Meldonium, Tennis Star Maria Sharapova’s Performance-enhancing Drug Explained

Tennis star Maria Sharapova has admitted to using the performance-enhancing drug meldonium, which boosts brain and body power and endurance. Here’s how it works.

Sharapova

Meldonium was developed for the Soviet military and given to Soviet soldiers in the Afghanistan invasion. The drug increases endurance for physically and cognitively demanding tasks when the body is under physiological stress. Also known as mildronate, the drug has since been used for various medical purposes, notably for treating cardiac conditions and diabetes, but also for many neurological disorders including stroke, Parkinson’s, Alzheimer’s disease, and others. The drug is not available for use in the United States.

 

Meldonium works like an octane booster in gasoline to increase the power produced by the body’s metabolic machinery inside the mitochondria of cells.   Mitochondria produce cellular energy by a metabolizing the sugar, glucose, in a reaction that requires many steps and produces a sequence of intermediate products and byproducts to ultimately synthesize the high-energy phosphate bonds in ATP–the fundamental fuel for all cells in the body.

 

One of the important molecules in cellular metabolism is L-carnitine, which is required for transporting molecules, called fatty acids, into the mitochondria of cells. Meldonium lowers the amount of L-carnitine in cells. The cells respond to this by increasing other molecules on the membrane of mitochondria that suck L-carnitine into the organelles (carnitine palmitoyltransferase-1) and also by several other metabolic changes to compensate for the lower levels of L-carnitine. Another effect of melodium is to stimulate insulin-dependent glucose uptake into cells, which makes the drug useful as an anti-diabetic medication.

 

The result of these compensatory cellular responses is that, melodium protects mitochondria from being damaged under conditions of cellular stress, notably when oxygen, glucose, or blood flow are reduced. Extreme physical activity (for example marching with heavy packs in an army, climbing mountains, or competing at world-class level in tennis) depletes the blood of glucose and oxygen, and the performance of muscles, neurons, and other cells suffers, like a sputtering racecar running out of gas. Chronic physiological stress can lead to wide-spread cellular injury or death of many types of cells.

 

Such a fundamental effect on cellular metabolism from meldonium will have a wide range of effects including many effects on the brain. In studies on laboratory animals, meldonium has been shown to protect neurons from death caused by lack of oxygen, reduced blood flow, and certain neurotoxic substances. For example in a rat model of Parkinson’s disease, melodium protected neurons from death (Klusa et al., 2013). Cognitive enhancement by melodium has been shown in studies of learning and memory in rodents (Klusa et al., 2013; Beitnere et al., 2014), and the compound has been suggested as potentially useful to enhance cognition in patients with neurodegenerative diseases that result in dementia.

 

Sharapova denies taking the drug to cheat in competitive tennis. Meldonium was only banned as a performance-enhancing drug in January, 2016, but Sharapova states that she has taken the drug for a decade because of a family history of diabetes.

 

References

Beitnere, U., et al., (2014) Carnitine congener mildronate protects against stress- and haloperidol-induced impairment in memory and brain protein expression in rats. Eur. J. Pharmacol. 745: 76-83.

Birnbaum, M. Drug linked to Sharapova rooted in Soviet military, The Washington Post, March 9 2016

Dambrova, M., et al., (2016) Pharmacological effects of meldonium: Biochemical mechanisms and biomarkers of cardiometabolic activity. Pharmacological Research, on-line in advance of print. Doi 10.1016/j.phrs.2016.01.019.

Klusa, V. (2013) Mildronate enhances learning/memory and changes hippocampal protein expression in trained rats. Pharmacol. Biochem. Behav. 106: 68-76.

 

Photocredit: Justin Smith https://www.flickr.com/photos/reefoto-com/3660393408

 

 

 

 

This entry was posted in by Douglas Fields, Chemicals, Diet and Exercise, Diseases & Disorders, In Society, Injury, Learning and Memory, Neuroethics, Stress and Anxiety, Uncategorized and tagged , , , , , , , , , ,
The Society for Neuroscience and its partners are not responsible for the opinions and information posted on this site by others.
Douglas Fields

About Douglas Fields

R. Douglas Fields is Chief of the Nervous System Development and Plasticity Section at the National Institutes of Health, NICHD, in Bethesda, Maryland, and author of the new book about sudden anger and aggression “Why We Snap,” published by Dutton, and a popular book about glia “The Other Brain” published by Simon and Schuster. Dr. Fields is a developmental neurobiologist with a long-standing interest in brain development and plasticity, neuron-glia interactions, and the cellular mechanism of memory. He received degrees from UC Berkeley, San Jose State University, and UC San Diego. After postdoctoral fellowships at Stanford and Yale Universities he joined the NIH in 1987. Dr. Fields also enjoys writing about neuroscience for the general public. In addition to serving on editorial boards of several neuroscience journals, he serves as scientific advisor for Odyssey and Scientific American Mind magazines. He has written for Outside Magazine, The Washington Post Magazine, Scientific American and Scientific American Mind, and he publishes regularly for The Huffington Post, Psychology Today, and Scientific American on-line. Outside the lab he enjoys building guitars and rock climbing.

The opinions stated in the blog are the personal opinion of the author and not those of the federal government.

Leave a Comment