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Cyproterone information from DrugsUpdate
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.
Pharmacodynamics
Cyproterone is a progestogen with anti-androgenic properties.
Pharmacokinetics
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.
Cyproterone Indications / Cyproterone Uses
In Contraception, Hirsutism, Acne, Palliative treatment of prostatic carcinoma, Hot flushes, Libido in severe hypersexuality or sexual deviation.
Cyproterone Adverse Reactions / Cyproterone Side Effects
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.
Special Precautions
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.
Other Drug Interactions
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.
Other Interactions
Efficacy may be reduced by alcohol. St John's wort may reduce the levels of cyproterone.
Dosage
Food(before/after)
Should be taken with food. (Take after meals.)
List of Contraindications
Cyproterone and Pregnancy
Caution when used during Pregnancy.
Cyproterone and Lactation
Caution when used during Lactation.
Storage
Oral: Store below 25°C.
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