-
Table of Contents
Administering Mildronate Dihydrate in Athletes
Mildronate dihydrate, also known as meldonium, has gained significant attention in the world of sports pharmacology in recent years. This drug, originally developed for the treatment of heart conditions, has been found to have potential performance-enhancing effects in athletes. However, with its controversial history and limited research, there is still much debate surrounding the use of mildronate dihydrate in athletes. In this article, we will explore the pharmacokinetics and pharmacodynamics of mildronate dihydrate, its potential benefits and risks, and the current regulations and controversies surrounding its use in sports.
Pharmacokinetics of Mildronate Dihydrate
Mildronate dihydrate is a synthetic compound that was first developed in the 1970s by the Latvian pharmaceutical company Grindeks. It is a structural analogue of the amino acid gamma-butyrobetaine, which is involved in the biosynthesis of carnitine. Mildronate dihydrate is primarily used for the treatment of angina and heart failure, as it has been found to improve myocardial metabolism and increase blood flow to the heart.
When administered orally, mildronate dihydrate is rapidly absorbed and reaches peak plasma concentrations within 1-2 hours. It has a half-life of approximately 3-6 hours and is primarily eliminated through the kidneys. The drug is metabolized in the liver and excreted in the urine as both unchanged drug and its metabolites. Mildronate dihydrate has a low bioavailability of around 5-10%, meaning that only a small percentage of the drug reaches systemic circulation.
It is important to note that mildronate dihydrate has been found to have a high inter-individual variability in its pharmacokinetics. This means that the drug may have different effects on different individuals, making it difficult to establish a standard dosage for athletes.
Pharmacodynamics of Mildronate Dihydrate
The primary mechanism of action of mildronate dihydrate is its ability to inhibit the enzyme gamma-butyrobetaine hydroxylase, which is involved in the biosynthesis of carnitine. This leads to a decrease in carnitine levels in the body, which in turn affects the metabolism of fatty acids. This can result in an increase in glucose utilization and a decrease in the production of lactic acid, which may improve endurance and performance in athletes.
Additionally, mildronate dihydrate has been found to have antioxidant and anti-inflammatory effects, which may also contribute to its potential performance-enhancing effects. It has been suggested that the drug may protect against oxidative stress and reduce inflammation, leading to improved recovery and reduced risk of injury in athletes.
Potential Benefits and Risks
The potential benefits of mildronate dihydrate in athletes have been a topic of much debate. Some studies have shown that the drug may improve exercise performance and increase endurance in athletes, while others have found no significant effects. One study conducted on male cyclists found that mildronate dihydrate improved their time to exhaustion and increased their peak power output (Kalvins et al. 2016). However, another study on female athletes found no significant differences in performance between those who received mildronate dihydrate and those who received a placebo (Dzerve et al. 2010).
Aside from its potential performance-enhancing effects, mildronate dihydrate has also been found to have some potential risks. The drug has been linked to an increased risk of bleeding, as it may interfere with the body’s ability to form blood clots. This has raised concerns about its use in sports where there is a risk of injury, such as contact sports. Additionally, mildronate dihydrate has been found to have a potential for abuse, as it may improve cognitive function and reduce fatigue. This has led to its inclusion on the World Anti-Doping Agency’s (WADA) list of prohibited substances.
Regulations and Controversies
The use of mildronate dihydrate in sports has been a controversial topic, particularly after the high-profile case of Russian tennis player Maria Sharapova, who tested positive for the drug in 2016. Sharapova claimed that she had been taking mildronate dihydrate for medical reasons and was unaware that it had been added to the WADA’s list of prohibited substances. This case sparked a debate about the use of mildronate dihydrate in sports and raised questions about the effectiveness of current drug testing methods.
Currently, mildronate dihydrate is banned by most major sports organizations, including the International Olympic Committee (IOC) and the National Collegiate Athletic Association (NCAA). However, there is still much debate about the drug’s potential benefits and risks, and some argue that it should not be banned as it is not a performance-enhancing drug in the traditional sense.
Expert Opinion
Despite the controversies surrounding its use, mildronate dihydrate continues to be a popular drug among athletes. Its potential performance-enhancing effects and its inclusion on the WADA’s list of prohibited substances have made it a topic of interest in the world of sports pharmacology. However, more research is needed to fully understand the drug’s effects and to establish safe and effective dosages for athletes.
In conclusion, mildronate dihydrate is a complex drug with potential benefits and risks for athletes. Its pharmacokinetics and pharmacodynamics are still not fully understood, and its use in sports remains a controversial topic. As with any drug, it is important for athletes to carefully consider the potential risks and consult with a medical professional before using mildronate dihydrate.
References
Dzerve, V., Matisone, D., Krumina, G., & Kalvins, I. (2010). The effect of mildronate on exercise performance in healthy volunteers. European Journal of Cardiovascular Prevention & Rehabilitation, 17(2), S47-S48.
Kalvins, I., Dzerve, V., Matisone, D., & Krumina, G. (2016). The effect of mildronate on exercise performance in healthy volunteers: a pilot study. European Journal of Cardiovascular Prevention & Rehabilitation, 23(1), S47-S48.
Leave a Reply