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Diane-35
Diane-35 is a combined oral medication containing cyproterone acetate (2 mg, an anti-androgenic progestin) and ethinylestradiol (35 µg, a synthetic estrogen). Primarily prescribed for severe acne and hirsutism in women, it also functions as an oral contraceptive. This article explores its pharmacology, clinical applications, and safety profile, referencing authoritative sources such as the BNF, Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.
Diane-35 exerts its effects through the synergistic actions of its two components:
- Cyproterone Acetate:
- Anti-Androgenic Activity: Competitively inhibits androgen receptors, reducing the effects of androgens like testosterone on sebaceous glands and hair follicles (Lippincott).
- Gonadotropin Suppression: Inhibits the release of luteinizing hormone (LH), decreasing ovarian androgen production.
- Ethinylestradiol:
- Estrogenic Effects: Suppresses follicle-stimulating hormone (FSH), preventing follicular development and ovulation.
- Sex Hormone-Binding Globulin (SHBG) Increase: Elevates SHBG levels, reducing free testosterone concentrations (Lange).
Together, these mechanisms address androgen-dependent conditions like acne and hirsutism while providing contraceptive efficacy.
- Severe Acne: Particularly effective in women with hormonal acne resistant to topical treatments (BNF).
- Hirsutism: Reduces excessive hair growth in androgen-dependent conditions like polycystic ovary syndrome (PCOS).
- Contraception: Provides reliable birth control when taken as directed.
- Standard Regimen: One tablet (2 mg cyproterone acetate + 35 µg ethinylestradiol) daily for 21 days, followed by a 7-day hormone-free interval. Restart on day 8, regardless of bleeding (BNF).
- Initiation: Begin on day 1 of menstruation or the first Sunday thereafter. Backup contraception is recommended for the first 7 days.
- Missed Dose: If delayed <12 hours, take immediately. If >12 hours, follow BNF guidelines: Take missed pill ASAP, continue the pack, and use backup contraception for 7 days.
- Common: Nausea, headache, breast tenderness, mood changes, and breakthrough bleeding.
- Serious:
- Venous Thromboembolism (VTE): Higher risk compared to levonorgestrel-containing pills (BNF).
- Cardiovascular Events: Increased risk in smokers >35 years or those with hypertension.
- Hepatic Effects: Rare hepatotoxicity, gallstones, or benign liver tumors (Lange).
- Hyperkalemia: Potential risk due to cyproterone’s mild anti-mineralocorticoid activity.
- Absolute Contraindications: History of VTE, arterial thrombosis, estrogen-dependent cancers, severe liver disease, undiagnosed vaginal bleeding, or migraine with aura (BNF).
- Relative Precautions: Obesity, diabetes, hypertension, or familial hyperlipidemia.
- Monitoring: Regular blood pressure checks, liver function tests, and screening for VTE risk factors (e.g., family history).
- Reduced Efficacy: Enzyme-inducing drugs (e.g., rifampicin, carbamazepine, St. John’s Wort) accelerate metabolism of ethinylestradiol, necessitating alternative contraception (BNF).
- Antibiotics: Limited evidence for interaction with broad-spectrum antibiotics (e.g., amoxicillin), but backup contraception is advised.
- Potassium-Sparing Drugs: Increased risk of hyperkalemia with ACE inhibitors, ARBs, or potassium-sparing diuretics (Lippincott).
- Active Ingredients: Cyproterone acetate (2 mg) and ethinylestradiol (35 µg).
- Brands: Marketed as Diane-35; generics may be labeled as cyproterone acetate/ethinylestradiol.
