Topical antifungal and anti-inflammatory.
In vitro studies suggest that ketoconazole impairs the synthesis of ergosterol, which is a vital component of fungal cell membranes.
Microbiology: Ketoconazole is broad-spectrum synthetic antifungal agent which inhibits the growth of the following common dermatophytes and yeasts by altering the permeability of the cell membrane.
Dermatophytes: Trichophyton rubrum, T. mentagrophytes, T. tonsurans, Microsporum canis, M. audouini, M. gypseum and Epidermophyton floccosum; yeasts: Candida albicans and C. tropicalis; and the organism responsible for tinea versicolor, Malassezia furfur (Pityrosporum orbiculare). Development of resistance to ketoconazole has not been reported.
Pharmacokinetics: When Nizoral (ketoconazole) 2% Cream was applied dermally to intact or abraded skin of Beagle dogs for 28 consecutive days at a dose of 80 mg, plasma concentrations did not significantly differ from the lower detection limit (2 ng/mL) of the method employed. After a single topical application to the chest, back and arms of normal volunteers, systemic absorption of ketoconazole was not detected at the 5 ng/mL level in blood over a 72-hr period.
Two dermal irritancy studies, a human sensitization test, a phototoxicity study and a photoallergy study conducted in 38 male and 62 female volunteers showed no contact sensitization of the delayed hypersensitivity type, no irritation, no phototoxicity and no photoallergenic potential due to Nizoral Cream.