This is indicated in Acne, Contraception, Hirsutism, Prostatic carcinoma, Libido, Hot flushes
Oral Contraceptive preparations, Oral Hormonal preparations for Acne
Cyproterone is a steroid compound with potent antiandrogenic, progestogenic and antigonadotrophic activity. It exerts its antiandrogenic effect by blocking androgen receptors. It also reduces androgen synthesis by a negative feedback effect on the hypothalamo-pituitary-ovarian systems. The estrogen component (Ethinylestradiol) increases levels of sex hormone binding globulin (SHBG) and thus reduces the free circulating plasma levels of androgens. Cyproterone has no tendency to reduce SHBG levels.
If used alone in women,Cyproterone leads to menstrual cycle disturbances which are avoided when combined with Ethinylestradiol. When this tablet is administered in a cyclic manner, it has the added effect of preventing ovulation and possible conception.
The components of this tablet are rapidly absorbed after oral administration. Due to the long terminal half-life of Cyproterone, a 4-fold increase in plasma levels occurs after 6 to 12 days of daily dosing. Long-term therapy (36 months) with this product did not have a significant influence on lipid metabolism. A trend to increase plasma cholesterol and triglyceride levels was observed. There was a slight decrease in low density lipoprotein (LDL) with a simultaneous increase in high density lipoprotein (HDL).
Acne, Contraception, Hirsutism: 2 mg/day (with ethinylestradiol) for 21 days of the menstrual cycle. Palliative treatment for prostatic carcinoma: Initial: 300 mg/day in 2-3 divided doses. Maintenance: 200-300 mg/day. Control of libido: 50 mg twice daily. Hot flushes 50 mg/day, may increase to 150 mg/day in 3 divided doses if needed.
Concurrent use of the following drugs may result in reduced efficacy of this tablet and increased incidence of breakthrough bleeding: Ampicillin, Analgesics, Antihistamines, Antimigraine preparations, Chloramphenicol, Griseofulvin, Isoniazid, Neomycin, Nitrofurantain, Penicillin V, Phenylbutazone, Sulfonamides and Tetracycline.
Concurrent use of anticoagulants with estrogen/progestogen combinations may reduce the anticoagulant effect. Effectiveness of the following drugs may be altered when used concurrently: Antihypertensive, Benzodiazepines (those that undergo oxidative degradation), Beta-adrenergic blockers,Caffeine, Corticosteroids, Hypoglycemic, Phenothiazine, Theophylline, Tricyclic antidepressants and Vitamins.
Concurrent use of the following drugs may reduce the efficacy of this tablet because of accelerated estrogen metabolism caused by the induction of hepatic enzymes: Carbamazepine, Phenobarbital, Phenytoin, Pyrimidine and Rifampicin.
Diabetics using estrogen/progestogen combinations may require adjustment of their antidiabetic medication. Concurrent administration of vitamin C (ascorbic acid) with estrogen/ progestogen combinations has been reported to result in a significant rise in plasma Ethinylestradiol levels.
Rule out pregnancy before treatment is begun. Because of the antiandrogenic action of this tablet,feminization of male fetuses has occurred in animal studies and may possibly occur in humans.
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. 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.
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.
Pregnancy Category X. Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh potential benefits.
Symptoms and Treatment:There have been no reports of overdose with this tablet. There are no specific antidotes and treatment should be symptomatic, based on the knowledge of the pharmacological action of the constituents.
Store below 30°C and in dry place. Protect from light. Keep out of the reach of children.
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