Contraception

Acne Products; Estrogen and Progestin Combination

Cyproterone:
Absorption: Oral: Complete
Metabolism: Hepatic; primary metabolite is 15beta-hydroxy-cyproterone acetate
Distribution: Vd: IM: 20.6 L/kg
Bioavailability: Oral: 88%
Half-life elimination: Oral: 38 ± 5 hours
Excretion: Feces (60%); urine (33%; mainly as unconjugated metabolites)
Ethinyl estradiol:
Absorption: Rapid
Bioavailability: 43% to 55%
Distribution: Vd: 2 to 4 L/kg
Protein binding: >95% to albumin
Metabolism: Hepatic via oxidation and conjugation in GI tract; hydroxylated via CYP3A4 to metabolites; first-pass effect; enterohepatic recirculation; reversibly converted to estrone and estriol
Half-life elimination: 19 to 24 hours
Excretion: Urine (as estradiol, estrone, and estriol); feces

Hypersensitivity to ethinyl estradiol, cyproterone, or any component of the formulation;
breast cancer or other estrogen- or progestin-dependent neoplasms;
history of or actual thrombophlebitis or thromboembolic disorders, cerebrovascular disorders, or myocardial infarction or coronary arterial disease;
severe diabetes with vascular changes;
hepatic tumors or disease;
history of cholestatic jaundice; pregnancy;
undiagnosed abnormal vaginal bleeding;
ocular lesions arising from ophthalmic vascular disease, such as partial or complete loss of vision or defect in visual fields;
history of otosclerosis with deterioration during pregnancy;
concomitant use with other estrogen/progesterone combinations or estrogens or progestins alone

X (All Trimesters)

Infant risk has been demonstrated.

Cardiovascular: Varicosity (3%), edema (2%) Central nervous system: Headache (5%), nervousness (4%), depression (3%), dizziness (1%) Dermatologic: Chloasma (4%) Endocrine & metabolic: Change in libido (3%) Gastrointestinal: Nausea (2%) Genitourinary: Dysmenorrhea (10%), breast tenderness (7%)