Pharmacology: Pharmacodynamics: Ethinyl estradiol: Estrogen is responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens modulate the pituitary secretion of gonadotropins, luteinizing hormones, and follicle-stimulating hormone through a negative feedback system. Estrogen increases levels of sex hormone-binding globulin (SHBG) and may reduce unbound androgen levels. Ethinyl estradiol is a synthetic derivative of estradiol. The addition of the ethinyl group prevents rapid degradation by the liver.
Cyproterone: Steroid compound with anti-androgenic, anti-gonadotropic and progestin-like activity.
Pharmacokinetics: Cyproterone: Cyproterone acetate is completely absorbed. Cyproterone is metabolized by liver. Half-life elimination is 38 hours (range 33-43 hours). Time to peak is 3-4 hours and excreted in feces (60%) and urine (33%).
Ethinyl estradiol: Estradiol is well absorbed from the gastrointestinal tract, mucous membranes, and the skin. It is widely distributed with high concentrations in the sex hormone target organs. Ethinyl estradiol is bound to sex hormone-binding globulin and albumin. Ethinyl estradiol is partially lipid metabolized by CYP3A4 hepatic enzymes. Oral estradiol also undergoes enterohepatic recirculation by conjugation in the liver. Estradiol is excreted in urine.
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