Cyproterone Acetate + Ethinylestradiol
Indications
Cyproterone Acetate + Ethinylestradiol is used for:
Acne, Contraception, Hirsutism, Prostatic carcinoma, Libido, Hot flushes
Adult Dose
Oral
Contraception; Hirsutism; Acne
Adult: 2 mg daily (with 35 mcg of ethinylestradiol daily) for 21 days of the menstrual cycle. Start 1st treatment course on the 1st day of menstrual cycle; subsequent courses are started after 7 medication-free days following the preceding course. Withdraw treatment 3 or 4 cycles after condition has resolved.
Child Dose
Renal Dose
Administration
Should be taken with food. Take after meals.
Contra Indications
Markedly impaired liver function or cholestasis; Dubin-Johnson or Rotor syndrome, hepatic adenoma; malignant or wasting diseases; severe chronic depression; severe diabetes with vascular changes; sickle-cell anaemia; history of thromboembolic disorders; renal impairment. Youths <18 yr.
Precautions
Prostate cancer, hepatic impairment, DM, history of depression, familial defects in lipoprotein metabolism, CV diseases. Monitor LFT, adrenocortical function, LDL and HDL levels, and RBC count during treatment. In women: Interrupt treatment if persistent or recurrent bleeding occurs to exclude the possibility of organic diseases. May increase risk of thrombo-embolic diseases. Ineffective for male hypersexuality in chronic alcoholism. May impair ability to drive or operate machinery. Pregnancy, lactation.
Pregnancy-Lactation
Interactions
Metabolism may be reduced by inhibitors of CYP3A4 e.g. ketoconazole, itraconazole, clotrimazole, ritonavir. Inducers of CYP3A4 e.g. rifampicin, phenytoin may reduce the levels of cyproterone.
CYP1A2 and CYP3A4 inducers such as aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together. Altered anticoagulant effect when used with dicoumarol.
Potentially Fatal: Antibiotics (ampicillin, tetracycline, sulphonamides and chloramphenicol) can cause intermenstrual bleeding or failure of contraception. Reduced efficacy of antihypertensives or hypoglycaemic drugs.
Adverse Effects
Side effects of Cyproterone Acetate + Ethinylestradiol :
Inhibits spermatogenesis, reduces volume of ejaculate, causes infertility, produces abnormal spermatozoa, gynecomastia and enlargement of mammary glands; galactorrhoea and benign nodules. Depressive mood changes. Alterations in hair pattern, skin reactions. Fatigue and lassitude, breathlessness, wt changes.
Mechanism of Action
Cyproterone is a progestogen with anti-androgenic properties.Oestradiol is the major oestrogen in pre-menopausal women. Ethinylestradiol has similar actions as oestradiol. It is responsible for the development and maintenance of female reproductive system and secondary sexual characteristics. It also inhibits anterior pituitary by negative feedback effect and causes capillary dilation, fluid retention and protein anabolism.