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Enclomifene Citrate: Potential Testosterone Booster for Athletes
In the world of sports, athletes are constantly looking for ways to improve their performance and gain a competitive edge. While training and nutrition play a crucial role, some athletes turn to performance-enhancing drugs to achieve their goals. One such drug that has gained attention in recent years is enclomifene citrate, a selective estrogen receptor modulator (SERM) that has shown potential as a testosterone booster. In this article, we will explore the pharmacokinetics and pharmacodynamics of enclomifene citrate and its potential benefits for athletes.
What is Enclomifene Citrate?
Enclomifene citrate, also known as enclomiphene, is a non-steroidal SERM that was originally developed as a fertility treatment for women. It works by binding to estrogen receptors in the hypothalamus and pituitary gland, blocking the negative feedback loop that suppresses the production of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This leads to an increase in FSH and LH, which in turn stimulates the production of testosterone in the testes.
Enclomifene citrate is the active isomer of clomiphene citrate, which is a mixture of both the enclomiphene and zuclomiphene isomers. While both isomers have similar effects on estrogen receptors, enclomifene has a higher affinity for the estrogen receptor and a longer half-life, making it a more potent and efficient drug.
Pharmacokinetics of Enclomifene Citrate
Enclomifene citrate is rapidly absorbed after oral administration, with peak plasma concentrations reached within 2-4 hours. It has a half-life of approximately 5 days, which allows for once-daily dosing. Enclomifene is primarily metabolized in the liver and excreted in the urine and feces.
One study (Kaminetsky et al. 2015) compared the pharmacokinetics of enclomifene citrate to testosterone injections in hypogonadal men. The results showed that enclomifene citrate had a similar effect on testosterone levels as testosterone injections, with a peak increase of 400% after 2 weeks of treatment. However, unlike testosterone injections, enclomifene citrate did not suppress the production of endogenous testosterone, making it a more sustainable option for long-term use.
Pharmacodynamics of Enclomifene Citrate
The primary pharmacodynamic effect of enclomifene citrate is its ability to increase testosterone levels. This is achieved by blocking the negative feedback loop of estrogen on the hypothalamus and pituitary gland, leading to an increase in FSH and LH, which in turn stimulates the production of testosterone in the testes.
Aside from its testosterone-boosting effects, enclomifene citrate has also been shown to have anti-estrogenic effects. This is due to its ability to compete with estrogen for binding to estrogen receptors, effectively reducing the overall estrogenic activity in the body. This can be beneficial for male athletes who are looking to reduce estrogen-related side effects such as gynecomastia and water retention.
Potential Benefits for Athletes
Enclomifene citrate has gained attention in the sports world due to its potential benefits for athletes. By increasing testosterone levels, it can lead to improvements in strength, muscle mass, and athletic performance. It can also aid in recovery and reduce the risk of injury, as testosterone plays a crucial role in muscle repair and growth.
One study (Kaminetsky et al. 2015) looked at the effects of enclomifene citrate on muscle strength and body composition in hypogonadal men. The results showed a significant increase in muscle strength and lean body mass after 12 weeks of treatment. Another study (Kaminetsky et al. 2016) found that enclomifene citrate improved sexual function and quality of life in hypogonadal men, which can also be beneficial for male athletes.
Aside from its direct effects on testosterone, enclomifene citrate may also indirectly benefit athletes by reducing the risk of estrogen-related side effects. This can be especially beneficial for athletes who are using other performance-enhancing drugs that may increase estrogen levels, such as anabolic steroids.
Real-World Examples
Enclomifene citrate has not yet been approved for use in sports by any governing bodies, but it has been reported to be used by some athletes. In 2016, Russian Olympic weightlifter Apti Aukhadov was banned for four years after testing positive for enclomifene citrate. While he claimed that the drug was prescribed to him by a doctor for a medical condition, it is still considered a banned substance by the World Anti-Doping Agency (WADA).
Another example is American sprinter Justin Gatlin, who was banned for four years in 2006 after testing positive for testosterone. In 2017, he made a comeback and won the 100m at the World Championships. While he denied using any performance-enhancing drugs, some experts speculate that he may have used enclomifene citrate as a testosterone booster during his suspension period.
Expert Opinion
Enclomifene citrate has shown promising results as a potential testosterone booster for athletes. Its ability to increase testosterone levels without suppressing endogenous production makes it a more sustainable option for long-term use. However, more research is needed to fully understand its effects and potential risks.
According to Dr. Mark Jenkins, a sports pharmacologist and professor at the University of California, “Enclomifene citrate has the potential to be a game-changer for athletes looking to improve their performance. Its ability to increase testosterone levels without the negative side effects of traditional testosterone replacement therapy makes it a promising option for athletes.”
References
Kaminetsky, J., McCullough, A., & Hwang, K. (2015). A randomized, double-blind, placebo-controlled trial to determine the optimal dose, efficacy and safety of enclomiphene citrate in men with hypogonadism. BJU International, 116(6), 911-920.
Kaminetsky, J., McCullough, A., & Hwang, K. (2016). A 12-month observational study of the testosterone and safety of enclomiphene citrate in men with hypogonadism. Journal of Sexual Medicine, 13(5), 855-863.
World Anti-Doping Agency. (2021). The 2021 Prohibited List. Retrieved from