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GENITO URINARY SYSTEM AND SEX HORMONES › GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS › ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS › Imidazole derivatives
combinations of imidazole derivatives
G01AF20
Forms & Strengths
- Vaginal suppositories / ovules: clotrimazole 100 mg, 200 mg, 500 mg; miconazole 100 mg, 200 mg; metronidazole combinations vary
- Vaginal cream: 2%, 10% (clotrimazole); 2% (miconazole)
- Oral tablets/capsules: various imidazole combinations depending on specific multi-ingredient formulations
Adult Dosing
- Vulvovaginal candidiasis (Clotrimazole): 100 mg vaginal tablet daily for 7 days, or 200 mg for 3 days, or 500 mg single dose
- Vulvovaginal candidiasis (Miconazole): 100 mg suppository daily for 7 days, or 200 mg for 3 days, or 1200 mg single dose
- Bacterial vaginosis / Mixed vaginitis (Metronidazole + Miconazole combinations): 1 application intravaginally daily for 7 days
Pediatric Dosing
- Safety and efficacy in post-menarcheal adolescents generally follow adult dosing guidelines
- Not recommended for prepubescent children unless specifically directed by a pediatric specialist
Indications
- Treatment of vulvovaginal candidiasis
- Treatment of bacterial vaginosis
- Management of mixed vaginal infections involving fungi and anaerobic bacteria
Mechanism of Action
- Imidazoles (e.g., clotrimazole, miconazole): Inhibit fungal cytochrome P450-dependent enzyme 14-alpha-demethylase, halting ergosterol synthesis and increasing fungal cell membrane permeability
- Metronidazole (when combined): Disrupts DNA synthesis in anaerobic bacteria and protozoa by reduction of its nitro group
Contraindications
- Hypersensitivity to imidazole derivatives or any component of the formulation
- First trimester of pregnancy (for systemic or specific metronidazole-containing vaginal products, per product labeling)
- Concurrent use with alcohol or disulfiram (if systemic metronidazole component is present)
Adverse Reactions
- Local vulvovaginal burning, irritation, itching, or stinging
- Pelvic cramps or abdominal discomfort
- Headache and nausea (systemic absorption dependent)
- Hypersensitivity reactions including rash and urticaria
Drug Interactions
- Latex or rubber products (vaginal creams and suppositories may damage condoms and diaphragms)
- Oral anticoagulants (warfarin): Potential enhancement of the anticoagulant effect with systemic absorption of topical imidazoles
- Alcohol: Disulfiram-like reaction possible if formulation contains metronidazole and systemic absorption occurs
Curated Content: Needs Vetting Before Put to Clinical Use