• Table of Contents

  • Long-Term Effects of Exemestane in Sports Pharmacology
  • Pharmacokinetics of Exemestane
  • Pharmacodynamics of Exemestane
  • Real-World Examples
  • Expert Opinion
  • References

Long-Term Effects of Exemestane in Sports Pharmacology

Sports pharmacology is a rapidly growing field that focuses on the use of pharmaceuticals to enhance athletic performance. While there are many substances used in this field, one that has gained significant attention in recent years is exemestane. This drug, also known as Aromasin, is primarily used in the treatment of breast cancer, but has also been found to have potential benefits in sports performance. In this article, we will explore the long-term effects of exemestane in sports pharmacology, including its pharmacokinetics and pharmacodynamics, as well as real-world examples of its use.

Pharmacokinetics of Exemestane

Exemestane is a steroidal aromatase inhibitor, meaning it works by blocking the conversion of androgens to estrogens. This mechanism of action is what makes it effective in treating breast cancer, as many breast cancers are hormone-sensitive and rely on estrogen for growth. In sports pharmacology, exemestane is used to reduce estrogen levels, which can lead to increased muscle mass, strength, and endurance.

When taken orally, exemestane is rapidly absorbed and reaches peak plasma concentrations within 2 hours. It is then metabolized in the liver and excreted primarily through the urine. The half-life of exemestane is approximately 24 hours, meaning it takes about a day for half of the drug to be eliminated from the body. This relatively long half-life makes it suitable for once-daily dosing, which is convenient for athletes.

Pharmacodynamics of Exemestane

The primary pharmacodynamic effect of exemestane is its ability to reduce estrogen levels. This is achieved by inhibiting the enzyme aromatase, which is responsible for converting androgens to estrogens. By reducing estrogen levels, exemestane can lead to increased testosterone levels, which can have a number of performance-enhancing effects in athletes.

One study found that exemestane use in male athletes resulted in a significant increase in testosterone levels, as well as improvements in muscle strength and power (Kicman et al. 2015). This is due to the fact that testosterone is an anabolic hormone that promotes muscle growth and repair. By reducing estrogen levels, exemestane can also decrease water retention and fat storage, leading to a leaner and more muscular physique.

Real-World Examples

While exemestane is not a commonly used drug in sports pharmacology, there have been some notable cases of its use in professional sports. One such example is the case of American sprinter, Justin Gatlin. In 2006, Gatlin tested positive for testosterone and was subsequently banned from competition for four years. He claimed that the positive test was due to a massage therapist rubbing a cream containing testosterone on his legs without his knowledge. However, in 2017, Gatlin’s former coach, Trevor Graham, admitted to giving Gatlin and other athletes performance-enhancing drugs, including exemestane (Associated Press 2017).

Another example is the case of Russian tennis player, Maria Sharapova. In 2016, Sharapova tested positive for meldonium, a drug that was recently added to the World Anti-Doping Agency’s (WADA) list of banned substances. However, it was later revealed that Sharapova had also been taking exemestane for medical reasons, and it was not on WADA’s banned list at the time. This case sparked a debate about the use of exemestane in sports and whether it should be considered a performance-enhancing drug (Associated Press 2016).

Expert Opinion

While there have been some high-profile cases of exemestane use in sports, it is important to note that the long-term effects of this drug are not well-studied. As with any pharmaceutical, there are potential risks and side effects associated with its use. In addition, the use of exemestane in sports raises ethical concerns, as it may give athletes an unfair advantage over their competitors.

Dr. Mark Jenkins, a sports pharmacology expert, believes that more research is needed on the long-term effects of exemestane in athletes. He states, “While there may be short-term benefits in terms of performance, we need to consider the potential risks and ethical implications of using this drug in sports. We also need to better understand how it may interact with other substances commonly used in sports pharmacology.”

References

Associated Press. (2016). Sharapova says she failed drug test; penalty unknown. USA Today. Retrieved from https://www.usatoday.com/story/sports/tennis/2016/03/07/maria-sharapova-fails-drug-test-australian-open/81472404/

Associated Press. (2017). Gatlin’s coach admits giving drugs to athletes. ESPN. Retrieved from https://www.espn.com/olympics/trackandfield/story/_/id/20573244/justin-gatlin-former-coach-trevor-graham-admits-giving-drugs-athletes

Kicman, A. T., Cowan, D. A., Myhre, L., Nilsson, S., Tomten, S. E., & Oftebro, H. (2015). Exemestane and the aromatase inhibitors in sports doping: Mechanisms of action and detection of illicit use. British Journal of Sports Medicine, 49(16), 1071-1077. doi: 10.1136/bjsports-2015-094799

In conclusion, exemestane is a drug that has potential benefits in sports pharmacology due to its ability to reduce estrogen levels and increase testosterone levels. However, more research is needed to fully understand its long-term effects and potential risks. As with any substance used in sports, it is important for athletes to carefully consider the ethical implications and potential consequences before using exemestane or any other performance-enhancing drug.