What Is Meldonium?

Meldonium, the active ingredient in Mildronate, is a synthetic analogue of gamma-butyrobetaine, a compound naturally occurring in all human cells. According to the official drug information, Meldonium functions by preventing the accumulation of activated forms of unoxidized fatty acids in cells and by normalizing myocardial metabolism.

It helps restore the balance between oxygen delivery and its consumption in cells. It also enhances glycolysis without increasing oxygen demand, thereby reducing oxidative stress, minimizing cellular damage, and improving energy efficiency in the body. For a detailed review of Meldonium, please refer to our comprehensive review.

What Does Meldonium Do?

Meldonium is a protective agent that supports cells during stressful conditions and oxygen deprivation, such as ischemia. As the active ingredient in Mildronate, it shares a chemical structure similar to a specific amino acid and has long been utilized in the treatment of heart and brain conditions linked to restricted blood flow.

Meldonium works by reducing the levels of L-carnitine, which impacts how cells process fats. This prevents the accumulation of harmful byproducts and minimizes damage to cellular structures. Also, Meldonium enhances the ability of red blood cells to transport oxygen.Furthermore, Meldonium alters cellular energy metabolism, prompting cells to use glucose more effectively, particularly beneficial in low-oxygen situations.

To sum up:

• Meldonium helps cells use energy more efficiently under stress.
• Meldonium can balance the amount of oxygen cells need and receive.
• It prevents harmful metabolic by-products from building up in cells, thus protecting them from damage.

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Why Is Meldonium Banned In Sports?

Starting from January 1, 2016, Meldonium has been classified as a banned substance by the World Anti-Doping Agency (WADA) due to its documented use by athletes. One of the most prominent doping scandals related to Meldonium occurred in the case involving Maria Sharapova.

The renowned Russian tennis player acknowledged using Mildronate for several years, leading to her suspension from competition following an investigation.

Professor Kalvins, the creator of Meldonium, countered doping accusations by stating that the drug was designed solely as a cardioprotective agent to safeguard athletes’ cardiovascular systems under high physical stress, emphasizing it does not enhance performance beyond normal limits unlike doping substances.

Bibliography

1. Beitnere et al (2014) Carnitine congener mildronate protects against stress and haloperidol-induced impairment in memory and brain protein expression in rats https://www.ncbi.nlm.nih.gov/pubmed/25446926
2. Zhao et al (2015) Single- and Multiple-dose Pharmacokinetic, Safety and Tolerability Study of Mildronate Injection in Healthy Chinese Subjects Pharmacokinetic of Mildronate Injection https://www.ncbi.nlm.nih.gov/pubmed/26697890
3. Dambrova et al (2016) Pharmacological effects of meldonium: Biochemical mechanisms and biomarkers of cardiometabolic activity https://pubmed.ncbi.nlm.nih.gov/26850121/
4. Schobersberger et al (2016) Story behind meldonium-from pharmacology to performance enhancement: a narrative review https://pubmed.ncbi.nlm.nih.gov/27465696/
5. Di Cristo et al (2019) Meldonium improves Huntington’s disease mitochondrial dysfunction by restoring peroxisome proliferator-activated receptor γ coactivator 1α expression https://pubmed.ncbi.nlm.nih.gov/30362565/ 
6. Gureev et al (2021) Mildronate protects heart mtDNA from oxidative stress toxicity induced by exhaustive physical exercise https://pubmed.ncbi.nlm.nih.gov/33930377/
7. Savic et al (2021) Hyperpolarized magnetic resonance shows that the anti-ischemic drug meldonium leads to increased flux through pyruvate dehydrogenase in vivo resulting in improved post-ischemic function in the diabetic heart https://pubmed.ncbi.nlm.nih.gov/33458907/
8. Vilskersts et al (2021) Protective Effects of Meldonium in Experimental Models of Cardiovascular Complications with a Potential Application in COVID-19 https://pubmed.ncbi.nlm.nih.gov/35008470/