Fluconazole

Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC₉₉s range from 0.20 μg/mL to 0.39 μg/mL^[1]. In Vitro: Fluconazole inhibits 4 species ofAspergillus fumigatus with the IC₅₀s of 23.9-43.5 μg/mL. Fluconazole (0.20 μg/mL) inhibits significantly the mycelial-phase growth and germ tube elongation of C. albicans in a medium supplemented with serum^[1].
Fluconazole is a triazole antifungal agent that has been available for the treatment of infections due to Candida, Cryptococcus. The MIC₉₀ is highest for C. krusei (MIC ≥ 64 μg/mL) and C. glabrata (MIC, 32 μg/mL) and is ≤2 μg/mL for C. albicans (0.5 μg/mL), C. parapsilosis (2 μg/mL), C. tropicalis (2 μg/mL), C. lusitaniae (2 μg/mL), and C. kefyr (0.5 μg/mL)^[2].
Fluconazole (0.1-50.0 μg/mL) damages the fungal cells and reduces their viability^[3].
In Vivo: Fluconazole ( 0, 0.5, 1, 2.5, 5, 7.5, and 10 mg/kg; administered intraperitoneally (i.p.) as a single dose) results in a 50% reduction in fungal densities (ED50) of 4.87 mg/kg in a murine model of systemic candidiasis^[4]. Fluconazole exhibits terminal elimination half-life of 2.4 h) following i.p. administration.The terminal half-life does not change with the dose of fluconazole administered^[4].