• Table of Contents

  • Side Effects of Enclomifene Citrate in Athletes: What to Know
  • Pharmacokinetics and Pharmacodynamics of Enclomifene Citrate
  • Potential Side Effects of Enclomifene Citrate in Athletes
  • Real-World Examples of Enclomifene Citrate Use in Athletes
  • Expert Opinion on Enclomifene Citrate Use in Athletes
  • Conclusion
  • References

Side Effects of Enclomifene Citrate in Athletes: What to Know

Enclomifene citrate, also known as enclomiphene, is a selective estrogen receptor modulator (SERM) that is commonly used in the treatment of female infertility. However, it has also gained popularity among athletes as a performance-enhancing drug due to its ability to increase testosterone levels. While enclomifene citrate may offer benefits for athletes, it is important to understand the potential side effects that may occur with its use.

Pharmacokinetics and Pharmacodynamics of Enclomifene Citrate

Enclomifene citrate works by binding to estrogen receptors in the body, blocking the effects of estrogen and stimulating the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to an increase in testosterone levels, which can improve muscle mass, strength, and athletic performance.

The pharmacokinetics of enclomifene citrate have been studied in both men and women. In men, it is rapidly absorbed and reaches peak plasma levels within 2-3 hours after oral administration. It has a half-life of approximately 5 days, meaning it stays in the body for a longer period of time compared to other SERMs like tamoxifen. In women, enclomifene citrate has a similar half-life but is eliminated from the body more quickly due to differences in metabolism.

When it comes to pharmacodynamics, enclomifene citrate has been shown to increase testosterone levels by 2-3 times in men and 1.5-2 times in women. It also has a positive effect on sperm production and quality in men, making it a potential treatment for male infertility.

Potential Side Effects of Enclomifene Citrate in Athletes

While enclomifene citrate may offer benefits for athletes, it is important to be aware of the potential side effects that may occur with its use. These include:

• Estrogenic side effects: As a SERM, enclomifene citrate can have estrogenic effects in the body, leading to symptoms such as hot flashes, mood swings, and breast tenderness. These side effects are more common in women, but can also occur in men.
• Androgenic side effects: Enclomifene citrate can also have androgenic effects, which can lead to acne, oily skin, and increased body hair growth. These side effects are more common in men.
• Cardiovascular effects: There is some evidence that enclomifene citrate may have negative effects on cardiovascular health, including an increase in blood pressure and cholesterol levels. This is a concern for athletes who already have an increased risk of cardiovascular disease due to their intense training.
• Fertility issues: While enclomifene citrate can improve fertility in men, it may have the opposite effect in women. It can suppress ovulation and lead to a decrease in fertility, making it important for female athletes to carefully consider the potential risks before using this drug.

Real-World Examples of Enclomifene Citrate Use in Athletes

Enclomifene citrate has gained popularity among athletes, particularly in the bodybuilding community. It is often used as part of a post-cycle therapy (PCT) regimen to help restore natural testosterone production after a cycle of anabolic steroids. However, it has also been used as a standalone performance-enhancing drug by some athletes.

In 2016, Russian weightlifter Aleksey Lovchev was banned from competition for four years after testing positive for enclomifene citrate. Lovchev claimed that he had unknowingly ingested the drug through a contaminated supplement, but the Court of Arbitration for Sport rejected this defense and upheld his ban.

Another high-profile case involving enclomifene citrate was that of American sprinter Justin Gatlin. In 2006, Gatlin tested positive for testosterone and was banned from competition for eight years. He later admitted to using enclomifene citrate as part of his PCT regimen and claimed that he did not know it was a banned substance. Gatlin’s ban was eventually reduced to four years, but the incident tarnished his reputation and raised questions about the use of enclomifene citrate in sports.

Expert Opinion on Enclomifene Citrate Use in Athletes

Dr. Mark Jenkins, a sports pharmacologist and professor at the University of Queensland, believes that the use of enclomifene citrate in athletes is concerning. In an interview with the Australian Broadcasting Corporation, he stated, “It’s a drug that’s not approved for use in humans, and it’s being used in a way that’s not consistent with its intended use. That’s a concern.” He also expressed concerns about the potential side effects and long-term health consequences of using this drug in athletes.

Dr. Jenkins’ concerns are echoed by other experts in the field of sports pharmacology. In a study published in the Journal of Clinical Endocrinology and Metabolism, researchers found that enclomifene citrate use in male athletes was associated with adverse effects on cardiovascular health, including an increase in blood pressure and cholesterol levels. They also noted that the long-term effects of this drug on fertility and hormone levels are not well understood.

Conclusion

Enclomifene citrate may offer benefits for athletes in terms of increasing testosterone levels and improving performance. However, it is important for athletes to be aware of the potential side effects and risks associated with its use. As with any performance-enhancing drug, the use of enclomifene citrate should be carefully considered and monitored by a healthcare professional. It is also important for athletes to be aware of the potential consequences of using this drug, including negative impacts on their health and reputation.

References

Johnson, A. C., & Kicman, A. T. (2021). Enclomiphene citrate: a selective estrogen receptor modulator for the treatment of male hypogonadism. Expert Opinion on Pharmacotherapy, 22(1), 1-10.

Liu, P. Y., Swerdloff, R. S., & Wang, C. (2016). Drug insight: testosterone and selective androgen receptor modulators as anabolic therapies for chronic illness and aging. Nature Clinical Practice Endocrinology & Metabolism, 2(3), 146-159.

McLachlan, R. I., O’Donnell, L., Meachem, S.