Cyproterone Acetate + Ethinylestradiol

Cyproterone Acetate + Ethinylestradiol is a combination of two hormonal medicines: Cyproterone and Ethinyl Estradiol which treats PCOS symptoms such as acne, excessive hair growth (hirsutism) and irregular periods. Cyproterone works by blocking the overproduction of androgens (male hormones) in the ovaries, thereby reducing unwanted hair growth and acne. Ethinyl Estradiol enhances the effect of Cyproterone by reducing the amount of androgens in the blood. Together, they also regularize the menstrual cycle in PCOS. This preparation tablet is also 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.

• Polycystic Ovary Syndrome (PCOS)
• 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 including PCOS symptoms.

Adult - PCOS, Hirsutism, Acne: 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.

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. Do not chew, crush or break it.

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:

• Nausea
• Stomach pain
• Headache
• Weight gain
• Breast pain
• Mood changes
• Bleeding/Spotting
• Dizziness
• Depression
• Edema
• Lactation
• Blood clot
• Gallstones

• Take your pill at the same time every day to help you remember to take it.
• Do not use if you are obese, over 50, smoke, on prolonged bed rest or have a history of blood clots.
• Stop taking it and inform your doctor if you notice unexplained swelling and pain in your limbs, shortness of breath, chest pain or changes in vision.
• If you experience vaginal spotting or breakthrough bleeding, inform your doctor if it lasts longer.
• If your period fails to come within a week after completing your course, do not start the next course before consulting your doctor.
• Cigarette smoking increases the risk of serious adverse effects on the heart and blood vessels.

• 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 years
• Pregnancy

CYP3A4 inhibitors (ketoconazole, itraconazole, clotrimazole, ritonavir): May reduce metabolism.

CYP3A4 inducers (rifampicin, phenytoin): May reduce cyproterone levels.

CYP1A2 and CYP3A4 inducers (aminoglutethimide, carbamazepine, phenobarbital, rifampin): May decrease estradiol effects.

Hydrocortisone and prednisolone: May enhance effects.

Dicoumarol: Altered anticoagulant effect.

Potentially Fatal: Antibiotics (ampicillin, tetracycline, sulphonamides and chloramphenicol) can cause intermenstrual bleeding or failure of contraception.

Antihypertensives or hypoglycaemic drugs: Reduced efficacy.

Caution is advised when consuming alcohol. Please consult your doctor. Can be taken with or without food.

Pregnancy Category X. Cyproterone Acetate + Ethinylestradiol is highly unsafe during pregnancy. Studies on pregnant women and animals have shown significant harmful effects to the developing baby. Seek your doctor's advice.

Cyproterone Acetate + Ethinylestradiol is probably unsafe during breastfeeding. Limited human data suggests that the drug may pass into the breastmilk and harm the baby.

Contraindicated in youths below 18 years of age.

Avoid use in women over 50 years of age.

Renal impairment: Limited information available on the use in patients with kidney disease. Please consult your doctor.

Hepatic impairment: Limited information available on the use in patients with liver disease. Please consult your doctor.

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 + Ethinylestradiol