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Where can I buy Meldonium. Mildronate - not doping, or even vitamin

25 Feb 2017

What is actually done so much noise meldonium (trademark Mildronat), the use of which may lead to the disqualification of a number of leading Russian athletes?

This in an interview said the head of the Latvian Institute of Organic Synthesis academician Ivars Kalvins.

Mildronat was developed by you in 70 years, and the time of its creation coincided with the operation in Afghanistan, and then later became a drug cure "from the heart" and has been gaining popularity, including the athletes, all the post-Soviet space. How and for what purpose it was designed for real?

- Work on the preparation lasted for about five years. I molecule invented at the end of 70th and the first registration is officially held in 1984. Creating the drug it was based on a desire to influence the effects of negative stress, provoking various diseases. We were looking for the cause of trying to establish a substance whose resources are drying up in the body during prolonged stress. I assumed that the physical and psychological overload can cause shortages of some unknown neurotransmitters in the human body.

The concept of "stress" (English stress -. Tension, pressure) introduced the Canadian scientist Hans Selye, based on numerous experimental studies have found that exposure to all sorts of stimuli - stressors (cold, exhaustion, fear, frustration, humiliation, etc.) - there is a stereotypical reaction, which he called "general adaptation syndrome". This syndrome is the basis of the stress - state of the body tension, which manifests itself in the revitalization of its protective and adaptive mechanisms in response to excessive stressor (in strength, frequency or duration of effect).

My hypothesis was simple: there is some substance that carries a signal from nerve cells to the cells to execute the order. When the stress load is exhausted - we are exposed to global regulation on the part of the brain. I was looking for this stuff and found a suitable candidate - gammabutyrobetaine (GBB), which is synthesized in response to the stress of the terminal amino acid molecules in the connective tissue, and this muscle, etc...

If the molecule is synthesized, it is rapidly converted to carnitine, a natural substance, related B vitamins are well known for use as a food additive in bodybuilding. Once disconnected end of the molecule, the signal can not be synthesized.

We tried to slow down the conversion of GBB in carnitine. I have created a molecule substantially the same GBB, only one carbon is replaced by nitrogen. It turned out that it is possible to restore the concentration of GBB, carnitine concentration and falls. As a consequence, reduced blood transport of fatty acids into the cells, which leads to some reduction in physical performance, but at the same time turn on the use of sugar, and it is very useful when you do not have enough oxygen. If burned sugar, we can obtain the same amount of power using a smaller amount of oxygen.

A detailed study of pharmacology and biochemistry confirmed that lowers meldonium carnitine in the human body and stores the rate of metabolism and the rate of fatty acid oxidation for energy production is reduced. This allows the cells to compensate for the lack of oxygen during physical exertion. So meldonium is a protective drug that does not lead to an increase in energy efficiency or the physical abilities of the person.

- When is it prescribed to athletes? What is the impact on the body meldonium?

- Athletes train a lot of work on the limits of their physical capabilities. It is advisable to encourage them Mildonium as cell protection, in order to protect them from heart attacks and damage to muscles in the case of overtraining.

It should be borne in mind that one gram of fat energy can produce 2.5 times more than a gram of glucose. The process of reducing the rate of fatty acid oxidation can not result in more energy production, but it protects cells from death, which occurs when the oxygen deficiency, since then the fats accumulate in the cell in an activated form and completely block transport across the produced energy, i.e. ATP from production place to place of consumption. Moreover, these activated fatty acid - a «soap», which dissolves all cell membranes, and the cell dies.

So, if using mildronate you reduce the flow of fatty acids into the cell, in the case of oxygen starvation of the cell is alive! The cell can not work more than before, just energy will be less - but she survived. And for the athlete is the insurance of his life and his health. Since the oxidation of glucose reduces the oxygen demand for energy, the heart is protected from ischemic damage in case of overload. So meldonium is the protector of the heart during ischemia, which allows to train more stable and safe for the health of the athlete.

If the athlete crossed the line when stress begins before training, when cells begin to die, against the background of mildronate consequences are catastrophic, it will not have any microinfarcts or large massive heart attack. Even if the athlete fell, the last effort before reaching the finish line, the next day it will not lie on a hospital bed.

- And yet, the "official" is mildronat - doping vitamin or medicine?

- Mildronate - not a drug and does not improve the results, it does not increase the athlete's ability to work above the normal. Doping is, in fact, depletes your body's reserves. With his admission that something is introduced into the body, which exceeds the norm that there can be - steroid hormones in excess and so on, and ultimately - you injure your health. Meldonium and not a vitamin. It's really good acting drug that prevents cell death in case of overload.

- But the World Anti-Doping Agency classifies Meldonium to extremely serious S4 category - hormones and modulators of metabolism. For his use of an athlete can be suspended from playing for a period of up to four years. How do you assess the decision of WADA? How it was made, whether the submitted proof of justification for this decision? Did you consult with the representatives of WADA?

- The decision to ban mildronate was taken without any scientific justification was. Five years ago I was approached from a European WADA department asking if I could tell what mildronate how it works and whether it is doping. I wrote them all that I know about mildronat, and brought a scientific basis that the drug is not doping. They thanked me for clarification and agreed with me.

I believe that the inclusion in the list of banned mildronate unacceptable. For me it is unlawful decision. Athletes have the same rights as those of any other people. They have the right to use drugs that prevent harm to their health. Especially when there is no evidence that the drug makes them stronger. This is the same that prohibit athletes to eat meat with a high content of carnitine, increases the rate of fatty acid oxidation and stimulates the production of energy.

- In such a case can be considered similar to WADA exclusively political decision?

- Of course! We live in an era of evidence-based medicine. Which means that if you make a claim, prove it! No further medical research to prove the harmfulness mildronate, was not carried out. So, if the medicine, 32 years benefiting healthy and sick people suffering from diseases related to oxygen starvation, called doping, it is nothing else, as the allegation.

- Is it possible to overturn this decision, WADA? What does that require?

- Obviously, it is necessary that the athletes, coaches and doctors have started this fight. And I'm happy to join them. It is not proven that the use of meldonium increases "productivity" of athletes, the ban should be lifted.

- Recently it was reported that your Institute has created a new molecule, the effectiveness of the drug on the basis of which is 40 times higher than the efficiency of mildronate. Whom he will target?

- The calculation here is - 20 times lesser dosage can achieve the effect of increasing twice. In fact, this new molecule, which was developed by my lab, will treat a heart attack, even if the first injection will be administered two hours after the onset of infarction.

- When the new wonder-drug may be on the market?

- Five years. Already completed preclinical studies - is a fundamental stage in the development and implementation of the drug in clinical practice.

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