MELDONIUM, aka: Mildronate, has been around since 2005 and is produced by a Latvian Pharmaceutical Company. WADA (World Anti-Doping Agency) made it a banned substance effective January 1st, 2016. Maria Sharapova admitted in her press conference today that she has been using it for ten years and tested positive at the Australian Open earlier this year.
Meldonium is an anti-ischemic agent, whose mechanism of action is to inhibit fatty acid oxidation by inhibiting y-butyrobetaine hydroxylase which is necessary for the biosynthesis of carnitine. Meldonium also regulates energy metabolism by its ability to bind carnitine acetyltransferase and is considered a central nervous system stimulant; restores balance between oxygen delivery and consumption; and it causes vasodilatation, which improves blood flow to tissues which in turn improves oxygen delivery.
What is carnitine? An amino acid derivative and nutrient involved in fat metabolism.
Ischemia is decreased or inadequate oxygenation in tissues; thus, this drug increases oxygenation, thereby enhancing one’s performance or exercise capacity; in other words it can be used as a performance-endurance enhancer for athletes.
This drug was initially manufactured to treat patients suffering from coronary artery disease who suffer from angina (chest pain caused by poor blood flow to the heart) or has had a myocardial infarction (heart attack). It also is used for treatment of patients who have ischemic cerebrovascular disorders.
From my research, this drug has amazing benefits for life-threatening medical conditions and the potential for abuse by people wanting to enhance their athletic performance. The drug insert clearly states that “Meldonium positively affects energetic metabolism and moderately activates the central nervous system”; thus, anyone using it other than for it’s anti-ischemic properties, must have known they were using a drug that was giving them an unfair advantage.
- excessive CNS stimulation (agitation)
- headache, dizziness, increased heart rate (due to drop in blood pressure)
- allergic skin reactions- skin redness, urticarial, itching, edema an eosinophilia
- Why did WADA decide to ban the substance this year?
- Sharapova has been using it for ten years, hasn’t she had an unfair advantage against her opponents?
- Whether the drug was legal last year and illegal this year, is anyone concerned about the ethics displayed?
- Did Sharapova know of the performance enhancing benefits?
Drug Testing and Analysis vol.7, Issue 11-12, pgs. 973-979, Nov-Dec 2015