-
Econazole
- indication:For topical application in the treatment of tinea pedis, tinea cruris, and tinea corporis caused by <i>Trichophyton rubrum</i>, <i>Trichophyton mentagrophytes</i>, <i>Trichophyton tonsurans</i>, <i>Microsporum canis</i>, <i>Microsporum audouini</i>, <i>Microsporum gypseum</i>, and <i>Epidermophyton floccosum</i>, in the treatment of cutaneous candidiasis, and in the treatment of tinea versicolor.
- pharmacologypharmacology:
- mechanism: Econazole interacts with 14-&alpha; demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.
- toxicity: Overdosage of econazole in humans has not been reported to date. In mice, rats guinea pigs and dogs, the oral LD 50 values were found to be 462, 668, 272, and > 160 mg/kg, respectively.
- absorprion: After topical application to the skin of normal subjects, systemic absorption of econazole nitrate is extremely low. Although most of the applied drug remains on the skin surface, drug concentrations were found in the stratum corneum which, by far, exceeded the minimum inhibitory concentration for dermatophytes.
- halflife:
- roouteelimination:
- volumedistribution:
- clearance: