Cyproterone Acetate

What it is and how it works

Cyproterone acetate competitively blocks androgen receptors in target tissues and, through its progestogenic activity, suppresses gonadotrophin secretion and thus testosterone production.

Indications

Palliative treatment of prostate cancer (including suppression of the flare with GnRH agonists); control of hypersexuality and sexual deviation in men; in women, severe androgenisation such as hirsutism and androgenic alopecia when other treatments are unsuitable.

Dosage and administration (summary)

Prostate cancer: typically 200–300 mg daily in divided doses after food; hypersexuality in men: usually 50 mg twice daily. Doses in women are lower and given cyclically with an oestrogen; treatment should use the lowest effective dose.

Contraindications

Hepatic disease, existing or previous meningioma, history of thromboembolic disease, severe diabetes with vascular changes, sickle-cell anaemia, severe chronic depression and (except in prostate cancer) malignant tumours; adolescents before completion of bone maturation.

Warnings and precautions

Dose-related hepatotoxicity, including hepatitis and hepatic failure, has been reported; monitor liver function. Risk of meningioma increases with cumulative dose, so high-dose use is restricted to cases where alternatives are unsuitable. May cause thromboembolism, adrenocortical suppression, depression and fatigue impairing driving.

Pregnancy

Contraindicated in pregnancy because of the risk of feminisation of the male fetus.

Storage and supply

Store below 25 °C.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.