Meldonium

Products

Meldonium is on the market mainly in Eastern European countries and states of the former Soviet Union in the form of capsules and as an injectable, for example in Russia, Belarus, Ukraine, and Latvia (Mildronate). However, it is not registered in many countries, in the EU and in the USA. Meldonium was developed in the 1970s by Ivars Kalvins at the Institute of Organic Synthesis in Latvia.

Structure and properties

Meldonium (C6H14N2O2, Mr = 146.2 g/mol) is structurally closely related to carnitine and its precursor γ-butyrobetaine. It exists in the drug as meldonium dihydrate (- 2 H2O).

Effects

Meldonium (ATC C01EB22) has anti-ischemic properties. The effects are attributed to inhibition of carnitine biosynthesis by inhibition of the enzyme γ-butyrobetaine hydroxylase. As a result, meldonium reduces the breakdown of fatty acids in ischemic tissue (β-oxidation) and more glucose is consumed. As a result, fewer toxic intermediates are formed and less oxygen is consumed. In addition, other mechanisms play a role.

Indications

  • Cardiovascular disease: Angina pectoris, chronic heart failure, cardiomyopathy, myocardial infarction.
  • Physical and psychoemotional overload.
  • During the recovery period after cerebrovascular disease, head injury and encephalitis.
  • Other areas of application

Dosage

According to the SmPC. The drug can be administered perorally or parenterally. The capsules are usually taken once or twice daily.

Abuse

Meldonium can be abused as a doping agent and has been banned in professional sports since January 1, 2016. In March 2016, it became known that tennis player Mariya Sharapova tested positive during a doping control at the Australian Open. She had been taking the drug for ten years and was apparently unaware that it had been banned since the beginning of the year. In sports, meldonium can, among other things, boost endurance, improve recovery and enhance mental abilities. In addition to Mariya Sharapova, other athletes tested positive earlier this year.

Contraindications

  • Hypersensitivity
  • Hepatic and/or renal insufficiency
  • Pregnancy and lactation
  • Children under 18 years

Full precautions can be found in the drug label.

Adverse effects

The most common possible adverse effects include indigestion, hypersensitivity reactions, and headache.