What You Need to Know Before Using Meldonium (Mildronate)

For most of the years since it has been around, meldonium was a rather obscure drug. But its popularity has surged tremendously in the last couple of years after a popular tennis player tested positive to it. There has been so much debate on efficacy, even though its use in sports is prohibited.

What do sports people hope to benefit from using this substance? Does it offer real medical benefits? We cover all you need to know about meldonium in this article.

What is Meldonium?

Meldonium is the same thing as the drug known as Mildronate – the latter is its most popular trade name. Although some think of it as a steroid, it is not really that type of compound. The drug is a structural analogue of gamma-butyrobetaine.

To create this drug, the C-4 methylene of gamma-butyrobetaine is replaced with an amino group. Meldonium comes in a white crystalline powder form. Gamma-butyrobetaine is a precursor to carnitine, which is a major reason behind the beneficial effects of the drug.

Meldonium was created by Ivars Kalvins at the Institute of Organic Synthesis of the Latvian SSR Academy of Sciences in the 1970s. Its production is primarily done today by a Latvian drug company named Grindeks. It is reportedly one of the former Soviet nation's biggest medical exports. The company reported sales of €65 million in 2013.

Use in animals was among its earliest uses. It was used to boost sperm motility and sexual performance of boars. It was reportedly also used to promote growth in livestock and poultry.

Aside Mildronate, meldonium has been marketed under a number of other names. These include Mildronats, MET-88, Quaterine, and THP.

Medical Uses

In medicine, meldonium is principally used in the treatment of cardiac health issues. Doctors, particularly in Eastern Europe, use it to treat coronary heart disease. It is believed to help against angina and myocardial infarction, which many people know as heart attack.

Heart problems can give rise to ischemia. This is a condition where insufficient amounts of blood flow to organs in the body, including the heart. Meldonium supposedly helps to dilate blood vessels to improve the flow of blood and oxygen.

The drug alters pathways for carnitine through inhibition of the enzyme gamma-butyrobetaine dioxygenase (GBB). This reduces production of carnitine in the body, forcing the mitochondria to use glucose for energy generation. What this means is less oxidative stress and cellular damage than when reliance is on fatty acid beta oxidation.

It is believed Mildronate lowers the levels of trimethylamine N-oxide, a carnitine breakdown product thought to contribute to atherosclerosis and congestive heart failure. It supposedly promoted peripheral circulation and exercise capability in a 2005 study when combined with lisinopril, a substance which inhibits angiotensin converting enzymes.

The drug has been shown to be effective for treatment of acute ischemic stroke. It also appears to have anticonvulsants and antihypnotic benefits, making it potentially beneficial for seizure and alcohol intoxication treatments. Other conditions meldonium is used for include ocular ischemic syndrome and cerebral ischemia.

There is also talk of Mildronate offering nootropic benefit. It purportedly improves alertness and cognitive function.

Uses in Sports

Many people were not aware of the existence of a drug named meldonium until tennis superstar Maria Sharapova tested positive to it in 2016. That incident effectively brought it into the limelight.

However, meldonium is a controversial compound. There are claims and counterclaims about its efficacy. While its mechanism of action and findings from certain studies show that it can enhance performance, critics say there is really no definite and reliable evidence that it improves athletic performance.

But the fact that this drug has been on the list of banned substances by the World Anti-Doping Agency (WADA) since 2016 can easily be seen as a confirmation that meldonium is a performance enhancer.

And by looking at the mechanism of action, you may easily notice that this one offers potential for improved performance. It is obvious that when blood flow and oxygen levels improve in the body a person is likely to perform better.

A study that appeared in the journal Drug Testing and Analysis in 2015 noted that meldonium improved the endurance levels and performance of athletes. It helps sport people to also recover faster following workouts. The drug also enhances activations of neurons in the central nervous system (CNS), thus improving athletes’ reaction time.

By the way, among the early users of meldonium were Soviet troops fighting in Afghanistan. It was meant to boost the endurance of the soldiers by improving their body oxygen levels in the mountainous terrain of the South Asian country.

Apart from Sharapova, numerous other athletes have returned positive samples for the drug. The notable ones include:

Ekaterina Bobrova (Russian figure skater)
Abeba Aregawi (Ethiopian-born Swedish runner)
Pavel Kulizhnikov (Russian speed skater)
Semion Elistratov (Russian short track speed skater)
Andrei Rybakou (Belarusian weightlifter)
Gabriela Petrova (Bulgarian triple jumper)
Maxwell Holt (American volleyball player)

Most of these were cleared or had their bans lifted. They reportedly used the drug before its use was prohibited by WADA.

How is Meldonium Used?

Meldonium comes as tablets, capsules, or vials. The amount to use may be influenced by the form in which you are taking it.

For therapeutic purposes, daily dosage mostly ranges between 500 mg and 1000 mg. This will be divided into 2-4 smaller doses to be taken at different times of a day. The recommendation for treatment of chronic alcoholism is 500 mg taken four times a day.

The main company making meldonium recommends that therapy should ideally not last for more than 4-6 weeks. Duration of therapy is even shorter in the case of chronic alcoholism, and mental and physical stress.

Those interested in Mildronate for its athletic benefits are to take 500mg to 1000 mg two times per day. This may be lower when combining the drug with some other compounds.

And when talking about stacking, there is no notable information on what other compounds to combine meldonium with to improve athletic performance.

Sports people typically use the drug before training. Duration of use during preparatory phase is about 2-3 weeks. Another two weeks, or less, of use then follows in the lead up to a competition.

You will do well to first discuss with your doctor before commencing meldonium use.

Availability Of Mildronate

Mildronate is considered a limited-market drug. It is mainly available in select countries. More specifically, it widely sells in Eastern European and Central Asian countries. It is a licensed medical drug in these places, where it is not hard to get over the counter.

Grindeks has its offices spread across over a dozen countries in Eastern Europe. It sells the drug as an anti-ischemia medication there.

You may not be wrong describing Mildronate as a Eastern European drug then. Most of the athletes that have tested positive to it till date were from that part of the world.

Meldonium is not approved for use in the United States or by the European Union. It currently has too little evidence for the U.S. Food and Drug Administration to grant it approval. Huge sum of money, more than Grindeks can provide, may be needed to carry out necessary research.

In terms of the legal status, meldonium is not a scheduled substance in America. But that doesn't necessarily make it legal to use for whatever purpose.

Risks and Side Effects Of Meldonium

There is insufficient research on effects of Mildronate in humans. Most studies focused on animals and human trials are not of satisfactory standards to many experts. What this means is that not a lot can be said about adverse reactions.

However, some side effects that are thought possible from use include:

Rash
Itching
Swelling
Allergic reactions
Irregular heartbeat
Blood pressure changes

Some experts think that those using meldonium right now are somewhat putting themselves forward as guinea pigs. Other people will likely learn about the drug’s safety, or lack of, from effects on such individuals.

Conclusion

Meldonium is a drug that exhibits clear mechanism of promoting cardiac health and boosting athletic ability. However, it still lacks significant research, making it a subject of so much debate.

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REFERENCES

Meldonium - Wikipedia (https://en.wikipedia.org/wiki/Meldonium)

Meldonium (Mildronate): What Is It And What Does It Do? (https://www.medicalnewstoday.com/articles/309165.php)

Benefits of Meldonium and Side Effects (https://nootropicsreviewed.com/meldonium-benefits-side-effects/)

What Would Happen If You Took Meldonium? - Men's Journal (https://www.mensjournal.com/health-fitness/what-would-happen-if-you-took-meldonium-w200313/)

MILDRONATE®, (aka Meldonium, THP, MET-88, Mildronats, Quaterine) 40pills/pack, 250mg/pill (http://rupharma.com/mildronate/)