Meldonium: What does the drug Maria Sharapova just got busted for do to an athlete’s body?

Sick or tired?
Sick or tired?
Image: AP Photo/Damian Dovarganes
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International tennis star Maria Sharapova announced Monday that she tested positive for a drug called Meldonium that was added to the World Anti-Doping Agency’s list of banned drugs on January 1, 2016.

The drug, known commercially as Mildronate, was developed by the Latvian Institute of Organic Synthesis in the 1980s and is manufactured and marketed by Latvian company Grindeks today. It is primarily used to treat people with heart conditions that affect the blood’s ability to deliver oxygen to the body. As it happens, oxygen delivery is key to an athlete’s performance, too.

Here’s what Meldonium does:

It reduces the amount of oxygen needed to keep tissues alive by changing the way muscle cells metabolize various substances in the blood. Typically, long-chain fatty acids enter cell mitochondria, which is where the metabolic process occurs. Meldonium blocks this action, instead sending carbohydrates to the mitochondria.

Metabolizing carbs requires less oxygen than metabolizing fatty acids, so giving the mitochondria carbs instead of fatty acids can keep cells alive when there’s not enough oxygen in the blood.  This can save lives when poor circulation reduces blood supply and oxygen to tissues. For the same reason, reducing the need for oxygen can enhance athletic performance. 

When we push our bodies to their limits, those limits are largely set by our blood’s ability to deliver oxygen to our cells. Over the course of a workout, as our bodies use oxygen, our blood becomes oxygen deficient—because we’re using up oxygen at a faster rate than our lungs can replace it.

Not so if you’re Maria Sharapova on Meldonium. Her blood stays oxygen-rich longer, allowing her to perform longer in practice and in matches. And because the drug changes the actual substance that is metabolized in the body, it changes the way Sharapova feels after a workout, too. Less lactate and urea—the two cellular byproducts of burning fatty acids that make your muscles feel stiff after a run—are produced in ischemic metabolization, so Sharapova can get in more workouts in less time when she uses Meldonium. 

At a press conference on Monday, Sharapova said she has been taking the drug for the past 10 years, after being prescribed it by a doctor in 2006.

“I was first given this medicine by my doctor for several health issues I was having back in 2006,” Sharapova said. ”I was getting sick a lot. I was getting the flu every couple of months. I had irregular EKG results.”

Sharapova also said she may have had a risk of developing diabetes at the time when she began taking Meldonium. ”I had a deficiency in magnesium and a family history of diabetes, and there were signs of diabetes. That is one of the medications, along with others, that I received,” she said.

Studies on the drug in rats have found that it can treat diabetes, which is caused by the buildup of glucose in the blood. Meldonium reduces the amount of glucose in the blood by forcing cells to metabolize carbohydrates, which are composed of glucose.

Additional studies have found that Meldonium can improve mood and motor function in humans with neurological disorders and brain circulatory problems. It has even been shown to enhance cognitive ability and prevent dementia in rats.

Meldonium currently is not approved by the FDA in the United States. It has not been submitted for approval, according to a spokesperson for Grindeks, because the cost associated with getting FDA approval is too high. 

It is approved in the Baltic states and Russia, according to the spokesperson, who said the approval process in these countries is shorter and cheaper than it is in the United States. 

Studies in rats have found that the drug has no long term adverse effects on heart or liver function. Hopefully the same goes for humans who have taken it for a decade, like Sharapova.