Thursday, March 10, 2016

Sharapova and a Crime of Intent

Meldonium is also known as mildronate. It is manufactured in Latvia and only distributed in Baltic countries and Russia. It is said that Meldonium is used to treat ischemia: a lack of blood flow to parts of the body, particularly in cases of angina or heart failure. It works by dilating blood vessels and increasing blood flow, which in turn improves exercise capacity, physical and mental endurance, and also brain function.

Now that is quite a claim. Such a drug would have a lot of applications in many of the problems that are a function of poor blood flow. But surprisingly it is used only in the Eastern Block. Perhaps it will soon be coming to a Mexican clinic near you.
The World Anti-Doping Agency  found "evidence of its use by athletes with the intention of enhancing performance" by virtue of carrying more oxygen to muscle tissue.
L'Equipe reported that the scientific advisor to the French Agency Against Doping (AFLD), Professor Xavier Bigard, said in interviews with athletes at last year's European Games in Baku that a wide proportion of athletes admitted taking meldonium.
The drug was name-checked in the latest investigative documentary on Russian doping reforms by the German Hajo Seppelt. The documentary referred to a 2015 study in which 17% of Russian athletes (724 of 4,316) tested were found to have meldonium in their system. A global study found 2.2% of athletes had it in their system.
Several athletes have been suspended since the turn of 2016 after testing positive for the drug. Abebe Aregawi, the 2013 women's 1,500m world champion, has been provisionally suspended after meldonium was found in a sample she provided. Endeshaw Negesse, the 2015 Tokyo marathon champion, was also banned after reportedly testing positive for the same substance. Others include Olga Abramova and Artem Tyschcenko, two Ukrainian biathletes, Eduard Vorganov, a Russian cyclist and Ekaterina Bobrova, a Russian ice dancer.

But just because people use it does not mean it works.  has a summary of the drug's claims and purported mechanism of action.
The mechanism of action is based on the regulation of energy metabolism pathways through l-carnitine lowering effect. l-Carnitine biosynthesis enzyme γ-butyrobetaine hydroxylase and carnitine/organic cation transporter type 2 (OCTN2) are the main known drug targets of meldonium, and through inhibition of these activities meldonium induces adaptive changes in the cellular energy homeostasis. Since l-carnitine is involved in the metabolism of fatty acids, the decline in its levels stimulates glucose metabolism and decreases concentrations of l-carnitine related metabolites, such as long-chain acylcarnitines and trimethylamine-N-oxide.
Image for unlabelled figure

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