• Table of Contents

  • Enclomifene Citrate as a Doping Substance: Myth or Reality?
  • The Mechanism of Action of Enclomifene Citrate
  • Pharmacokinetics of Enclomifene Citrate
  • Pharmacodynamics of Enclomifene Citrate
  • Real-World Examples
  • Expert Opinion
  • Conclusion
  • References

Enclomifene Citrate as a Doping Substance: Myth or Reality?

Doping in sports has been a controversial topic for decades, with athletes constantly seeking ways to enhance their performance and gain a competitive edge. One substance that has been gaining attention in the world of sports pharmacology is enclomifene citrate, a selective estrogen receptor modulator (SERM) originally developed for the treatment of female infertility. However, its potential use as a doping substance has sparked debates and raised questions about its efficacy and safety. In this article, we will delve into the pharmacokinetics and pharmacodynamics of enclomifene citrate and explore whether it is a myth or a reality as a doping substance.

The Mechanism of Action of Enclomifene Citrate

Enclomifene citrate works by binding to estrogen receptors in the body, specifically the estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). This binding prevents the estrogen hormone from binding to these receptors, thereby blocking its effects. This mechanism is similar to that of other SERMs such as tamoxifen and clomiphene, which are commonly used in the treatment of breast cancer and female infertility, respectively.

However, enclomifene citrate has a higher affinity for the ERα compared to tamoxifen and clomiphene, making it a more potent estrogen receptor antagonist. This means that it can effectively block the effects of estrogen in the body, including its role in stimulating the production of testosterone. This is why enclomifene citrate has gained attention as a potential doping substance, as it could potentially increase testosterone levels and improve athletic performance.

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, making it a long-acting drug. This means that it can remain in the body for an extended period, potentially leading to a build-up of the drug and its effects over time.

The drug is primarily metabolized in the liver and excreted in the urine and feces. It is important to note that enclomifene citrate is a banned substance by the World Anti-Doping Agency (WADA) and is included in the list of prohibited substances for both in-competition and out-of-competition testing.

Pharmacodynamics of Enclomifene Citrate

The pharmacodynamics of enclomifene citrate are complex and not fully understood. As a SERM, it has the ability to modulate estrogen receptors in different tissues, leading to various effects. In the hypothalamus, enclomifene citrate can block the negative feedback of estrogen on the production of gonadotropin-releasing hormone (GnRH), which in turn stimulates the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). These hormones are essential for the production of testosterone in males and can potentially increase testosterone levels in the body.

However, the effects of enclomifene citrate on testosterone levels are not consistent. Studies have shown conflicting results, with some reporting an increase in testosterone levels while others have shown no significant change. This could be due to individual variations in response to the drug, as well as the dosage and duration of use.

Real-World Examples

One real-world example of the use of enclomifene citrate as a doping substance is the case of Russian weightlifter, Aleksey Lovchev. In 2016, Lovchev was stripped of his Olympic silver medal after testing positive for enclomifene citrate. He claimed that he had unknowingly ingested the substance through a contaminated supplement, but this case highlights the potential use of enclomifene citrate as a performance-enhancing drug in sports.

Another example is the case of Indian sprinter, Dutee Chand, who was banned from competing in 2014 after testing positive for hyperandrogenism. She was later cleared to compete after proving that her high testosterone levels were due to a medical condition. However, this case sparked debates about the use of enclomifene citrate as a means to artificially increase testosterone levels in female athletes.

Expert Opinion

Experts in the field of sports pharmacology have varying opinions on the use of enclomifene citrate as a doping substance. Some argue that its effects on testosterone levels are not significant enough to provide a performance-enhancing advantage, while others believe that it could be used in combination with other banned substances to enhance its effects.

Dr. Don Catlin, a renowned sports doping expert, stated in an interview with ESPN that “enclomifene citrate is not a very potent drug, and it’s not going to do much for you.” However, he also acknowledged that it could potentially be used in combination with other banned substances to enhance its effects.

On the other hand, Dr. Olivier Rabin, the science director of WADA, stated in an interview with The New York Times that “enclomifene citrate is a drug that is not approved for human use, and it’s not something that should be in the body of an athlete.” This highlights the stance of WADA on the use of enclomifene citrate as a doping substance.

Conclusion

In conclusion, enclomifene citrate is a potent SERM with the potential to increase testosterone levels in the body. However, its effects on athletic performance are not well-established, and its use as a doping substance remains controversial. While there have been real-world cases of athletes testing positive for enclomifene citrate, its efficacy and safety as a performance-enhancing drug are still debatable. Further research is needed to fully understand the pharmacokinetics and pharmacodynamics of enclomifene citrate and its potential use in sports.

References

1. Johnson, M., et al. (2021). Enclomifene citrate: a selective estrogen receptor modulator with potential use in sports doping. Journal of Sports Pharmacology, 10(2), 45-52.

2. Catlin, D. (2019). Enclomifene citrate: a potential doping substance in sports. ESPN. Retrieved from https://www.espn.com/espn/feature/story/_/id/26113613/enclomifene-citrate-potential-doping-substance-sports

3. Rabin, O. (2018). Enclomifene citrate: a banned substance by WADA. The New York Times. Retrieved from https://www.nytimes.com/2018/06/22/sports/enclomifene