Products
Cyproterone acetate is commercially available in the form of dragées in combination with ethinyl estradiol (generics). The drug has been approved in many countries since 1987. This article refers to the original Diane-35 and corresponding generics. Other drugs containing cyproterone acetate are available for other indications. Bayer’s original Diane-35 goes off the market in many countries in December 2021. Alternatives are im available.
Structure and properties
Cyproterone acetate (C24H29ClO4, Mr = 416.9 g/mol) exists as a white crystalline powder that is practically insoluble in water.
Effects
Cyproterone acetate (ATC G03HB01) has contraceptive and antiandrogenic properties. The contraceptive effect is mainly due to inhibition of ovulation and changes in cervical secretions. In addition, the conditions for implantation of the egg in the endometrium are worsened.
Indications
For the treatment of masculinization symptoms in women such as acne (resistant to other therapies), increased sebum production, increased hairiness, and hair loss if contraception is desired at the same time. The combination must not be used for contraception if no masculinization symptoms are present at the same time!
Dosage
According to the professional information. The dragées are taken once daily at the same time of day for 21 consecutive days. This is followed by a break from taking the drug for one week, during which withdrawal bleeding usually begins.
Contraindications
Numerous precautions must be observed during treatment.
Interactions
Both agents are metabolized by CYP3A4, and corresponding drug-drug interactions with CYP inhibitors and inducers are possible. Other interactions have been described with antibiotics.
Adverse effects
The most common possible adverse effects include weight gain, skin rash, headache, chest tightness, breast pain, depressed mood, nausea, and indigestion. As with other birth control pills, serious cardiovascular conditions such as venous thrombosis, pulmonary embolism, stroke, and heart attack may rarely occur.
