Meldonium Effects for Athletes: What is Mildronate Used for?

In connection with the frequent doping scandals, many sports fans today are interested in the question of what Meldonium is, and why is it used by professional athletes? It will not be possible to answer so immediately, at least because there are cases of unintentional intake of Meldonium by athletes and athletes.

To give a complete answer, we delved deeper into the study of the topic. And now we want to tell you about the most interesting facts that we managed to find out.

The history of Meldonium (Mildronate, Mildronāts and other trade names) as a sports doping began relatively recently. Namely, from the scandal around the titled Russian tennis player Maria Sharapova. Then, in 2016, after a positive doping test at the Australia Open tournament, the athlete was accused of using a prohibited drug.

When the details of the case were not yet known, the media attributed to Maria the use of steroids (mainly about oxandrolone), erythropoietin and other hormones. But none of the initially named options turned out to be correct. To the surprise of the public, the culprit was a cardio drug, which until that moment was known only to a few people as an effective doping agent.

Key facts about Meldonium:

• Meldonium was developed by Soviet pharmacists as an industrial and veterinary medicine.
• According to its pharmacological action, Meldonium is an inhibitor of fatty acid oxidation, an analogue of gamma-butyrobetaine.
• The use of Meldonium products in sports is prohibited by WADA (World Anti-Doping Agency) and is punishable by sanctions up to life suspension.
• The main indication for the use of Meldonium in medicine is the treatment of cardiovascular diseases, but the general list of medicinal indications is much wider.
• Currently Meldonium is an unlicensed drug in the USA (banned for use and distribution). But in the Russian Federation and other countries of the former Soviet Union, this is the official drug.
• There is information indicating the widespread use of Meldonium during the war in Afghanistan (to raise the combat capabilities of Soviet soldiers).

History

Meldonium was synthesized by Soviet chemists in the mid 70s of the last century. Nowadays the Latvian pharmaceutical company “Grindex” is actively engaged in its production under the Mildronate trademark. Thus, in 2013, the sales of the drug amounted to 56 million €, which made “Grindex” one of the main exporters on the Latvian market.

The compound was originally patented as a growth stimulating agent for plants, animals and poultry. In addition, it was reported about its use in light industry (for the synthesis of polyamide resins). In veterinary medicine, one of the initial indications for the use of Meldonium was to improve the fertility of male pigs and other domestic animals (supposedly increasing the volume of ejaculate production).

Meldonium underwent a mass “test” on humans between 1979 and 1989. It was delivered to Afghanistan and tested on the Soviet military. For what? According to the inventor of the active substance, Professor Ivars Kalvins, the effect of Meldonium is to enhance the transport of oxygen in the body. And for the Soviet soldiers, it came in handy in the mountainous regions of Afghanistan, increasing endurance and improving well-being after the first intake.

Today Meldonium (Mildronate and its analogues) is an official drug that is widely used in Eastern Europe and Central Asia (mainly the countries of the former Soviet Union). Our drug is useful in various fields of medicine, but most often it is used in cardiology. For example, in treatment after myocardial infarction and stroke. In Western countries including England, France and the USA, Meldonium has never been certified.

It is no longer a secret that in addition to traditional medicine, the active substance is widely and unofficially used in sports. Regular viewers learned about its effectiveness as a functional doping only in the last 5-10 years. It was blacklisted by WADA on January 1, 2016, a few months before the accusations against the famous Russian tennis player Maria Sharapova.

Meldonium in Medicine

To simplify medical indications, Meldonium is intended for patients who have impaired blood supply to certain organs and parts of the body, in particular with problems with the heart and brain – coronary artery disease, heart attack and stroke treatment. Its effectiveness in this direction is confirmed by clinical trials: an experiment in 2005, a study in 2013.

In the Russian Federation and in neighboring countries, including Georgia, Moldova and Latvia, Meldonium can also be used to elevate mood and improve motor function in debilitated patients. It is able to eliminate nausea and dizziness. And one more useful property: Mildronate and its analogues alleviate hangover symptoms after alcohol abuse.

Other (additional / alternative) indications for use:

• Angina;
• Stomach ulcer;
• Damage to the visual organs;
• Infections of the lungs and respiratory tract.

If you study the instructions of any official drug with meldonium as an active ingredient, it will be indicated that it “improves physical performance and mental activity.” In this case, there is always a postscript that the drug “does not affect sports performance.”

Inconsistency on the face, or rather deliberate deception. If pills or injections are ways to improve performance, then they a priori affect athletic performance. After all, the effectiveness of most doping drugs used today in athletics, swimming, biathlon, football, hockey, tennis, and even in martial arts is based on the principle of increasing endurance and concentration.

WADA explained its decision to add Meldonium to the list of prohibited drugs with this property: “It increases athletic performance by stimulating the supply of oxygen to muscle tissue and the cardiovascular system.” So, no matter how the official manufacturers try to convince us otherwise, the use of Meldonium undoubtedly affects the results of athletes and athletes.

What Does Meldonium Do for Athletes?

Following the allegations in March 2016, Maria Sharapova organized a press conference where she confessed that she had used Meldonium for the past 10 years (intermittently) as directed by her doctor. The athlete claims that she simply missed the moment when the active substance was banned by WADA. Otherwise, she would immediately stop taking it, replacing it with an analogue approved by the World Anti-Doping Agency.

As a result, during 2016, the sales of the Latvian Mildronate increased several times.

Almost simultaneously with Maria, the domestic figure skater Ekaterina Bobrova was disqualified from WADA for Meldonium. Also, until the end of the year, a ban for a freshly banned substance was given to the world champion in 1500 meters Abeba Aregawi (Sweden) and the winner of the Tokyo marathon in 2015 Endeshaw Negesse (Ethiopia). But the scandalous news does not end there. 13 medalists of the European Games in Baku also tested positive for Meldonium. According to experts, at those competitions Mildronate used at least 470 athletes and athletes. This is almost 8% of the total number of participants.

Thus, the geography of Meldonium has grown from Russia and the CIS to foreign countries: Sweden, Germany, Great Britain, Canada, Egypt, Algeria, Ethiopia, and this is not a complete list. It is believed that about 17% of Russian athletes have ever used or continue to use the drug banned in 2016. In the West, the figure is more modest, but still impressive – about 2% (in terms of souls – hundreds, if not thousands of professionals from all over the world).

It is difficult to call this a reason for pride, but the recent high-profile scandal with our Olympians, which continues to this day, has strengthened Russia in the status of the leader of the world doping industry. Against this background, the news about Meldonium seems to be an old, forgotten stain on the reputation.

According to the WADA classification, Meldonium belongs to the class of metabolic modulators. Insulin belongs to the same category of active substances.

For reference, the World Anti-Doping Agency recognizes a drug as prohibited if it meets at least one of the following criteria:

• Improves functional performance;
• Poses a threat to the health of athletes;
• Breaks the spirit of competition.

The meaning of the first criterion is clear: an athlete who takes a drug that improves his functional performance gains an advantage over his rivals. With the second, everything is also more or less obvious. Although, judging by such a vague wording, any drug can be considered doping. After all, there are no medications without side effects. Even ascorbic acid can be poisoned if consumed uncontrollably. And what about the third point? It is the most controversial, because neither WADA nor other anti-doping organizations define the spirit of competition. The athletes themselves roughly understand what this means, and that’s okay.

Returning to the description of Meldonium, scientific studies from 2002 to 2015 allowed us to summarize its positive effects on the athlete’s body:

“The active ingredient demonstrates the ability to increase endurance, speed of recovery, physical and mental performance, provides anti-stress protection and stimulates the functions of the central nervous system.”

If you list all the positive effects of Meldonium in sports point by point, you get an impressive list of benefits:

• Improves the transport of oxygen to the muscles;
• Increases the supply of glucose to the cells of the heart and brain;
• Stimulates the central nervous system (this is important for the speed of reaction);
• Reduces psychological stress during the competition;
• Accelerates the elimination of decay products from the body.

It is clear that in terms of the severity of the doping properties, Meldonium is inferior to most hormonal agents, especially anabolic steroids. But it is unlikely that even among the most “repulsed” experts there will be a madman who would argue that Mildronate and its analogues were accidentally included in the list of prohibited drugs. Why they got there only now is an interesting question.

Mechanism of Action

The therapeutic effect of Meldonium is due to the suppression of gamma-butyrobetaine hydroxinase, inhibition of carnitine synthesis and blocking the transport of long-chain fatty acids through the cell membrane, preventing the accumulation of activated forms of unoxidized fatty acids in cells.

In simple terms, when performing aerobic exercises that actively use oxygen, the drug promotes the functions of the cardiovascular system, increases energy efficiency or reduces body fatigue.

On the other hand, when anaerobic exercise is performed, Meldonium, by slowing down the production of carnitine and inhibiting the oxidation of fats, activates the use of glucose as the main (and in this case more efficient) source of energy, since it does not require as much oxygen to oxidize it. In addition, the active ingredient directly stimulates glycolysis, which further improves the performance or recovery of the athlete.

Meldonium and Bodybuilding

A controversial issue, since each pitching has its own goals in the gym.

Globally, Meldonium is considered an athletics doping (most effective in sports where aerobic activity prevails). On its own, it does not in any way affect the set of muscle mass or the increase in strength indicators. However, this does not mean that the drug is completely useless for iron sports fans.

For example, bodybuilders can use it to relieve symptoms of overtraining. It can also be beneficial for weight loss and drying, that is, in the active phase of cardio training. It’s up to everyone to decide whether it’s better to stick to a moderate exercise without the risk of overwork, or add another drug to the medicine cabinet to avoid overtraining.

Let’s be honest, among the classic sports pharmacology there is a more effective doping for endurance, ranging from oxandrolone to erythropoietin. Therefore, if you decide to break the rules for the sake of results, it is better to do it with “chemistry” that works 200%.

As for the rest of the athletes, just keep in mind that after 2016, steroids and Meldonium are subject to identical sanctions.

How Long Does Meldonium Stay in Your System?

No official research has ever been conducted to determine when Meldonium was found, so there is no definitive answer to this question.

According to some sources, after a single dose, the half-life (half-life) of the active substance does not exceed 24 hours. And if the application is carried out regularly, as for sports purposes, then in this case the metabolites of Meldonium remain in the body for up to several months.

If you give some specific figures, then, according to the developers, the complete elimination of the active substance can take up to 100-120 days. However, there are cases when an athlete drank Meldonium 3-4 months before the competition, and the doping test before the tournament still gave a positive result. The deadline, which is called on the Internet, is 6 months by gas chromatography / mass spectrometry.

How to Take Meldonium?

The main indication for the use of Meldonium in sports is considered to be a prolonged state of overtraining.

In clinical studies that demonstrate the beneficial effects of Meldonium preparations for professional athletes, doses of 0.25-1 grams are generally used twice a day for 2-3 weeks of active training, for example 2-3 weeks before a competition.

When used for sports purposes, it is very important to determine the individual dosage. On average, the daily dose is selected according to the formula 10-20 milligrams of active ingredient per 1 kilogram of its own weight.

In strength sports, the dosage regimen of Meldonium is slightly different. Here, the drug is recommended to be used once a day (15-45 minutes before training).

How long can Mildronate (or equivalent) be used without adverse effects on the body?

The duration of athletic courses varies from 6 weeks to 3 months. After that, the body develops tolerance (immunity) to the active substance. Take a 4-week break before continuing or repeating the cycle. This period is usually enough to restore sensitivity to the drug.

Meldonium is commercially available in two forms of release – a tablet in a hard shell or a suspension for injections. A single dose of tablets should not exceed 2 grams. Injections have about 2 times higher bioavailability than oral agents.

We add that on the Internet you can find a recommendation to drink or put Meldonium together with L-carnitine and Riboxin. The first option looks at least illogical, because the therapeutic effect of Meldonium is precisely due to the inhibition of the natural production of carnitine. The Riboxin option is not satisfactory if you want to limit yourself only to pharmacy products.

Conclusion

Thus, what we managed to find out about Meldonium:

1. Initially it is a drug, even a veterinary drug. So in veterinary medicine they wanted to use it to stimulate the growth of weakened animals and poultry, but not only.
2. In traditional medicine, Meldonium is primarily valued as a cardio drug. It is used to treat heart failure, heart attacks, stroke (circulatory disorders in the brain). But the full list of indications for the use of the active substance is not limited to cardiology.
3. If we consider Meldonium as a sports doping, then the mechanism of action of the drugs is determined by blocking carnitine and then switching to using glucose as the main and more efficient source of energy for the body of an athlete or athlete.
4. Probably, in narrow circles, Meldonium was in demand even before the scandal with Maria Sharapova, but it became widespread only in 2016, after the WADA ban and against the background of accusations against the Russian tennis player. Then the benefits of the active substance during the competition were proven.
5. A key effect of Meldonium for athletes is increased energy efficiency – improved oxygen transport and increased overall endurance. In addition, the drug has an anti-stress effect.
6. The use of Meldonium preparations in bodybuilding is impractical. For strength sports, it is recommended purely for specific purposes, for example, to reduce the symptoms of overtraining.
7. Its average single dose for sports purposes is 10-20 milligrams per 1 kilogram of its own body weight. Reception is carried out shortly before training.
8. Removal of Meldonium metabolites from the body can take up to 3-4 months, respectively, during this period it is easily detected during a doping test.
9. The indisputable advantage of the drug is the almost complete absence of side effects. Not a single case of overdose has been officially registered.

In conclusion, it should be clarified that this article is by no means a call for the use of Meldonium for sports purposes. We just wanted to consider in detail this active substance as a doping, so that even people far from sports could understand why professionals need Meldonium, and why they are punished for it.