The side effects of cyproterone acetate (CPA), a steroidal antiandrogen and progestin, including its frequent and rare side effects, have been studied and characterized. It is generally well-tolerated and has a mild side-effect profile, regardless of dosage, when it used as a progestin or antiandrogen in combination with an estrogen such as ethinylestradiol or estradiol valerate in women.[1][2] Side effects of CPA include hypogonadism and associated symptoms such as demasculinization, sexual dysfunction, infertility, and osteoporosis; breast changes such as breast tenderness, enlargement, and gynecomastia; emotional changes such as fatigue and depression; and other side effects such as vitamin B12 deficiency, weak glucocorticoid effects, and elevated liver enzymes.[3] Weight gain can occur with CPA when it is used at high doses.[4][5] Some of the side effects of CPA can be improved or fully prevented if it is combined with an estrogen to prevent estrogen deficiency.[6][7] Few quantitative data are available on many of the potential side effects of CPA.[8] Pooled tolerability data for CPA is not available in the literature.[9]
At very high doses in aged men with prostate cancer, CPA can cause cardiovascular side effects. Rarely, CPA can produce blood clots, liver damage, excessively high prolactin levels, prolactinomas, and meningiomas. Upon discontinuation from high doses, CPA can produce adrenal insufficiency as a withdrawal effect.
^Bachelot A, Chabbert-Buffet N, Salenave S, Kerlan V, Galand-Portier MB (February 2010). "Anti-androgen treatments". Ann. Endocrinol. (Paris). 71 (1): 19–24. doi:10.1016/j.ando.2009.12.001. PMID 20096826.
^Hammerstein, J. (1990). "Antiandrogens: Clinical Aspects". Hair and Hair Diseases. pp. 827–886. doi:10.1007/978-3-642-74612-3_35. ISBN 978-3-642-74614-7.
^Cite error: The named reference pmid10352926 was invoked but never defined (see the help page).
^Cite error: The named reference pmid2946604 was invoked but never defined (see the help page).
^Diamanti-Kandarakis E (October 1998). "How actual is the treatment with antiandrogen alone in patients with polycystic ovary syndrome?". J. Endocrinol. Invest. 21 (9): 623–9. doi:10.1007/BF03350788. PMID 9856417. S2CID 46484837.
^Diamanti-Kandarakis E (September 1999). "Current aspects of antiandrogen therapy in women". Curr. Pharm. Des. 5 (9): 707–23. doi:10.2174/1381612805666230111201150. PMID 10495361.
^Guay DR (January 2009). "Drug treatment of paraphilic and nonparaphilic sexual disorders". Clin Ther. 31 (1): 1–31. doi:10.1016/j.clinthera.2009.01.009. PMID 19243704. No quantitative data on these adverse events are available, even in the product prescribing information and data sheets.
^Cite error: The named reference pmid10673793 was invoked but never defined (see the help page).
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