Clotrimazole
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Clotrimazole
Lotrimin, Mycelex, Gyne-Lotrimin; OTC widely
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Summary
Common uses
Tinea pedis0, Tinea corporis / cruris0, Cutaneous candidiasis0, Vulvovaginal candidiasis0, Oropharyngeal candidiasis (troche)0
Pharmacy
Starting dose
Topical: 1% cream BID × 2-4 weeks; vaginal: 1% or 2% cream nightly × 7 days, or 100/200/500 mg vaginal tablet single or 3-day regimens; troche: 10 mg PO five times daily × 2 weeks for thrush
Preparations
1% topical cream, lotion, solution; 1%, 2% vaginal cream; 100, 200, 500 mg vaginal tablets; 10 mg oral troches; combination with betamethasone (Lotrisone, Rx)
US FDA Max
Topical: BID; troche: 5×/day
Pharmacology
Routes
Topical, vaginal, oral troche
Onset
Days
Duration
Hours per application
Half-life
Not meaningfully described (minimal systemic absorption from topical use)[1]
Bioavailability
Topical: minimal systemic; troche: ~3% systemic[1]
Pregnancy
Topical and vaginal generally considered safe; widely used.[citation needed]
Legal status
OTC (lower strengths) and Rx-only (combination with betamethasone) in US
Purported mechanism
Clotrimazole is an imidazole antifungal that inhibits fungal cytochrome P450 14α-demethylase (CYP51), blocking ergosterol biosynthesis and disrupting fungal cell membrane integrity.0 Active against dermatophytes (Trichophyton, Microsporum, Epidermophyton), Candida species, Malassezia, and some gram-positives at high concentrations. Topical use largely avoids the CYP-mediated drug interactions and hepatotoxicity that limit oral ketoconazole[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Lotrimin AF (clotrimazole) OTC monograph, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/017812s041lbl.pdf