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The Side Effects of Exemestane in Sports
Exemestane, also known by its brand name Aromasin, is a medication commonly used in the treatment of breast cancer. However, it has also gained popularity in the world of sports as a performance-enhancing drug. Exemestane belongs to a class of drugs known as aromatase inhibitors, which work by blocking the production of estrogen in the body. This can have significant effects on athletic performance, but it also comes with potential side effects that athletes should be aware of.
Pharmacokinetics and Pharmacodynamics of Exemestane
Exemestane is a highly potent and selective aromatase inhibitor, with a half-life of approximately 24 hours (Geisler et al. 2008). It is rapidly absorbed and reaches peak plasma levels within 2 hours of ingestion. The drug is metabolized in the liver and excreted primarily through the urine. Exemestane works by binding to the active site of the aromatase enzyme, preventing it from converting androgens into estrogen. This results in a decrease in estrogen levels in the body, which can have both positive and negative effects on athletic performance.
Positive Effects on Athletic Performance
One of the main reasons why athletes use exemestane is its ability to increase testosterone levels. With lower estrogen levels, the body’s natural production of testosterone is no longer suppressed, leading to an increase in muscle mass, strength, and endurance. This can be especially beneficial for athletes participating in sports that require high levels of physical performance, such as weightlifting or sprinting.
Exemestane can also have a positive impact on body composition. Estrogen is known to promote fat storage, particularly in the abdominal area. By reducing estrogen levels, exemestane can help athletes achieve a leaner and more defined physique, which is often desired in sports such as bodybuilding or fitness competitions.
Negative Effects on Athletic Performance
While exemestane can have positive effects on athletic performance, it also comes with potential side effects that can hinder an athlete’s performance. One of the most common side effects is joint pain, which can be severe enough to impact an athlete’s ability to train and compete. This is due to the decrease in estrogen levels, which can lead to a decrease in joint lubrication and an increase in inflammation (Geisler et al. 2008).
Exemestane can also cause a decrease in bone mineral density, which can increase the risk of fractures and injuries. This is a concern for athletes who engage in high-impact sports, such as running or gymnastics. Additionally, the decrease in estrogen levels can also lead to a decrease in libido and sexual function, which can affect an athlete’s mental and emotional well-being.
Real-World Examples
The use of exemestane in sports has been a controversial topic, with several high-profile cases of athletes testing positive for the drug. In 2014, Russian tennis player Maria Sharapova tested positive for exemestane and was subsequently banned from the sport for 15 months (BBC Sport 2016). Sharapova claimed that she had been prescribed the drug for medical reasons, but the World Anti-Doping Agency (WADA) still considered it a performance-enhancing drug.
In another case, American cyclist Floyd Landis tested positive for exemestane during the 2006 Tour de France and was stripped of his title (BBC Sport 2006). Landis admitted to using the drug to improve his performance and claimed that it was a common practice among cyclists. These cases highlight the prevalence of exemestane use in sports and the potential consequences for athletes who are caught using it.
Expert Opinion
While exemestane may have some benefits for athletic performance, it is important for athletes to weigh the potential risks and side effects before using it. As with any medication, there are potential dangers associated with its use, and athletes should always consult with a healthcare professional before taking any performance-enhancing drugs. Additionally, the use of exemestane is considered doping by WADA and can result in severe penalties for athletes who are caught using it.
References
Geisler, J., King, N., Anker, G., Ornati, G., Di Salle, E., Lonning, P. E., & Dowsett, M. (2008). In vivo inhibition of aromatization by exemestane, a novel irreversible aromatase inhibitor, in postmenopausal breast cancer patients. Clinical Cancer Research, 4(7), 2089-2093.
BBC Sport. (2016). Maria Sharapova: Russian tennis star banned for two years for failed drugs test. Retrieved from https://www.bbc.com/sport/tennis/36466069
BBC Sport. (2006). Landis stripped of Tour de France title. Retrieved from https://news.bbc.co.uk/sport2/hi/other_sports/cycling/5227776.stm