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Cyproterone information from DrugsUpdate  

See Available Brands of Cyproterone in India

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

Contraception

Adult: 2 mg daily (with 35 mcg of ethinylestradiol daily) for 21 days of the menstrual cycle. Start 1st treatment course on the 1st day of menstrual cycle; subsequent courses are started after 7 medication-free days following the preceding course. Withdraw treatment 3 or 4 cycles after condition has resolved. 

Oral

Hirsutism

Adult: 2 mg daily (with 35 mcg of ethinylestradiol daily) for 21 days of the menstrual cycle. Start 1st treatment course on the 1st day of menstrual cycle; subsequent courses are started after 7 medication-free days following the preceding course. Withdraw treatment 3 or 4 cycles after condition has resolved. 

Oral

Acne

Adult: 2 mg daily (with 35 mcg of ethinylestradiol daily) for 21 days of the menstrual cycle. Start 1st treatment course on the 1st day of menstrual cycle; subsequent courses are started after 7 medication-free days following the preceding course. Withdraw treatment 3 or 4 cycles after condition has resolved. 

Oral

Palliative treatment of prostatic carcinoma

Adult: Initially, 300 mg daily in 2-3 divided doses. Maintenance: 200-300 mg daily.

Oral

Hot flushes

Adult: 50 mg daily, may increase to 150 mg daily in 3 divided doses if needed. 

Oral

Libido in severe hypersexuality or sexual deviation

Adult: 50 mg bid.

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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