Meldonium (Mildronate): What is it and What does it do?

In light of recent media attention surrounding meldonium and its detection in elite athletes, we thought it best to share reliable information about the drug, its intended purpose, and potential use as a performance-enhancing substance.

Blog Article Contributed by Eric Smith, PharmD.

Expert Consultant for the Resource Exchange Center (REC), Powered by Drug Free Sport™

The World Anti-Doping Agency (WADA) added meldonium (Mildronate) to their 2016 Prohibited List in late September 2015. This modification—among others­­—went into effect January 1, 2016. WADA added meldonium as a prohibited substance due to “evidence of its use by athletes with the intention of enhancing performance.”

A Latvian pharmaceutical company with primary distribution in Eastern Europe and Russia manufactures meldonium under the brand name Mildronate. In the 1970s, Mildronate was developed to promote the growth of livestock. Currently, the drug is marketed to treat a variety of medical conditions including ischemic heart disease, heart failure, stroke, peripheral artery disease, and alcohol withdrawal.  Also indicated for use in healthy individuals experiencing physical and mental stress, Mildronate targets athletes as well.

Recent studies identified Mildronate as having anti-ischemic properties. Ischemia is a medical term used to describe a decrease in blood supply to certain parts of the body. A reduction in blood circulation minimizes the delivery and availability of oxygen and sugars needed by the body’s cells. Having anti-ischemic properties makes Mildronate beneficial for treating situations associated with decreased blood supply.   

The drug primarily functions to increase oxygen efficiency in certain body tissues. This makes sense when you reconsider that decreased blood supply (ischemia) reduces oxygen delivery to the tissues. Mildronate works to optimize energy production by interfering with energy pathways that use more oxygen (less efficient) and alternatively promoting pathways that use less oxygen (more efficient).

Mildronate achieves this by blocking pathways involved in carnitine production. Carnitine is an amino acid derivative used in the process of breaking fats down into fatty acids and converting them into energy.  Mildronate creates lower levels of carnitine thereby reducing the body’s ability to breakdown fats for energy.

The body adjusts by increasing the use of an alternative energy pathway called glycolysis.  Glycolysis is more efficient than fatty acid metabolism because it not only uses less oxygen, but also decreases the amount of toxins (such as lactic acid) that build up in cells during energy production.

For athletes, taking this medication could potentially increase muscle and nervous system oxygen efficiency. Using oxygen more effectively in working tissues may lead to performance enhancing benefits such as improved exercise tolerance, improved recovery, stress protection, and improved central nervous system functions. 

Isn’t biochemistry and pharmacology fun?

Mildronate is not approved by the Food and Drug Administration (FDA) for sale in the United States.