A fixed-dose combination tablet containing a low-dose anti-androgen (cyproterone acetate), a low-dose estrogen (ethinyl estradiol), and a high-dose folic acid supplement. Primarily used in the management of moderate to severe androgen-dependent conditions in women, such as acne, hirsutism, and female pattern hair loss, where oral contraceptives with anti-androgenic properties are indicated. The addition of folic acid is a unique feature in the Indian market, intended to address potential folate depletion associated with long-term hormonal therapy and to support general health, though its necessity in this combination is debated.
Adult: One tablet daily for 21 consecutive days, followed by a 7-day tablet-free interval. A withdrawal bleed usually occurs during this break. A new pack is started after the 7-day break, regardless of whether bleeding has stopped. For acne/hirsutism, treatment for at least 3-6 months is needed for initial response; long-term therapy may be required.
Note: Take at the same time each day, with or without food. If a tablet is missed, refer to specific patient leaflet instructions (generally, take missed pill as soon as remembered, and next pill at usual time; if >24 hours late, use backup contraception). Start on Day 1 of menstrual cycle or first Sunday after period begins.
Cyproterone acetate competitively inhibits the binding of dihydrotestosterone (DHT) to androgen receptors in target tissues (sebaceous glands, hair follicles). It also has potent progestogenic activity which suppresses the hypothalamic-pituitary-ovarian axis, reducing ovarian androgen production. Ethinyl estradiol increases Sex Hormone-Binding Globulin (SHBG), reducing free, biologically active testosterone. The combination provides effective ovulation inhibition. Folic acid acts as a cofactor in single-carbon transfer reactions essential for DNA synthesis, repair, and methylation.
Pregnancy: CONTRANDICATED (Category X). Must be discontinued immediately if pregnancy occurs. The folic acid component is beneficial for neural tube defect prevention, but the hormonal components are teratogenic risk. A pregnancy test is recommended before initiation.
Driving: Usually no effect. Patients experiencing dizziness, migraine, or visual disturbances should avoid driving.
| Enzyme Inducers (Rifampicin, Rifabutin, Phenytoin, Carbamazepine, Phenobarbital, St. John's Wort) | Markedly reduce plasma levels of hormonal components, leading to contraceptive failure and increased breakthrough bleeding. | Major |
| Antibiotics (e.g., Ampicillin, Tetracyclines) | Theorized to reduce enterohepatic recirculation of ethinyl estradiol, potentially reducing efficacy. Evidence is conflicting. | Moderate |
| Anticoagulants (Warfarin) | Ethinyl estradiol may reduce anticoagulant effect; monitor INR closely. | Major |
| Antidiabetics (Insulin, Oral agents) | Hormones may impair glucose tolerance; dose adjustment may be needed. | Moderate |
| Cyclosporine | Ethinyl estradiol may increase cyclosporine levels, risk of toxicity. | Major |
| Lamotrigine | Ethinyl estradiol significantly reduces lamotrigine levels, increasing seizure risk. | Major |
| Selegiline | Increased risk of hypertension when combined with ethinyl estradiol. | Moderate |
| Ascorbic Acid (High Dose) | May increase ethinyl estradiol plasma levels. | Minor |
| Methotrexate | Folic acid supplementation can reduce toxicity of methotrexate but also potentially its efficacy in conditions like rheumatoid arthritis (not used for cancer). | Major |
Same composition (Cyproterone (2mg) + Ethinyl Estradiol (0.035mg) + Folic Acid (5mg)), different brands: