Reviews & Comparisons
What is Meldonium?
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Meldonium, the active ingredient in Mildronate, is a synthetic analogue of
gamma-butyrobetaine
Gamma-Butyrobetaine
— A natural compound in the body involved in the synthesis of L-carnitine, which helps transport fatty acids into mitochondria for energy.
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, 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
Myocardial Metabolism
— The process by which the heart muscle (myocardium) produces energy to keep pumping efficiently.
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.
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
Oxidative Stress
— An imbalance of free radicals and antioxidants in the body that leads to cell damage.
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, minimizing cellular damage, and improving energy efficiency in the body.
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
Metabolism
— Metabolism is the set of chemical processes that convert food into energy and building blocks for the body.
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, prompting cells to use glucose more effectively, which is particularly beneficial in low-oxygen situations. Meldonium also alters how the body utilizes fatty acids, a mechanism somewhat comparable to how Phenibut or Noopept modulate neurotransmitter balance under stress.
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.
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.
Conclusion
While Meldonium is often associated with controversy in the world of sports, its original purpose lies in protecting cells from damage and maintaining healthy energy metabolism under stress. In clinical settings, it continues to be used as a supportive therapy for cardiovascular and neurological conditions. The debate around its classification highlights the fine line between medical support and performance enhancement, a reminder that even beneficial compounds can take on different meanings depending on their context and use. You can read more about Meldonium, its history, benefits & effects, sports scandals, and guidelines in our comprehensive review.
References
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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 “.
PubMed Central.
Link -
Gureev et al. (2021).
“Mildronate protects heart mtDNA from oxidative stress toxicity induced by exhaustive physical exercise “.
PubMed Central.
Link -
Di Cristo et al. (2019).
“Meldonium improves Huntington’s disease mitochondrial dysfunction by restoring peroxisome proliferator-activated receptor γ coactivator 1α expression “.
PubMed Central.
Link -
Schobersberger et al. (2016).
“Story behind meldonium-from pharmacology to performance enhancement: a narrative review “.
PubMed Central.
Link -
Dambrova et al. (2016).
“Pharmacological effects of meldonium: Biochemical mechanisms and biomarkers of cardiometabolic activity “.
PubMed Central.
Link -
Zhao et al. (2015).
“Single- and Multiple-dose Pharmacokinetic, Safety and Tolerability Study of Mildronate Injection in Healthy Chinese Subjects Pharmacokinetic of Mildronate Injection “.
PubMed Central.
Link -
Beitnere et al. (2014).
“Carnitine congener mildronate protects against stress and haloperidol-induced impairment in memory and brain protein expression in rats “.
PubMed Central.
Link
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