Apo-cyproterone - General Information
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]
Pharmacology of Apo-cyproterone
Apo-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).
Additional information about Apo-cyproterone
Apo-cyproterone Indication: For the palliative treatment of patients with advanced prostatic carcinoma.
Mechanism Of Action: The direct antiandrogenic effect of cyproterone is blockage of the binding of dihydrotestosterone to the specific receptors in the prostatic carcinoma cell. In addition, cyproterone exerts a negative feed-back on the hypothalamo-pituitary axis, by inhibiting the secretion of luteinizing hormone resulting in diminished production of testicular testosterone.
Drug Interactions: Not Available
Food Interactions: Take after a meal.
Generic Name: Cyproterone
Synonyms: Cyproterone acetate
Drug Category: Androgen Antagonists
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Cyproterone: Androcur; Apo-cyproterone; Gen-Cyproterone; Novo-cyproterone; CyPat;
Absorption: Completely absorbed following oral administration.
Toxicity (Overdose): Not Available
Protein Binding: Not Available
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.
Half Life: Elimination Following oral or intramuscular administration, the plasma half-life is 38 and 96 hours, respectively.
Dosage Forms of Apo-cyproterone: Liquid Intramuscular
Chemical IUPAC Name: Not Available
Chemical Formula: C22H27ClO3
Cyproterone on Wikipedia: http://en.wikipedia.org/wiki/Cyproterone
Organisms Affected: Humans and other mammals