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Antimyzetische Aktivität des neuen Azols UK‐109, 496 (Voriconazol)
Author(s) -
Kappe R.
Publication year - 1999
Publication title -
mycoses
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.13
H-Index - 69
eISSN - 1439-0507
pISSN - 0933-7407
DOI - 10.1111/j.1439-0507.1999.tb00019.x
Subject(s) - voriconazole , blastomyces dermatitidis , microbiology and biotechnology , fluconazole , candida glabrata , candida albicans , aspergillosis , cryptococcus neoformans , amphotericin b , coccidioides immitis , azole , candida krusei , biology , medicine , immunology , blastomycosis , antifungal
Summary The in vitro activity of voriconazole fully includes Aspergillus , and also emerging moulds like Fusarium, Pseudallescheria boydii , and Penicillium marneffei . The minimal inhibitory concentrations of voriconazole for Candida krusei and Candida glabrata , which are resistant or less susceptible to fluconazole, promise clinical efficacy, although they are ten times higher (0.30–0.39 μ g/ml) than those for Candida albicans and other Candida spp. (0.001–0.05 μ g/ml). The endemic fungal pathogens Histoplasma capsulatum, Coccidioides immitis, Blastomyces dermatitidis, Paracoccidioides brasiliensis , as well as Cryptococcus neoformans , and the dermatophytes are also fully susceptible to voriconazole. The zygomycetes and Sporothrix schenckii remain a problem. Voriconazole has been shown to be effective against invasive aspergillosis (IA) and fluconazole‐resistant candidosis in animal models, when administered in doses between 2.5 and 45 mg/kg/day. The pharmacokinetics of voriconazole in man produced sustained high blood and tissue levels following oral and intravenous applications of 50 to 200 mg/day. Side effects included fully reversible mild to moderate visual disturbances (8 to 44 %) and raised liver function enzymes (6 to 8 %). In conclusion, voriconazole is highly active against Aspergillus and most other medically relevant fungi, it is applicable intravenously, and it appears to have an acceptable safety profile.