Cyproterone Acetate + Ethinyl Estradiol

Cyproterone Acetate + Ethinyl Estradiol belongs to the oral contraceptive preparations and oral hormonal preparations for acne group. This preparation tablet is indicated for the treatment of women with severe acne, unresponsive to oral antibiotic and other available treatments, with associated symptoms of androgenization, including seborrhea and mild hirsutism. 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.

• Severe acne (unresponsive to oral antibiotics and other treatments)
• Seborrhea
• Mild hirsutism
• Associated symptoms of androgenization

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.

Cyproterone blocks androgen receptors and reduces androgen synthesis via negative feedback on the hypothalamo-pituitary-ovarian systems. Ethinylestradiol increases SHBG levels, reducing free circulating androgens. Together, they prevent ovulation and improve androgen-related conditions.

First Treatment Course: The patient is instructed to take 1 tablet daily for 21 consecutive days beginning on day 1 of her menstrual cycle. The tablets are then discontinued for 7 days (1 week).

Subsequent Courses: The patient begins her next and all subsequent 21-day course of tablets (following the same 21 days on, 7 days off) on the same day of the week that she began her first course.

Treatment should be continued for several months, since improvement may not be observed for at least 3 months. The drug should be discontinued 3 to 4 cycles after signs have completely resolved.

Take 1 tablet daily at the same time each day. Take the first tablet from the blister pack out of the section marked with the corresponding day of the week and swallow it with some liquid.

If the patient forgets to take a tablet at the usual time, the tablet may be taken within the next 12 hours. If more than 12 hours have elapsed, the missed tablet must be discarded and the remaining tablets continued at the usual time. A supplementary nonhormonal method of contraception must be employed until the pack is empty.

Common Side Effects:

• Bleeding
• Dizziness
• Depression
• Weight gain
• Headache
• Edema
• Breast pain
• Lactation
• Blood clot
• Gallstones

• Cigarette smoking increases the risk of serious adverse effects on the heart and blood vessels. Women over 35 years of age who smoke should not use this medication.
• Discontinue medication at the earliest manifestation of thromboembolic and cardiovascular disorders.
• Use with caution in patients with hypertension, diabetes, hyperlipidemia.
• Consult your doctor about discontinuing medication before surgery.
• Discontinue if migraine or new pattern of headache develops.

• Thrombophlebitis, thromboembolic disorders, or a history of these conditions
• Cerebrovascular disorders
• Myocardial infarction or coronary artery diseases
• Active liver disease or hepatic adenomas or carcinomas
• History of cholestatic jaundice
• Known or suspected carcinoma of the breast
• Known or suspected estrogen-dependent neoplasia
• Undiagnosed abnormal vaginal bleeding
• Any ocular lesion arising from ophthalmic vascular disease
• When pregnancy is suspected or diagnosed
• Previous or existing liver tumors
• Severe diabetes with vascular changes
• A history of otosclerosis with deterioration during pregnancy

Drugs that may reduce efficacy and increase breakthrough bleeding: Ampicillin, Analgesics, Antihistamines, Antimigraine preparations, Chloramphenicol, Griseofulvin, Isoniazid, Neomycin, Nitrofurantain, Penicillin V, Phenylbutazone, Sulfonamides and Tetracycline.

Anticoagulants: May reduce the anticoagulant effect.

Hepatic enzyme inducers (Carbamazepine, Phenobarbital, Phenytoin, Pyrimidine, Rifampicin): May reduce efficacy due to accelerated estrogen metabolism.

Vitamin C (ascorbic acid): May significantly increase plasma Ethinylestradiol levels.

Antidiabetic drugs: Dose adjustment may be required.

Can be taken with or without food. No specific information on alcohol interaction.

Pregnancy Category X. Unsafe during pregnancy. Fetal abnormalities have been reported in offspring of women who have taken estrogen/progestogen combinations in early pregnancy. Rule out pregnancy as soon as it is suspected.

Use during breastfeeding is not advisable. Hormonal components are excreted in breast milk and may reduce its quantity and quality.

No information on use in children and adolescents. Indicated only for adult women.

Not applicable for elderly women. Use in women over 35 years only in exceptional circumstances.

Avoid in severe liver or kidney disease. Use with caution in patients with history of liver disease.

There have been no reports of overdose with this tablet. There are no specific antidotes and treatment should be symptomatic.

Store below 30°C and in dry place. Protect from light. Keep out of reach of children.

Cyproterone Acetate + Ethinyl Estradiol