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Meldonium

Meldonium
Meldonium.svg
Clinical data
Trade names Mildronate, Mildronāts
ATC code
Legal status
Legal status
  • US: Unscheduled
Identifiers
Synonyms THP, MET-8 Mildronāts or Quaterine
CAS Number
PubChem CID
ChemSpider
UNII
ChEBI
ECHA InfoCard 100.224.143
Chemical and physical data
Formula C6H14N2O2
Molar mass 147.19 g/mol
3D model (Jmol)
Solubility in water >40 mg/mL mg/mL (20 °C)

Meldonium (INN), trade-named as Mildronate among others, is a limited-market pharmaceutical, developed in 1970 by Ivars Kalviņš, Latvian Institute of Organic Synthesis (USSR), and manufactured primarily by Grindeks of Latvia and several generic manufacturers. It is distributed in Eastern European countries as an anti-ischemia medication.

Since 1 January 2016, it has been on the World Anti-Doping Agency (WADA) list of substances banned from use by athletes. However, there are debates over its use as an athletic performance enhancer. Some athletes are known to have been using it before it was banned. It is currently unscheduled in the US.

Don Catlin, a long-time anti-doping expert and the scientific director of the Banned Substances Control Group (BSCG) said “There’s really no evidence that there’s any performance enhancement from meldonium - Zero percent.”

Meldonium may be used to treat coronary artery disease. These heart problems may sometimes lead to ischemia, a condition where too little blood flows to the organs in the body, especially the heart. Because this drug is thought to expand the arteries, it helps to increase the blood flow as well as increase the flow of oxygen throughout the body. Meldonium has also been found to induce anticonvulsant and antihypnotic effects involving alpha 2-adrenergic receptors as well as nitric oxide-dependent mechanisms. This, in summary, shows that meldonium given in acute doses could be beneficial for the treatment of seizures and alcohol intoxication. It is also used in cases of cerebral ischemia, ocular ischemic syndrome and other ocular disease caused by disturbed arterial circulation and may also have some effect on decreasing the severity of withdrawal symptoms caused by the cessation of chronic alcohol use.

Meldonium is believed to exert its cardioprotective effects through its ability to cause vasodilation in the coronary arteries via increased nitric oxide synthesis, reducing blood glucose concentrations through increased oxidation of glucose and also by preconditioning the heart to handle ischaemic situations, among other effects. It also has been implicated in the use of cerebral ischaemia. This is all done through its inhibition of carnitine synthesis.


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