in the form of ampoules for injections.

Indications for the use of Mildronate are:

  • Cardiac ischemia;
  • Heart attack;
  • Stroke;
  • Heart failure;
  • Nervous and physical exhaustion;
  • Decreased performance due to excessive loads;
  • Postoperative period (to accelerate recovery);
  • Insufficiency of blood circulation;
  • Abstinence in alcoholism 2-3 stages;
  • Chronic bronchitis, asthma and other pathologies of the respiratory system, accompanied by oxygen deficiency;
  • Ophthalmic (eye) diseases (retinopathy, thrombosis of the eye veins, hemorrhages in the retina);
    Complications of diabetes.
  • The use of meldonium in sports is justified by its stimulating effect, but there is an opinion that it is inexpedient to apply this medication to absolutely healthy people.

The active substance of mildronate accelerates the synthesis and movement of ATP in cellular structures, which positively affects the functional and energy status of the cells and tissues themselves. With infarcts, the substance slows the irreversible necrosis of the heart muscles, and with strokes and ischemia of any etiology improves blood circulation. When hypoxia (oxygen deficiency), the drug helps to deliver oxygen to the cells in accordance with their needs in such.

The tablet form of the drug is well absorbed in the digestive tract. Bioavailability of the drug – 78%, the maximum content of active substance in the blood is reached after 60-90 min. after the reception. Time to remove meldonia from the body – 12-24 hours, but some samples can detect the substance in the body, even 120 days after use.

Contraindications

The drug is contraindicated in pregnant women, children under 18 years (due to lack of clinical trials), people with individual intolerance to the active ingredient or excipients of the medication. It is not recommended to use without medical purpose. When an overdose is possible gastric disorders, tachycardia, pressure surges, skin allergic reactions in the form of redness, itching, edema.

In recent years, the impact of meldonia on the body of diabetics has been seriously studied. During the tests on animals, it was found that the substance is able to lower the concentration of glucose in the plasma, without affecting the level of insulin. In passing, the risk of acidosis and other consequences of metabolic disorders is reduced.

Application in sports

Meldonium in bodybuilding and in sport is used not so long ago. Most athletes until recently treated the drug as a vitamin that does not affect athletic performance. The doping scandal with meldonia changed the attitude to the medicine in Russian sports. Now the substance is officially classified as a class of hormones and modulators of metabolism, and its use is prohibited during the competitions and in the period of preparation for them.

Why do athletes take meldonies? Domestic and some foreign specialists in sports nutrition and pharmacology argue that meldonium has always been used by athletes as a means to adapt to increased loads and accelerate rehabilitation after heavy training, but has never been taken to stimulate and increase physical abilities.

Doping scandal and its analysis

Meldonium is on the list of banned drugs since January 1, 2016 (before that the substance was on the list of monitoring of the international committee). Now for the use of this substance during official competitions athletes are threatened with disqualification for 4 years.

Doping scandal in the Russian sport began with the recognition of Maria Sharapova in the application of meldonia for 10 years. According to the famous tennis player, she took medicine for medical purposes.

After that, several other athletes (mainly from the CIS countries) were also found to be using the drug. List of athletes who have been found meldonia, is very extensive. There is no need to quote all the names (there are more than 60 of them on the list), especially the scandal participants themselves do not agree with the conclusions of the doping commission.

Representatives of the government of the Russian Federation support the position of the sportsmen: Deputy Prime Minister A. Dvorkovich stated that the Russian side instructs on conducting additional studies on this issue. At the same time, the Russian president believes that it is not worthwhile to look for signs of an international conspiracy in the doping scandal and urged sports functionaries to respond promptly to changes in the list of banned drugs.

The opinion of the creator of the drug Professor Calvins is unequivocal: substance is not doping by definition. Medical means, which contain meldonia, are used in the therapy of cardiac pathologies: there is no scientific evidence for the influence of this component on a person’s physical capabilities.

Such studies were simply not carried out, but in theory, athletes taking mildronate or its analogs should expect a deterioration in the results, since the active substance slows down (inhibits) the oxidation of fatty acids. The decision of the Anti-Doping Commission Ivars Kalvinsh considers a serious professional mistake.

Сonclusions

Not all specialists agree with the statement that meldonium is a dope and affects the increase in performance in athletes. But there are a number of undeniable factors concerning this drug. Let’s list the most important of them:

  • Meldonium is used as an effective medicine for heart diseases and some other pathologies.
  • Full-scale studies confirming the effect of the drug (or lack thereof) on endurance have not been conducted. This casts doubt on WADA’s unequivocal conclusions about the presence of pronounced doping properties in meldonium.
  • Healthy people should refrain from unauthorized use of mildronate as a stimulant for physical and mental stress.
  • The drug positively affects the health of athletes with medical problems of cardiovascular nature, but does not guarantee victory in competitions.

It is clear that until the end of the doping scandal take molodonium and its counterparts athletes is not recommended. But people who are prescribed by qualified doctors should continue the therapy without fear of negative consequences.

local_offerevent_note November 9, 2017

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