Add time:08/31/2019         Source:sciencedirect.com

Fluconazole is a triazole antifungal agent available for oral or intravenous use in the treatment of a number of localized and disseminated mycoses. Animal models have shown in vivo activity against infections caused by Candida spp. and Crytococcus neoformans. Fluconazole is also active in animal infections caused by Blastomyces dermatitidis, Coccidioides immitis, Histoplasma capsulatum, and dermatophytes. Fluconazole acts by inhibiting synthesis of ergosterol, an essential sterol in fungal cell membranes. The drug is water-soluble, rapidly absorbed after oral dosing, and penetrates well into body fluids and tissues, including cerebrospinal fluid. It is excreted largely unchanged in urine and has an elimination half-life of approximately 30 h, allowing once-daily dosing. Extensive clinical trials document clinical efficacy in candidiasis — including oropharyngeal, esophageal, and disseminated forms — as well as in acute or suppressive therapy of cryptoccal meningitis. Other potential indications studied include prophylaxis of fungal infection in immunocompromised cancer patients, treatment of coccidioidal meningitis, and single-dose therapy of vaginal candidiasis. Fluconazole is generally well tolerated and infrequently associated with serious adverse effects or laboratory test abnormalities.

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