Cyproterone Acetate + Ethinyl Estradiol

Innovator's Monograph


This is indicated in Acne, Contraception, Hirsutism, Prostatic carcinoma, Libido, Hot flushes

Therapeutic Class

Oral Contraceptive preparations, Oral Hormonal preparations for Acne


Cyproterone is a progestogen with anti-androgenic properties.Oestradiol is the major oestrogen in pre-menopausal women.

Ethinylestradiol has similar actions as oestradiol. It is responsible for the development and maintenance of female reproductive system and secondary sexual characteristics. It also inhibits anterior pituitary by negative feedback effect and causes capillary dilation, fluid retention and protein anabolism.

Dosage & Administration

Acne, Contraception, Hirsutism: 2 mg/day (with ethinylestradiol) for 21 days of the menstrual cycle.

Palliative treatment for prostatic carcinoma: Initial: 300 mg/day in 2-3 divided doses. Maintenance: 200-300 mg/day.

Control of libido: 50 mg twice daily. Hot flushes 50 mg/day, may increase to 150 mg/day in 3 divided doses if needed.


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.

CYP1A2 and CYP3A4 inducers such as aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together. Altered anticoagulant effect when used with dicoumarol.

Potentially Fatal: Antibiotics (ampicillin, tetracycline, sulphonamides and chloramphenicol) can cause intermenstrual bleeding or failure of contraception. Reduced efficacy of antihypertensives or hypoglycaemic drugs.


Markedly impaired liver function or cholestasis; Dubin-Johnson or Rotor syndrome, hepatic adenoma; malignant or wasting diseases; severe chronic depression; severe diabetes with vascular changes; sickle-cell anaemia; history of thromboembolic disorders; renal impairment. Youths <18 yr.

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.

Pregnancy & Lactation

Pregnancy Category X. Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh potential benefits.


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.

Available Brand Names