- Also called:
- MET-88
meldonium
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What is meldonium?
Meldonium is a drug that protects against tissue damage caused by ischemia, a condition where blood flow is reduced, leading to decreased oxygen availability. Typically, it serves as a cardioprotective agent against ischemic damage to the heart and is used in treating certain neurological conditions related to ischemia. Marketed as Mildronate and Mildronāts, it is produced by the Latvian pharmaceutical company Grindeks.
Meldonium is considered a performance-enhancing drug and was added to the World Anti-Doping Agency's list of banned substances in January 2016. It gained notoriety when tennis player Maria Sharapova tested positive for it that year. It is believed to protect cells against the harmful effects of ischemia and potentially improve rehabilitation after exercise, though it is uncertain if it enhances athletic performance.
Reported side effects of meldonium include decreased blood pressure, dizziness, headache, increased heart rate, nervousness, and sleeplessness. Research on animals suggests potential long-term effects, such as increased anxiety and imbalances in the gut microbiome.
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What is meldonium used for?
Meldonium is a drug that protects against tissue damage caused by ischemia, a condition where blood flow is reduced, leading to decreased oxygen in tissues. It is commonly used as a cardioprotective agent for ischemic damage to the heart and to treat certain neurological conditions related to ischemia.
Meldonium is suspected to be a performance-enhancing drug and is therefore banned by the World Anti-Doping Agency since January 2016. It gained notoriety when Russian tennis player Maria Sharapova tested positive for it in March 2016. Meldonium may protect cells against the harmful effects of ischemia and potentially improve rehabilitation after exercise, though it is uncertain whether it enhances endurance or athletic performance. Side effects include decreased blood pressure, dizziness, headache, increased heart rate, nervousness, and sleeplessness.
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How does meldonium affect the body?
Meldonium blocks an enzyme called gamma-butyrobetaine dioxygenase (GBB), which reduces the production of carnitine. By blocking GBB and carnitine synthesis, meldonium decreases fatty acid metabolism, forcing cells to create energy through aerobic glucose metabolism and glycolysis. Because these pathways require less oxygen, meldonium helps restore the balance between the supply and demand of oxygen within cells affected by low-oxygen conditions.
Reported side effects of meldonium include decreased blood pressure, headache, dizziness, increased heart rate, nervousness, and sleeplessness. Research on animals also suggests that long-term use could potentially increase anxiety and cause an imbalance in gut microorganisms. Because it may protect cells against the detrimental effects of ischemia and potentially facilitate improved rehabilitation following exercise, meldonium is a suspected performance-enhancing drug with the potential for abuse by athletes.
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Why is meldonium sometimes used by athletes?
Meldonium is considered a performance-enhancing drug because it may protect cells from the harmful effects of ischemia and potentially improve rehabilitation after exercise. It is thought to restore the balance between oxygen demand and supply within cells affected by low-oxygen conditions by leveraging highly oxygen-efficient metabolic pathways.
Whether meldonium actually boosts endurance or provides other benefits to athletic performance remains uncertain. However, due to its potential for abuse, the World Anti-Doping Agency banned meldonium in January 2016.
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Is meldonium allowed in sports competitions?
Yes, meldonium is prohibited in sports competitions. The World Anti-Doping Agency added meldonium to its list of banned substances in January 2016, suspecting it to be a performance-enhancing drug. Several athletes, including Maria Sharapova and players from Russia's national under-18 hockey team, have tested positive for meldonium. Meldonium is believed to protect cells from the harmful effects of ischemia and potentially improve rehabilitation after exercise, though it is uncertain whether the drug increases endurance or otherwise benefits athletic performance.
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What are the possible side effects or risks of taking meldonium?
Meldonium is a drug primarily used to protect against tissue damage caused by ischemia, commonly used as a cardioprotective agent. Though it appears to have few side effects, some reported ones include decreased blood pressure, headache, increased heart rate, dizziness, nervousness, and sleeplessness. Animal research suggests long-term use could potentially increase anxiety and cause an imbalance in the gut microbiome.
Meldonium is considered a performance-enhancing drug and is banned by the World Anti-Doping Agency since 2016. Though suspected of improving rehabilitation and protecting cells against ischemia, it's uncertain whether it increases endurance or benefits athletic performance.
1 Britannica SourceCreated from Britannica articles using AI. AI can make mistakes, so verify using Britannica articles.
meldonium, drug used to protect against tissue damage caused by ischemia—a reduction in blood flow to a part of the body, resulting in decreased oxygen availability in affected tissues. Meldonium is typically used as a cardioprotective agent to defend against ischemic damage to the heart and in the treatment of certain neurological conditions involving ischemia. Meldonium is marketed under the trade names Mildronate and Mildronāts and is manufactured and sold by the Latvian pharmaceutical company Grindeks.
Discovery and uses
Meldonium was designed in the 1970s by Ivars Kalvins, a scientist at the Latvian Institute of Organic Synthesis. At the time, the drug was under investigation for its ability to promote growth in animals. The following decade, it was given to Soviet soldiers who were fighting in Afghanistan to help increase their stamina at high altitude. Meldonium was later registered for use in the treatment of coronary heart disease, angina pectoris (chest pain), and cerebrovascular disease in Russia as well as in various other republics that were then part of the Soviet Union, including Azerbaijan, Belarus, Georgia, Kazakhstan, Kyrgyzstan, Moldova, Ukraine, and Uzbekistan.
Mechanism of action
Meldonium exerts its effects by blocking the actions of an enzyme known as gamma-butyrobetaine dioxygenase (GBB). GBB is involved in the production of carnitine, a vitamin-like substance that is closely related to the amino acids and that serves an important role in the transport of long-chain fatty acids for energy metabolism. However, fatty acid transport and oxidation is highly demanding in terms of oxygen consumption, and, in the presence of oxygen deficiency, toxic intermediate compounds formed during fatty acid metabolism accumulate within cells.
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By blocking GBB and carnitine synthesis, meldonium causes a decrease in fatty acid metabolism. That forces cells to generate energy through such pathways as aerobic glucose metabolism and glycolysis, which require significantly less oxygen to generate energy in the form of adenosine triphosphate (ATP). Thus, overall, compared with fatty acid oxidation, glucose metabolism and glycolysis generate more ATP per molecule of oxygen. In leveraging highly oxygen-efficient metabolic pathways, meldonium is thought to help restore the balance between demand and supply of oxygen within cells that are affected by low-oxygen conditions, such as those associated with ischemia or exposure to high altitude.
Use in athletes
Meldonium is a suspected performance-enhancing drug, with potential for abuse by athletes. In January 2016 it was added to the World Anti-Doping Agency list of banned substances, owing to its widespread use in athletes from Russia and eastern European countries, where the drug is readily available. The drug gained particular notoriety in March 2016 after Russian tennis player Maria Sharapova announced that she had tested positive for it earlier in the year at the Australian Open. That same year, players on the Russian national under-18 hockey team tested positive for meldonium prior to the ice hockey U18 World Championships. For the competition, the entire team was replaced with players from the country’s under-17 roster.
Meldonium is suspected of enhancing athletic performance through its ability to protect cells against detrimental effects of ischemia and potentially facilitate improved rehabilitation following exercise. However, whether the drug actually increases endurance or otherwise benefits athletic performance is uncertain.
Side effects
Meldonium appears to have few side effects. Those that have been reported include decreased blood pressure, dizziness, headache, increased heart rate, nervousness, and sleeplessness. Research in animals suggests that long-term treatment with meldonium potentially increases behaviors linked to anxiety and causes an imbalance in the types of microorganisms that constitute the gut microbiome.
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