Meldonium, What was a Tennis Star, Maria S actually taking?

Mildronate was originally developed in the 1970’s in Latvia as a growth-promoting agent in animals. More recently it was discovered that it is also an anti-ischemic (prevent loss of blood flow) medication, which has cardioprotective effects. It has also been used for the treatment of neurodegenerative and bronchopulmonary disorders. Mildronate works by its effects on modulating the carnitine metabolism in the myocardium, the muscle cells of the heart.  Carnitine is the key molecule in the regulation of the cellular use of fatty acids for energy. Mildronate inhibits the synthesis of carnitine and also inhibits its entry into various cells in the body. This is the aspect that athletes may utilize to gain an edge in competition.

Under conditions of oxygen deficiency, when an athlete is exercising under anaerobic conditions and fatty acids start to be used for fuel, then metabolites can build up in the cells because there is a lack of oxygen to the cells; and these metabolites can be toxic to the cells. However, if an athlete takes Mildronate it will lead to less carnitine inside of the muscle cells. This will cause a decrease in fatty acid metabolism, and lessen subsequent cytotoxic metabolic accumulation, and will enhance glycolysis, which is the way the body uses sugar for fuel. For an athlete this can be of benefit because it can prepare the cells of the body to survive during times of ischemic stress, like an elite competitor may put their body through during competition.

There have been reports that the use of Mildronate does have positive effects on the athletic performance of elite athletes. So how exactly does it cause increased capabilities in athletes? Mildronate causes a decreased use of fatty acids by the cells and increases the use of sugar for fuel; in this way the cells optimize the use of oxygen that is available to them and can work better under ischemic conditions. It can also spare the use of glycogen (storage form of sugar) in the cell during prolonged exercise conditions. Therefore, the endurance capabilities of the athletes are improved; essentially this potentially allows them to work harder for longer.

Mildronate has also been shown to increase learning and boost memory performance. These are two other properties that can be beneficial to the elite athlete to help gain a competitive advantage.

So is there an actual medical use for Mildronate? In short, yes. Although the medication has not been approved by the FDA for medical use in the United States of America, other countries do use it (primarily Eastern Europe and Russia). In those countries it is used for treatment after heart attacks and for patients with stable angina (chronic chest pain related to the heart) for improvement of exercise tolerance. It has been proven to improve systolic function (how well the heart beats) and peripheral blood circulation. This has resulted in increased stress tolerance, reduced chest pain symptoms, and improved quality of life.

 

Chase King, MS-IV

David Carfagno, D.O., C.A.Q.S.M.

 

Resources:

Dambrova, M. "Mildronate Cardioprotective Action through Carnitine-Lowering Effect." Trends in Cardiovascular Medicine 12.6 (2002): 275-79. Web.

Dzerve, Vilnis. "A Dose-Dependent Improvement in Exercise Tolerance in Patients With Stable Angina Treated With Mildronate: A Clinical Trial “MILSS I”." Medicina (Kaunas) 47.10 (2011): 544-51. Research Institute of Cardiology, University of Latvia, Riga, Latvia. Web.

Dzintare, Maija, and Ivars Kalvins. "MILDRONATE INCREASES AEROBIC CAPABILITIES OF ATHLETES THROUGH CARNITINE-LOWERING EFFECT." 5th Baltic Sport Science Conference. Baltic Sport Science Society. N.p., Apr. 2012. Web.

Görgens, Christian, Sven Guddat, Josef Dib, Hans Geyer, Wilhelm Schänzer, and Mario Thevis. "Mildronate (Meldonium) in Professional Sports - Monitoring Doping Control Urine Samples Using Hydrophilic Interaction Liquid Chromatography - High Resolution/high Accuracy Mass Spectrometry." Drug Test. Analysis Drug Testing and Analysis 7.11-12 (2015): 973-79. Web.

Image 1 Credit: http://en.mercopress.com/data/cache/noticias/54403/0x0/mildronats-meldon...

Image 2 Credit: https://i.guim.co.uk/img/static/sys-images/Guardian/Pix/audio/video/2016...

 

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