Meldonium (Mildronate): What Is It And What Does It Do?

Meldonium, brand name Mildronate, is the basis of much debate in the world of sports doping. Initially designed in Latvia for use in animals, the drug is now under the watchful eye of the World Anti-Doping Agency.
Meldonium, also known as Mildronāts, Quaterine, MET-88, THP, trimethylhydrazinium propionate and 3-(2,2,2-trimethylhydraziniumyl)propionate, is primarily manufactured by a Latvian drug company called Grindeks.
It is a licensed medical drug used widely throughout Eastern Europe and Central Asia for a number of conditions, including cardiac complaints. Meldonium is not licensed for use in the US.
Since January 1, 2016, meldonium has been on the World Anti-Doping Agency's list of banned drugs. A number of athletes from America, Russia and Europe are currently facing bans for using meldonium.¹
In this article, we will look at the origins of meldonium, its medical uses and associated research.

Fast facts on meldonium (Mildronate)
Here are some key points about meldonium. More detail and supporting information is in the main article.

• A Latvian pharmaceutical company created meldonium
• Meldonium is a fatty acid oxidation inhibitor
• Use of meldonium in sports is banned by the World Anti-Doping Agency (WADA)
• As of April 2016, at least nine athletes have been provisionally suspended after testing positive for meldonium
• Meldonium is predominantly used to treat heart conditions but has a range of pharmaceutical uses
• Meldonium is not licensed for use in the US
• The drug was used extensively by Soviet troops in Afghanistan.

What is meldonium (Mildronate)?

Meldonium has a number of uses, one of which being performance enhancement.

One of meldonium's early uses was in animals; the drug was specifically used to enhance the sexual performance and sperm motility of boars. Its license was later expanded for use in humans.²
Meldonium is produced by the Latvian pharmaceutical company Grendiks. With sales of the drug reaching 56 million euros in 2013, it is one of Latvia's biggest medical exports.
Prior to the use of meldonium for cardiac health issues, large quantities of the drug were shipped to Soviet troops in Afghanistan between 1979 and 1989.
According to the drug's designer, Ivar Kalvins - chair of the scientific board of the Latvian Institute of Organic Synthesis - it was created to increase the body's oxygen-carrying capacity.
Because of Afghanistan's mountainous terrain and the need to carry large backpacks, Soviet soldiers would take meldonium to increase their endurance in the oxygen-reduced air.

Uses of meldonium (Mildronate)

Meldonium is a fatty acid oxidation inhibitor and, today, it is principally used to treat angina and heart attacks (myocardial infarction). Its therapeutic activity is produced by altering pathways for carnitine, a nutrient involved in fat metabolism.³
A study in 2005 found that meldonium, in combination with an angiotensin-converting enzyme inhibitor called lisinopril, improved exercise capability and peripheral circulation for individuals with chronic heart failure.⁴
A Chinese study group then tested meldonium for its efficacy in treating acute ischemic stroke, finding it as useful as cinepazide, a vasodilator commonly used to treat acute cerebral infarction.⁵
In some countries, including Latvia, Russia, Ukraine, Georgia, Kazakhstan, Azerbaijan, Belarus, Uzbekistan, Moldova and Kyrgyzstan, meldonium is used to treat problems with circulation in the brain and has been reported to elevate mood and improve motor symptoms, dizziness and nausea. Meldonium has also been found to help reduce withdrawal symptoms in people with alcoholism.
Other uses for meldonium include:⁶

• Immune system modulation
• Treating stomach ulcers
• Treating eye trauma
• Treating infections of the lungs and upper respiratory tract.

Meldonium (Mildronate) in sports

Meldonium has recently been added to WADA's list of banned substances because of "evidence of its use by athletes with the intention of enhancing performance." WADA classes meldonium as a metabolic modulator, in the same bracket as insulin.⁷
A study published in Drug Testing and Analysis in December 2015 summarized that meldonium:

"Demonstrates an increase in endurance performance of athletes, improved rehabilitation after exercise, protection against stress, and enhanced activations of central nervous system (CNS) functions."⁸

Meldonium hit the headlines in 2016 thanks to the former world number one tennis player - Maria Sharapova - who tested positive for the substance on March 7, 2016. Although she contested that she had been taking meldonium for 10 years to treat an ongoing medical issue, she was provisionally suspended.
On the same day that Sharapova's results became public, Russian ice skater Ekaterina Bobrova also announced that she had tested positive for the drug. Since then, at least another nine sportspeople from Russia, Ethiopia, Sweden, Germany and Ukraine have received provisional bans after positive tests for meldonium.
However, on April 13, 2016, WADA advised that any athletes who tested positive before March 1, 2016 could still compete. The change in decision came because reliable data on how long the body takes to excrete meldonium does not yet exist.^{9
Source- medicalnewstoday}