Meldonium (mildronate; 3-(2,2,2-trimethylhydrazinium) propionate; THP; MET-88) is a clinically used cardioprotective drug, which 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.
Mildronate is the leading agent of the cardiovascular group,antiischemic agent of a metabolic action:
- Acts as antiischemic cell protector in patients with angina pectoris, chronic heart failure, brain circulation disorders.
- Improves physical capacity and mental function in the case of ischemia and in healhty people.
Due to its unique mechanism of action Mildronate, depending on the prescribed dose, is widely used for the treatment of different heart and vascular diseases, as well as for the improvement of work capacity of healthy people at physical and mental overloads and during rehabilitation period.
- Improves Mental Processes (Memory, Learning, Focus, Concentration, Processing of Information)
- Reduces Fatigue, Increases Motivation & Alertness
- Improves Athletic Training & Competitive Performance
- Improves Microcirculation & Oxygen Delivery
Since January 1, 2016, it has been on the World Anti-Doping Agency (WADA) list of substances banned from use by athletes; some athletes are known to have been using it before it was banned.
On March 7, 2016, former world number one tennis player Maria Sharapova announced that she had failed a drug test in Australia due to the detection of meldonium. She said that she had been taking the drug for ten years for various health issues, and had not noticed that it had been banned. Earlier the same day, Russian ice dancer Ekaterina Bobrova announced she had also tested positive for meldonium at the 2016 European Figure Skating Championships.
Other athletes who are provisionally banned for using meldonium include Swedish Ethiopian-born middle-distance runner Abeba Aregawi, Ethiopian long-distance runner Endeshaw Negesse, Russian cyclist Eduard Vorganov, and Ukrainian biathletes Olga Abramova and Artem Tyshchenko.