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The in vivo antifungal activity of broad‐spectrum azoles
Author(s) -
van Cutsem Jan,
van Gerven Frans
Publication year - 1986
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430080135
Subject(s) - ketoconazole , miconazole , itraconazole , pharmacology , aspergillosis , potency , medicine , in vivo , mycosis , antifungal , amphotericin b , broad spectrum , chemistry , dermatology , biology , in vitro , immunology , biochemistry , microbiology and biotechnology , combinatorial chemistry
The antifungal activities (topical and oral) of miconazole, ketoconazole, and itraconazole were compared in laboratory animals. Miconazole at concentrations of 1 and 2% was an effective antifungal agent in the topical therapy of microsporosis and at 2% in vaginal candidosis. Ketoconazole was superior to miconazole in potency and efficacy, a concentration of 1% producing a 100% cure. With itraconazole the same efficacy was reached as with ketoconazole but at concentrations 4 to 8 times lower. Miconazole, administered orally, was marginally active in dermatophytosis and, after long‐term treatment, in candidosis. In contrast, ketoconazole was found to be a broad‐spectrum antifungal agent of high efficacy at 10 mg/kg. Itraconazole again was more potent (doses 1.25 to 2.50 mg/kg) and more effective than ketoconazole in dermatophytosis, candidosis, and mycoses due to dimorphic fungi. Moreover, itraconazole constitutes an important therapeutic progress in the oral treatment of aspergillosis and cryptococcosis. The three compounds were free of side effects in the present experimental conditions.