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.
