Cyproterone Acetate (Diane 35®)

Drug Class

Anti-androgen; progestin

Dosage Forms

Oral: Tablets: Cyproterone acetate 2mg w/ ethinyl estradiol 35mcg Diane-35®

Diane-35®, Cyproterone acetate is not commonly used by itself to minimize hair growth.

Cyproterone acetate has been found useful in androgen-related dermatologic disorders, such as hirsutism and acne vulgaris. The anti-androgen activity is responsible for the decreased sebum excretion rate and the inhibition of hair growth. If used alone in women cyproterone leads to menstrual cycle disturbances which can be avoided when combined with ethinyl estradiol.

This combination is also an effective contraceptive. Diane-35® may be used in women who have persistent acne failing to respond to antibiotics, with associated symptoms of androgenization including seborrhea and hirsutism.

Patient Monitoring

Liver function tests every 6 months are recommended.

Drug Safety Information

• Contraindicated in patients with hepatic dysfunction or active liver disease.
• Avoid in those who birth control pills are contraindicated
• Much publicity has surrounded Diane-35® in regards to the suggested elevation of risk of thrombosis compared with other oral contraceptive pills. It would appear that close analysis of these risks suggest that this drug poses no greater threat than any other equivalent birth control pill.

Adverse Effects

Cutaneous effects may include dry skin, thrombophlebitis, photosensitivity, alopecia, and maculopapular rash.

Gastrointestinal effects may include nausea, vomiting, and hepatitis. Endocrine effects may include decreased libido, gynecomastia, impaired glucose metabolism and weight gain.

Other effects may include headache, fatigue and depression.

FDA Pregnancy Category X

Contraindicated during pregnancy and lactation. Feminization will occur in the male fetus.

Major Drug Interactions

Concurrent use of antihypertensive, benzodiazepines, beta-adrenergic blockers, corticosteroids, hypoglycemic and tricyclic antibiotics may alter their efficacy; anticoagulant effect may be reduced; ampicillin, analgesics, antihistamines, chloramphenicol, penicillin and tetracyclines may reduce contraceptive efficacy.

Mechanism of Action / Pharmacokinetics

Cyproterone acetate blocks androgen receptors and reduces androgen synthesis through negative feedback on the hypothalamo-pituitary-gonadal axis. The antiandrogen activity is thought to lead to decreased hair growth as well reduce sebum production.

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