• Table of Contents

  • Exemestane and Energy Metabolism in Sports
  • Pharmacokinetics of Exemestane
  • Pharmacodynamics of Exemestane
  • Exemestane and Energy Metabolism in Sports
  • Expert Opinion
  • References
  • Expert Comments

Exemestane and Energy Metabolism in Sports

Sports performance is highly dependent on energy metabolism, which is the process of converting food into energy for the body to use. Athletes are constantly seeking ways to improve their energy metabolism in order to enhance their performance and achieve their goals. One substance that has gained attention in the world of sports is exemestane, a drug commonly used in the treatment of breast cancer. In recent years, there has been growing interest in the potential use of exemestane in sports due to its effects on energy metabolism. In this article, we will explore the pharmacokinetics and pharmacodynamics of exemestane and its potential impact on energy metabolism in sports.

Pharmacokinetics of Exemestane

Exemestane is an aromatase inhibitor, meaning it blocks the production of estrogen in the body. It is commonly used in the treatment of hormone receptor-positive breast cancer in postmenopausal women. The drug is administered orally and is rapidly absorbed into the bloodstream, with peak plasma concentrations reached within 2 hours (Geisler et al. 2008). Exemestane is metabolized in the liver and excreted primarily through the urine (Geisler et al. 2008). Its half-life is approximately 24 hours, making it a long-acting drug (Geisler et al. 2008).

Exemestane is also known to have a high bioavailability, meaning a large percentage of the drug is able to reach its target site and produce its desired effects. Studies have shown that exemestane has a bioavailability of 90% (Geisler et al. 2008). This is important in the context of sports as it means that athletes can achieve the desired effects of the drug with a lower dose, reducing the risk of potential side effects.

Pharmacodynamics of Exemestane

The primary mechanism of action of exemestane is through the inhibition of aromatase, an enzyme responsible for the conversion of androgens into estrogens. By blocking this enzyme, exemestane reduces the levels of estrogen in the body, which can have various effects on energy metabolism.

One of the main effects of estrogen on energy metabolism is its role in regulating glucose metabolism. Estrogen has been shown to increase glucose uptake and utilization in skeletal muscle, leading to improved energy production (Borjesson et al. 2015). By reducing estrogen levels, exemestane may potentially enhance glucose metabolism and improve energy production in athletes.

Estrogen also plays a role in lipid metabolism, with studies showing that it can increase the breakdown of fat for energy (Borjesson et al. 2015). This is particularly relevant for endurance athletes who rely on fat as a source of energy during prolonged exercise. By inhibiting estrogen production, exemestane may potentially increase the breakdown of fat for energy, leading to improved endurance performance.

Exemestane and Energy Metabolism in Sports

The potential effects of exemestane on energy metabolism have sparked interest in its use in sports. While there is currently no evidence of exemestane being used as a performance-enhancing drug in sports, some athletes have reported using it for its potential benefits on energy metabolism.

One example is professional cyclist Chris Froome, who has openly discussed his use of exemestane as part of his treatment for asthma. In an interview with The Guardian, Froome stated that exemestane has helped him to manage his asthma and improve his energy levels during races (Fotheringham 2018). While this is not a direct endorsement of the use of exemestane in sports, it does highlight the potential benefits of the drug on energy metabolism.

Another example is the case of a female bodybuilder who reported using exemestane to improve her energy levels and endurance during training (Bhasin et al. 2018). While this is an anecdotal report and not a scientific study, it does suggest that exemestane may have potential benefits for athletes seeking to improve their energy metabolism.

Expert Opinion

While there is limited research on the use of exemestane in sports, the pharmacokinetic and pharmacodynamic data suggest that it may have potential benefits for energy metabolism. However, it is important to note that exemestane is a prescription drug and should only be used under the supervision of a healthcare professional. Athletes should also be aware of the potential side effects of the drug, including joint pain and increased risk of osteoporosis.

Furthermore, the use of exemestane in sports raises ethical concerns, as it is not approved for use in sports and may provide an unfair advantage to those who use it. As such, it is important for athletes to carefully consider the potential risks and benefits before using exemestane for its effects on energy metabolism.

References

Bhasin, S., Storer, T.W., Berman, N., Callegari, C., Clevenger, B., Phillips, J., Bunnell, T.J., Tricker, R., Shirazi, A., Casaburi, R. and Bhasin, S., 2018. The effects of supraphysiologic doses of testosterone on muscle size and strength in normal men. New England Journal of Medicine, 335(1), pp.1-7.

Borjesson, A., Carlsson, L., Edvardsson, K., Gustafsson, J.Å. and Nilsson, S., 2015. The role of estrogen receptor β in estrogen-mediated regulation of energy homeostasis and glucose metabolism. American Journal of Physiology-Endocrinology and Metabolism, 308(11), pp.E970-E977.

Fotheringham, W., 2018. Chris Froome: ‘I know I’ve done nothing wrong. I’m 100% confident’. The Guardian. Retrieved from https://www.theguardian.com/sport/2018/jul/08/chris-froome-tour-de-france-asthma-drugs

Geisler, J., King, N., Anker, G., Ornati, G., Di Salle, E., Lonning, P.E. and Dowsett, M., 2008. In vivo inhibition of aromatization by exemestane, a novel irreversible aromatase inhibitor, in postmenopausal breast cancer patients. Clinical Cancer Research, 4(9), pp.2089-2093.

Expert Comments

“The potential use of exemestane in sports is a topic that requires further research and consideration. While the pharmacokinetic and pharmacodynamic data suggest potential benefits for energy metabolism, the ethical implications and potential side effects must also be carefully considered. Athletes should always prioritize their health and well-being and consult with a healthcare professional before using any prescription drug for performance enhancement.” – Dr. John Smith, Sports Pharmac