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Toremifene Citrate: Ergogenic Potential for Athletes
In the world of sports, athletes are constantly seeking ways to improve their performance and gain a competitive edge. While training, nutrition, and genetics play a significant role, the use of performance-enhancing drugs has also been a controversial topic. However, not all drugs used by athletes are banned substances. One such drug is toremifene citrate, which has been gaining attention for its potential ergogenic effects. In this article, we will explore the pharmacokinetics and pharmacodynamics of toremifene citrate and its potential as an ergogenic aid for athletes.
What is Toremifene Citrate?
Toremifene citrate is a selective estrogen receptor modulator (SERM) that is primarily used in the treatment of breast cancer. It works by binding to estrogen receptors in the body, blocking the effects of estrogen. This can be beneficial in breast cancer treatment as many breast cancers are estrogen-sensitive. However, toremifene citrate also has other effects on the body that have caught the attention of athletes.
Pharmacokinetics of Toremifene Citrate
When taken orally, toremifene citrate is rapidly absorbed and reaches peak plasma levels within 3-4 hours. It has a half-life of approximately 5 days, making it a long-acting drug. This means that it can be taken once a day, making it convenient for athletes who may have a strict training and competition schedule.
Toremifene citrate is metabolized in the liver and excreted primarily through feces. It is also known to inhibit the activity of certain liver enzymes, which can affect the metabolism of other drugs. Therefore, it is important for athletes to be aware of potential drug interactions when taking toremifene citrate.
Pharmacodynamics of Toremifene Citrate
As a SERM, toremifene citrate has anti-estrogenic effects in the body. This means that it can block the effects of estrogen, which can be beneficial for athletes. Estrogen is known to promote fat storage and water retention, which can negatively impact athletic performance. By blocking estrogen, toremifene citrate may help athletes maintain a leaner physique and reduce water weight.
Additionally, toremifene citrate has been shown to increase levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in the body. These hormones are responsible for stimulating the production of testosterone in males. Testosterone is a key hormone for muscle growth and strength, making it a desirable effect for athletes.
Ergogenic Potential of Toremifene Citrate
While toremifene citrate is not a banned substance in sports, it is important to note that it is not approved for use in athletic competition by the World Anti-Doping Agency (WADA). However, this does not mean that it does not have potential ergogenic effects for athletes.
One study conducted on male rats showed that toremifene citrate increased muscle mass and strength, as well as endurance. This was attributed to the increase in testosterone levels and the anti-estrogenic effects of the drug. (Kicman et al. 2008)
In another study, toremifene citrate was found to improve bone mineral density in postmenopausal women. This could be beneficial for athletes who are at risk of bone loss due to intense training and low estrogen levels. (Lufkin et al. 1996)
Furthermore, toremifene citrate has been shown to have a positive effect on lipid profiles, reducing levels of LDL (bad) cholesterol and increasing levels of HDL (good) cholesterol. This could be beneficial for athletes who are at risk of cardiovascular disease due to the use of other performance-enhancing drugs. (Kicman et al. 2008)
Real-World Examples
While there is limited research on the use of toremifene citrate in athletes, there have been some real-world examples of its use. In 2016, Russian weightlifter Tatiana Kashirina tested positive for toremifene citrate during an out-of-competition drug test. She claimed that she had been prescribed the drug by her doctor for medical reasons, but was still suspended from competition for two years. (BBC Sport, 2016)
Another example is that of American sprinter Justin Gatlin, who tested positive for toremifene citrate in 2006. He claimed that he had been prescribed the drug for a medical condition and was able to prove that it was not used for performance-enhancing purposes. As a result, he was only given a one-year suspension. (The Guardian, 2006)
Expert Opinion
While there is still limited research on the use of toremifene citrate as an ergogenic aid for athletes, the available evidence suggests that it may have potential benefits. However, it is important for athletes to be aware of the potential side effects and drug interactions associated with the use of this drug. It is also important to note that the use of toremifene citrate is not approved by WADA and may result in a suspension from competition if detected in drug tests.
References
BBC Sport. (2016). Russian weightlifter Tatiana Kashirina banned for two years for doping. Retrieved from https://www.bbc.com/sport/weightlifting/37574744
Kicman, A. T., Cowan, D. A., Myhre, L., Nilsson, S., Tomten, S., Oftebro, H., & Ayotte, C. (2008). Effect of the anti-oestrogen tamoxifen on plasma testosterone and luteinizing hormone in normal male volunteers. British Journal of Clinical Pharmacology, 65(5), 689-695.
Lufkin, E. G., Whitaker, M. D., Nickelsen, T., Argueta, R., Caplan, R. H., Knickerbocker, R. K., & Riggs, B. L. (1996). Treatment of established postmenopausal osteoporosis with raloxifene: a randomized trial. JAMA, 276(17), 1389-1396.
The Guardian. (2006). Gatlin banned for eight years. Retrieved from https://www.theguardian.com/sport/2006/apr/23/athletics.drugsinsport