Mildronate Ban and Doping Scandal

In 2015, 17% of Russian athletes and 2% of athletes from all countries tested positive for mildronate

Mildronate was one of the main components of pharmacological support for domestic athletes. According to French experts, mildronate tends to accumulate and remain in the body for up to 120 days.

Back in October 2015, at the international level, the anti-doping commission decided to include the drug mildronate-meldonium in the monitoring list.[1] The decision to ban came into force on January 1, 2016, while the doping scandal broke out in March.

News reports spread that mildronate was banned at the initiative of the U.S. Anti-Doping Agency (USADA). According to the source, the U.S. Anti-Doping Agency began researching meldonium back in 2014. In the fall of the same year, USADA obtained data on doping samples of athletes from the former Soviet Union, in which meldonium was detected. Of the 8,300 samples analyzed, 182 contained traces of the drug. As a result, based on these studies, the drug was officially added to the list of banned as of January 1, 2016.[2]

"The doping scandal" with Mildronate caused a sharp increase in interest from buyers: in the last three days, Mildronate and Cardionate meldonium drugs are the leaders of information demand among drugs. For example, according to the drug ordering service Apteka.ru, sales of Mildronate increased approximately 15-20 times over March 7-8. At the same time, no special promotional efforts were made for this product.[3]

Positive doping samples from athletes

Several Russian athletes have already been suspended from competitions for using mildronate. Positive doping tests for mildronate were given by Semyon Elistratov, leader of the Russian men's short track team, 2014 Olympic champion in the relay, 2015 world champion in the 1500m and 2016 European all-around champion, and 2014 Olympic champion in figure skating Ekaterina Bobrova, winner of five Grand Slam tournaments and 2012 Olympic tennis medalist Maria Sharapova, five-time world speed skating champion Pavel Kulizhnikov and volleyball player Alexander Markin of Dynamo Moscow and the Russian national team.

In April, a statement came out that the decision to temporarily disqualify athletes found to have used meldonium remains with the federation if the concentration of the substance in a doping sample taken before March 1, 2016 is between 1 and 15 mcg, or if in a doping sample taken after March 1 its concentration is less than 1 mcg. Thus, virtually all Russian athletes whose meldonium was detected in their bodies will be exonerated.

Indications for Use

Indications for the use of meldonium:

impaired performance;

Physical overexertion, including in athletes;

Coronary heart disease (angina pectoris, myocardial infarction, chronic heart failure, and cardiac dystrophy)

infectious allergic bronchial asthma and chronic non obstructive bronchitis (as an immunomodulator in combination therapy);

withdrawal syndrome in chronic alcoholism (in combination with specific alcohol therapy);

Acute circulatory disorders in the retina, acute and chronic circulatory disorders of the brain (cerebral strokes and chronic insufficiency of the cerebral circulation).

Contraindications for use:

Use with caution for long-term use in people with chronic liver and kidney disease.

Effects of mildronate in bodybuilding

Prevents the accumulation of activated forms of unoxidized fatty acids in cells.

In ischemia restores the balance of oxygen delivery and consumption in cells, preventing ATP transport disruption.

Activates glycolysis, which proceeds without additional oxygen consumption.

Improves muscle nutrition.

Increases training efficiency.

Reduces fatigue.

Protects the heart and increases myocardial contractility.

How to use and doses

"Attention" Mental and physical overload, including bodybuilding and powerlifting.

Adults 15 to 20 mg per kg of weight once daily, preferably 30 minutes before training. The recommended course of treatment is from 6 weeks to 3 months. Then it is advisable to take a break for a month so that the effectiveness of the effects of mildronate on the body is not reduced.

Heart disease

Stable angina pectoris. By 0.25 g orally three times a day for 3-4 days, then twice a week to 0.25 g orally three times a day. The course of treatment is 1-1.5 months. During long-term treatment the drug is combined with long-acting nitrates.

Unstable angina pectoris and myocardial infarction. It is 0.5-1.0 g by intravenous stream once a day, after which the patient is prescribed the drug orally by 0.25 g twice a day during the first 3-4 days, then twice a week by 0.25 g three times a day.

In acute coronary circulatory failure in the necrotic period of myocardial infarction orally 0.25 g twice a day during the first 3-4 days. Patients with acute heart failure additionally prescribe fast-acting cardiac glycosides (strophantine, corglycon, celanide) and diuretics.

Cardialgia against myocardial dyshormonal dystrophy. By 0.25 g orally twice a day in the morning and in the evening. The course of treatment - 12 days.

Additional information

Source: Methods of research and pharmacological correction of human physical performance.

Edited by I.B. Ushakov, Academician of the Russian Academy of Sciences, 2007.

Mildronate (mildronate) has cardioprotective, antianginal, antihypoxic, angioprotective effect. It is a structural synthetic analogue of γ-butyrobetaine, a precursor of carnitine. It inhibits γ-butyrobetaine hydroxylase enzyme, decreases carnitine synthesis and long-chain fatty acids transport through cell membranes, prevents accumulation of activated forms of unoxidized fatty acids in cells (including acylcarnitine, which blocks ATP delivery to cell organelles). It improves metabolic processes. In ischemia it prevents ATP transport disruption and activates glycolysis. The decrease in carnitine synthesis in the cell increases the content of γ-butyrobetaine, which has a vasodilatory effect. Against the background of heart failure it improves myocardial contractility and increases exercise tolerance. Increases cellular and humoral immunity. Improves performance, reduces symptoms of mental and physical stress, increases endurance. When taken orally it is well absorbed from the gastrointestinal tract. Bioavailability is about 78%. Maximum concentration in blood plasma is reached after 1-2 hours. The elimination half-life is 3-6 hours. Side effects are dyspepsia, agitation, tachycardia, hypotension, itching. Average dose for adults when taken orally is 250 mg 2-4 times a day.