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Meldonium – Effects, Uses and Doping

Meldonium is a drug originally developed to treat heart conditions. It affects fat metabolism and has been misused as a performance-enhancing substance in sports.

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Things worth knowing about "Meldonium"

Meldonium is a drug originally developed to treat heart conditions. It affects fat metabolism and has been misused as a performance-enhancing substance in sports.

What is Meldonium?

Meldonium (also known by the brand name Mildronate) is a synthetically produced compound originally developed in the Soviet Union. It belongs to the class of cardioprotective substances and is primarily used in Eastern Europe to treat heart disease and support cardiac function. Internationally, it became widely known after being added to the World Anti-Doping Agency (WADA) prohibited list in 2016.

Indications

In countries where it is approved -- primarily Russia and the Baltic states -- meldonium is used for the following medical indications:

Treatment of coronary artery disease (angina pectoris)
Support for patients with heart failure
Management of stroke and cerebral circulation disorders
Treatment of diabetic complications such as retinopathy
Recovery support in cases of physical exhaustion (in select countries)

Meldonium is not approved as a pharmaceutical drug in Germany, the European Union, or the United States.

Mechanism of Action

Meldonium inhibits the enzyme gamma-butyrobetaine hydroxylase, which plays a key role in the biosynthesis of carnitine. Carnitine is an essential transport molecule that carries long-chain fatty acids into the mitochondria, where they are oxidized to produce energy.

By inhibiting carnitine biosynthesis, meldonium causes:

A reduction in carnitine levels in tissue
A shift in energy metabolism from fatty acid oxidation toward glycolysis (glucose metabolism)
Reduced accumulation of toxic by-products from incomplete fatty acid oxidation during oxygen deprivation (ischemia)

This mechanism is thought to protect cardiac tissue during conditions of reduced oxygen supply -- a property referred to as cardioprotection.

Dosage and Administration

In clinical studies and medical practice, the following dosages have been used:

Oral: 500 mg to 1000 mg per day, divided into 1-2 doses
Intravenous: 500 mg per day in acute settings
Typical treatment duration: 4 to 6 weeks, depending on the indication

Since meldonium is not approved in many countries, it should only be used under medical supervision and only where it is legally available.

Side Effects

Meldonium is generally considered well tolerated; however, the following side effects may occur:

Gastrointestinal complaints (nausea, abdominal pain)
Headache and dizziness
Low blood pressure (hypotension)
Allergic reactions (rare)
Increased heart rate (tachycardia, rare)

Meldonium in Sports and Doping

Since January 1, 2016, meldonium has been included on the WADA Prohibited List, as it is suspected of enhancing athletic performance. Proposed performance-enhancing effects include:

Improved endurance performance through optimized energy supply
Faster recovery after intense physical activity
Potential protective effects on muscle cells during exertion

Several high-performance athletes, including tennis player Maria Sharapova, received bans following positive tests for meldonium. However, the scientific evidence for a genuine performance-enhancing effect in healthy athletes is not yet conclusively established.

Legal Status

Meldonium is not approved as a pharmaceutical drug in Germany, Austria, Switzerland, or most EU countries. It is available by prescription in Russia, Latvia, and some other Eastern European nations. Possession or use without a valid prescription may carry legal consequences depending on the jurisdiction.

References

Dambrova M. et al. - Pharmacological effects of meldonium: Biochemical mechanisms and biomarkers of cardiometabolic activity. Pharmacological Research, 2016.
World Anti-Doping Agency (WADA) - Prohibited List 2016, www.wada-ama.org
Schobersberger W. et al. - Meldonium use in sports: A review of the current evidence. Sports Medicine, 2017.

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