The history of meldonium in sports begins with the famous Russian tennis player Maria Sharapova. In 2016, she became a star of the doping scandal after a positive doping test at the Australia Open tournament.
The reason was not anabolic steroids, erythropoietin, or hormones, but a cardiac medication, surprising not only Sharapova but also the entire global community and even athletes who are heavily involved in pharmacology.
In this article, we will examine the facts about meldonium, learn about its medical purpose, mechanism of action, and possible side effects.
Main thoughts:
The total elimination time of meldonium from the body can reach 3-4 months with regular use.
Facts about meldonium
- Meldonium was developed by a Latvian pharmaceutical company.
- Meldonium is an inhibitor of fatty acid oxidation (it prevents their burning).
- The use of meldonium in sports is prohibited by the World Anti-Doping Agency (WADA).
- The primary indication for the use of meldonium in medicine is the treatment of heart problems, but the overall list of indications is much broader.
- Meldonium is banned for use (not licensed) in the United States, but is allowed in Russia and other countries of the former USSR.
- The drug was widely used by Soviet soldiers during the war in Afghanistan
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What is meldonium (mildronate)?
Meldonium was developed by the Latvian pharmaceutical company Grendiks.
One of the initial purposes of mildronate was to improve fertility (sperm volume) in male pigs and some other domestic animals. After that, the scope of application was expanded to humans 2.
The sales volume of the drug was 56 million euros in 2013, making Grendiks one of the main exporters in the Latvian pharmaceutical market.
From 1979 to 1989, mildronate underwent extensive “testing” on Russian military personnel: it was sent in large batches to Afghanistan during the period from 1979 to 1989.
Why?
According to the developer Ivan Kalvins, the action of meldonium consists of improving the supply of oxygen to the body.
Soldiers took meldonium while in the mountainous regions of Afghanistan when it was necessary to carry heavy equipment: the drug improved endurance in conditions of rarefied air.
Today, mildronate is a medical drug used in Eastern Europe and Central Asia (the countries of the former Soviet Union) to treat many medical conditions, but primarily cardiovascular diseases. It is banned in the United States and many other countries.
In addition to medical use, meldonium is widely used in sports as a doping agent that enhances performance.
Since the beginning of 2016, when Maria Sharapova brought it widespread fame, many athletes from different countries (including the USA, Russia, and European countries) have been blacklisted by WADA for its use.
Meldonium is a medication originally intended to increase fertility in pigs. Today, it is widely used to treat cardiovascular diseases.
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What is mildronate prescribed for in medicine?
In medicine, mildronate is prescribed to patients with impaired blood supply to certain parts of the body; in particular, for heart problems and coronary artery disease (which supply blood to the heart itself), for the treatment of angina and heart attack.
Scientific studies confirm its effectiveness for treating chronic heart failure 4 and stroke 5.
In some countries, including Russia, Latvia, Ukraine, Georgia, Kazakhstan, Azerbaijan, Belarus, Uzbekistan, Moldova, and Kyrgyzstan, doctors prescribe mildronate to improve blood supply to the brain 6.
It has been shown that it lifts mood and improves motor function, alleviating dizziness and nausea 8.
Additionally, meldonium relieves hangover symptoms after alcohol consumption.
Other indications for the use of mildronate 6:
- stomach ulcer;
- eye injuries;
- lung and respiratory infections.
If you read the instructions for the use of mildronate carefully, you will find phrases like “improves physical performance and mental activity,” although there will also be a disclaimer stating “does not affect sports performance.”
The inconsistency is evident, as it is clear that anything that improves blood supply also improves sports performance. This principle underlies the action of many doping substances.
WADA’s explanation for the inclusion of meldonium in the list of prohibited doping substances focuses precisely on this property: “meldonium increases sports performance by ensuring the delivery of oxygen to the cardiovascular system and muscles.”
In medicine, mildronate is prescribed to improve blood supply to various organs, including the heart and brain, as well as to alleviate hangover symptoms after alcohol intoxication.
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Mildronate (Meldonium) in Sports
The popularity of mildronate in sports was brought about by Russian tennis player Maria Sharapova, who failed a doping test in March 2016, three months after meldonium was added to WADA’s blacklist 1.
She admitted to using the drug for 10 years on a doctor’s prescription. See Cardiologists’ reviews on Sharapova’s use of meldonium.
Immediately after this admission, the sales volume of mildronate increased several times.
Almost simultaneously with Sharapova, Russian figure skater Ekaterina Bobrova received a ban from WADA, and that same year, the world champion in the 1500m Abeba Aregawi, and the winner of the Tokyo Marathon in 2015, Endeshaw Negesse, were also banned.
13 medalists from the European Games in Baku in 2015 also tested positive for the use of meldonium, and experts suggested that around 470 of all participants were using the drug during the event 17.
Since then, the geography of its use has significantly expanded, with athletes from Russia, Ethiopia, Sweden, Germany, and Ukraine being caught using meldonium at different times.
It is estimated that 17% of Russian athletes use meldonium and only 2% in other countries. If the figure is correct, it confirms its effectiveness.
The recent doping scandal and the ban on the participation of the ENTIRE Russian team in the Olympics indirectly indicate the recognition of the Russian doping industry, which supports professional sports, as one of the strongest and most advanced in the world.
Mildronate gained popularity in sports largely due to the name of Russian tennis player Maria Sharapova: after her admission, the sales volume of the drug increased several times.
According to WADA classification, meldonium belongs to the class of metabolic modulators, just like insulin 7.
For reference. A substance is included in the doping list if it:
- improves athletic performance;
- poses a threat to the health of athletes;
- violates the spirit of competition.
The meaning of the first criterion is obvious: an athlete taking such drugs gains advantages over others. The second criterion applies to almost any medical drug, as all of them have potential side effects. However, the meaning of the third is the most vague and allows for the “banning” of absolutely any substance.
The authors of one scientific study on the effectiveness of mildronate in sports summarize its positive effects as follows 8,15,16:
“Meldonium demonstrates improved endurance in athletes, faster recovery after training, anti-stress protection, and stimulation of central nervous system function.”
The overall list of benefits of meldonium in sports looks something like this:
- increases overall physical performance;
- improves oxygen supply to muscles;
- accelerates the excitability of nerve tissue (important for reaction speed);
- helps combat psychological stress during competitions;
- improves the supply of glucose = energy to heart and brain cells;
- accelerates the elimination of metabolic waste.
An important effect for athletes from taking mildronate is the improvement of oxygen and glucose supply to muscles, increased reaction speed, and anti-stress action.
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Mechanism of Action of Meldonium
The therapeutic action of meldonium consists of blocking the action of carnitine, which is involved in fat metabolism (burning them for energy), for the primary use of glucose 3.
During aerobic exercises (which consume a lot of oxygen), L-carnitine positively affects heart function, making fat oxidation for energy more efficient: about 80% of energy is generated through this mechanism 10.
However, in a state where there is insufficient oxygen, toxic substances – byproducts of fat oxidation – accumulate in the cells.
What meldonium does: it disables the fat oxidation mechanism using carnitine (reducing its concentration in the cells) and activates the use of glucose, which is a primary and more efficient energy source in the body, as it requires less oxygen for its oxidation 11-13.
Moreover, mildronate directly stimulates glycolysis, which further enhances the athlete’s energy efficiency 14.
The mechanism of action of meldonium consists of blocking the action of carnitine and switching the body to prioritize the use of glucose for energy instead of fats.
Is there any point in taking mildronate (meldonium) in bodybuilding?
Meldonium is especially popular in aerobic sports, such as among skiers and runners, where speed and reaction are important.
As for the use of meldonium in bodybuilding and powerlifting, contrary to popular belief, it DOES NOT directly affect muscle growth.
In strength sports, it is used to alleviate symptoms of overtraining, which is likely relevant only for professional athletes.
What is better: to reduce the load or to add another pill to your pharmacological arsenal – it’s up to you to decide.
Mildronate in bodybuilding does not directly affect muscle growth; it is used to combat symptoms of overtraining.
How to take mildronate for athletes: instructions
The indication for taking meldonium in sports is a regular state of overtraining.
In scientific studies demonstrating the positive effect of meldonium for professional athletes, doses of 0.25-1 g are typically used twice a day for 2-3 weeks of the training period, 10-14 days before competitions.
When taking it, accurate dosing is very important. The daily dose is calculated based on 15-20 mg per kilogram of body weight.
Meldonium in sports (and bodybuilding) is taken once a day 30 minutes before training.
– How long can mildronate be taken without a break?
The duration of the course is from 6 weeks to 3 months. After this, the body develops a tolerance to the drug, and it loses effectiveness. After a break of 4 weeks, sensitivity is restored.
Meldonium can be taken in two forms: tablets and injections. In tablet form, the daily dose should not exceed 2 grams. Injections are approximately twice as effective.
Sometimes mildronate is recommended to be taken together with L-carnitine and Riboxin. In the first case, there is a logical inconsistency, as the mechanism of action of mildronate consists of blocking the action of carnitine.
Meldonium in sports and bodybuilding is taken at a rate of 15-20 mg per kg of body weight once before training
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How long does meldonium stay in the body?
There is no definitive answer to the question of how long meldonium stays in the body, as it has not been studied by scientists.
Some sources report that the average elimination time is 24 hours after a single dose; if taken regularly, detection in the blood is possible even several months after stopping use.
Some experts say that complete elimination of mildronate from the body occurs within 100-120 days.
The total elimination time of meldonium from the body can reach 3-4 months with regular use
Mildronate: side effects
Existing scientific studies indicate the absence of serious side effects from meldonium.
However, according to cardiologists’ reviews, doctors consider this issue not well studied enough.
The instructions for the use of mildronate list typical side effects:
- allergy;
- tachycardia (increased heart rate);
- digestive disorders.
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Conclusion
Mildronate is a product of the domestic doping industry, which athletes from all over the world wish to try (thanks to Maria Sharapova for this).
The widespread use by Russian athletes indicates its probable effectiveness. A few scientific studies confirm the benefits of meldonium in aerobic sports (running, skiing, cycling) and indirectly in strength sports (bodybuilding, powerlifting).
Mildronate is eliminated from the body over several months and does not have serious side effects.
