Drug Groups

approved; investigational

Description

An anti-androgen that, in the form of its acetate (cyproterone acetate), also has progestational properties. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females. [Pubchem]

Indication

For the palliative treatment of patients with advanced prostatic carcinoma.

Pharmacology

Cyproterone is an antiandrogen. 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).

Affected Organisms

Biotransformation

Primarily hepatic. Cyproterone acetate is metabolized by the CYP3A4 enzyme, forming the active metabolite 15beta-hydroxycyproterone acetate, which retains its antiandrogen activity, but has reduced progestational activity.

Absorption

Completely absorbed following oral administration.

Half Life

Elimination Following oral or intramuscular administration, the plasma half-life is 38 and 96 hours, respectively.

Elimination

It is excreted approximately 60% in the bile and 33% through the kidneys.

References

External Links