P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *
Cyproterone acetate is an antiandrogen i.e., it suppresses the actions of testosterone (and its metabolite dihydrotestosterone on tissues). It acts by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels). Its main indications are prostate cancer, benign prostatic hyperplasia, priapism, hypersexuality and other conditions in which androgen action maintains the disease process.
Cyproterone is a progestogen with anti-androgenic properties.
Absorption: Oral admin: Rapid and complete; plasma concentrations peak in 3-4 hr.
Distribution: 96% bound to plasma proteins.
Metabolism: Hepatically metabolised.
Excretion: Urine: About 35% of a dose is excreted as free and conjugated metabolites; the remainder excreted in bile.
In Contraception, Hirsutism, Acne, Palliative treatment of prostatic carcinoma, Hot flushes, Libido in severe hypersexuality or sexual deviation.
Inhibits spermatogenesis, reduces volume of ejaculate, causes infertility, produces abnormal spermatozoa, gynecomastia and enlargement of mammary glands; galactorrhoea and benign nodules. Depressive mood changes. Alterations in hair pattern, skin reactions. Fatigue and lassitude, breathlessness, wt changes.
Prostate cancer, hepatic impairment, DM, history of depression, familial defects in lipoprotein metabolism, CV diseases. Monitor LFT, adrenocortical function, LDL and HDL levels, and RBC count during treatment. In women: Interrupt treatment if persistent or recurrent bleeding occurs to exclude the possibility of organic diseases. May increase risk of thrombo-embolic diseases. Ineffective for male hypersexuality in chronic alcoholism. May impair ability to drive or operate machinery. Pregnancy, lactation.
Metabolism may be reduced by inhibitors of CYP3A4 e.g. ketoconazole, itraconazole, clotrimazole, ritonavir. Inducers of CYP3A4 e.g. rifampicin, phenytoin may reduce the levels of cyproterone.
Efficacy may be reduced by alcohol. St John's wort may reduce the levels of cyproterone.
Should be taken with food. (Take after meals.)
Caution when used during Pregnancy.
Caution when used during Lactation.
Oral: Store below 25°C.