Ketoconazole is a time-honored imidazole that has demonstrated in vitro activity against many fungal pathogens. In vitro antifungal testing and corneofungimetry have demonstrated that ketoconazole compared favorably with regard to other imidazoles and antifungals of other classes. Its activity after topical applications on various dermatomycoses and seborrheic dermatitis has also been shown and confirmed over the years.
In vivo controlled, randomized, double blind trials were also performed with topical ketoconazole on healthy volunteers after induction of erythema, and in patients with seborrheic dermatitis. Biometrological methods were used for assessing the changes in erythema (E index – spectrophotometry) and in the skin barrier function (TEWL, transepidermal water loss). Ketoconazole exhibited anti-inflammatory effects and somewhat boosted the rate of normalization of the weakened stratum corneum barrier function.
In sum, topical ketoconazole exhibits a powerful in vivo antifungal activity combined with a clinically relevant anti-inflammatory effect. The 2% drug formulations are useful for treating superficial dermatomycoses. The 1% cosmetic formulations were designed for controlling Malassezia-driven skin disorders.
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