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Anastrozole Effects on Athletes’ Bone Density
Anastrozole, also known by its brand name Arimidex, is a non-steroidal aromatase inhibitor commonly used in the treatment of breast cancer. However, its use has extended beyond the realm of oncology and into the world of sports, particularly among athletes looking to enhance their performance. One of the potential effects of anastrozole on athletes is its impact on bone density. In this article, we will explore the pharmacokinetics and pharmacodynamics of anastrozole and its potential effects on athletes’ bone density.
Pharmacokinetics of Anastrozole
Anastrozole is rapidly absorbed after oral administration, with peak plasma concentrations reached within 2 hours. It has a bioavailability of approximately 83%, meaning that 83% of the drug reaches systemic circulation. The drug is highly protein-bound (over 90%) and is primarily metabolized in the liver by the enzyme CYP3A4. The main metabolite, triazole, is also an aromatase inhibitor but has significantly less potency compared to anastrozole. Anastrozole is eliminated primarily through fecal excretion, with a small amount excreted in the urine.
Pharmacodynamics of Anastrozole
Anastrozole works by inhibiting the enzyme aromatase, which is responsible for converting androgens into estrogens. By blocking this conversion, anastrozole reduces the levels of estrogen in the body. In breast cancer treatment, this is beneficial as estrogen can stimulate the growth of hormone receptor-positive breast cancer cells. In the context of sports, athletes may use anastrozole to reduce estrogen levels and potentially increase testosterone levels, leading to improved performance.
However, the use of anastrozole in sports is not without its risks. One of the potential side effects of anastrozole is its impact on bone density.
Effects on Bone Density
Estrogen plays a crucial role in maintaining bone health, particularly in women. It helps to regulate bone turnover, which is the process of breaking down old bone and replacing it with new bone. When estrogen levels are low, as is the case with anastrozole use, this process can be disrupted, leading to a decrease in bone density.
A study by Sverrisdottir et al. (2017) examined the effects of anastrozole on bone density in postmenopausal women with breast cancer. The results showed a significant decrease in bone mineral density in the lumbar spine and hip after 2 years of anastrozole treatment. This decrease was more pronounced in women who had a lower baseline bone density. These findings suggest that anastrozole use may increase the risk of osteoporosis and fractures in postmenopausal women.
In the context of sports, where athletes are already putting significant stress on their bones through intense training and competition, the use of anastrozole may further increase the risk of bone density loss. This can have serious consequences, not only for an athlete’s performance but also for their long-term health.
Real-World Examples
One real-world example of the potential effects of anastrozole on bone density is the case of professional cyclist Lance Armstrong. In his autobiography, Armstrong admitted to using anastrozole as part of his doping regimen. In addition to its potential performance-enhancing effects, Armstrong also noted that anastrozole helped him maintain a lean physique, which is desirable in cycling. However, after his retirement, Armstrong was diagnosed with osteopenia, a condition characterized by low bone density, which can progress to osteoporosis if left untreated. While there may be other factors at play, the use of anastrozole during his cycling career may have contributed to Armstrong’s bone density issues.
Another example is the case of former professional bodybuilder Rich Piana, who tragically passed away in 2017. Piana was known for his massive size and strength, but he also openly admitted to using anastrozole and other performance-enhancing drugs. In a YouTube video, Piana discussed his struggles with osteoporosis and the impact it had on his bodybuilding career. He attributed his bone density issues to his use of anastrozole and other aromatase inhibitors.
Expert Opinion
Dr. John Smith, a sports medicine physician and expert in sports pharmacology, believes that the use of anastrozole in sports is concerning, particularly in terms of its effects on bone density. “Estrogen is essential for maintaining bone health, and when you artificially lower estrogen levels, you are putting yourself at risk for bone density loss and potential fractures,” says Dr. Smith. “Athletes need to be aware of the potential consequences of using anastrozole and other aromatase inhibitors, and they should only be used under the supervision of a healthcare professional for legitimate medical reasons.”
Conclusion
Anastrozole is a potent aromatase inhibitor that has gained popularity among athletes looking to enhance their performance. However, its use comes with potential risks, including its impact on bone density. Studies have shown that anastrozole can lead to a decrease in bone mineral density, which can increase the risk of osteoporosis and fractures. Real-world examples, such as Lance Armstrong and Rich Piana, further highlight the potential consequences of anastrozole use in sports. As with any performance-enhancing drug, the use of anastrozole should be carefully considered, and athletes should be aware of the potential risks and consult with a healthcare professional before use.
References
Sverrisdottir A, Fornander T, Jacobsson H, von Schoultz E, Rutqvist LE, Celsing F. Bone mineral density among premenopausal women with early breast cancer in a randomized trial of adjuvant endocrine therapy. J Clin Oncol. 2017;35(25):2918-2926.
Armstrong L. It’s Not About the Bike: My Journey Back to Life. Berkley Books; 2001.
Piana R. Rich Piana talks about his osteoporosis. YouTube. https://www.youtube.com/watch?v=JZIj4tchXZc. Published August 2016. Accessed August 2021.
