Cyproterone
Classification: BATC code: G03HA01, G03HB01
Summary
Cyproterone is an antiandrogen which has different indications in men and women, making relevant analysis of sex differences in effect difficult. The most common adverse events, but not the serious adverse events, differ between men and women. Meningioma is an unusual adverse event of high dose cyproterone, a retrospective cohort study found a higher risk in women.
Additional information
Cyproterone is an antiandrogen with different indications in men and women. In men, it is primarily used to decrease the sex-drive in men with paraphilia or in sex offenders [1-2]. but also in prostate cancer [3]. In fertile women, it is used to treat extensive hirsutism [1-2]. The substance is also one of the main antiandrogen medications used in feminizing hormone therapy in transgender men [4].
In combination with ethinylestradiol cyproterone is used for treatment of moderate to severe acne or hirsutism in women [1-2]. It might also be used as an oral contraceptive drug in women but this is not a primary indication.
Pharmacokinetics and dosing
No studies comparing pharmacokinetic properties in men and women have been found. One small study in healthy men (n=28, ages 22-74 years) found an age-dependent change in apparent clearance and volume of distribution causing a longer terminal half-life of cyproterone in older men [5].
Effects
Cyproterone is used on different indications in men and women and thus comparison of effects is not relevant.
Adverse effects
The most common reported adverse events in men are decreased libido, erectile dysfunction, and reversible inhibition of the spermatogenesis. In women, the most commonly reported adverse events are spot bleedings, increased weight, and depression [1]. The most severe adverse events in both men and women are hepatotoxicity, benign and malignant hepatic tumors which may lead to intraabdominal bleeding, and thromboembolic events [1]. In rats, considerably higher doses (five-fold) have been needed to induce hepatic tumors [6].
Meningioma is an uncommon adverse effect of cyproterone treatment [7]. An observational retrospective cohort study from Spain (130 men, 326 women with meningiomas identified in 2 137 191 persons of which 2 474 used high dose cyproterone) found an increased risk of meningioma in those with high doses of cyproterone during a period of at least 2 years of 11.4 (95% CI 4.3, 30.8) (8). Women were found to have a risk ratio of 2.0 compared to men [7].
Reproductive health issues
Regarding teratogenic aspects, please consult the Drugs and Birth Defects Database (in Swedish, Janusmed fosterpåverkan).
Updated: 2019-02-26
Date of litterature search: 2017-07-11
References
- Androcur (cyproteron). Summary of Product Characteristics. Medical Products Agency (MPA); 2017.
- Cyproterone. Drugscom [www]. [cited 2017-07-11]. länk
- Fung R, Hellstern-Layefsky M, Tastenhoye C, Lega I, Steele L. Differential Effects of Cyproterone Acetate vs Spironolactone on Serum High-Density Lipoprotein and Prolactin Concentrations in the Hormonal Treatment of Transgender Women. J Sex Med. 2016;13:1765-1772. PubMed
- Ola Bratt. Prostatacancer. Internetmedicin [www]. [cited 2017-07-11]. länk
- Kuhnz W, Kulmann H, Fuhrmeister A. Investigation into the age-dependence of the pharmacokinetics of cyproterone acetate in healthy male volunteers. Eur J Clin Pharmacol. 1997;53:75-80. PubMed
- Ding W, Bishop ME, Pearce MG, Davis KJ, White GA, Lyn-Cook LE et al. Sex-specific dose-response analysis of genotoxicity in cyproterone acetate-treated F344 rats. Mutat Res Genet Toxicol Environ Mutagen. 2014;774:1-7. PubMed
- Gil M, Oliva B, Timoner J, Maciá MA, Bryant V, de Abajo FJ. Risk of meningioma among users of high doses of cyproterone acetate as compared with the general population: evidence from a population-based cohort study. Br J Clin Pharmacol. 2011;72:965-8. PubMed
- Läkemedelsstatistik. Stockholm: Socialstyrelsen. 2016 [cited 2017-06-20.] länk
Reviewed by: Mia von Euler
Approved by: Karin Schenck-Gustafsson