Name: Fluconazole (Diflucan)
Class: Antifungal (Triazole)
Mech.: Inhib. fungal cyt. P450 and sterol C-14 a-demethylation. Normal sterols depleted, 14-a-methyl sterols build up ® fungistatic.
Absorption: Oral absorption @ IV absorption (rare phenom.)
Distribution: Low plasma protein binding. Vd close to total body water. Good saliva, good CSF (~80%), conc. in urine and skin.
Metab.:
Excretion, t½: 80% appears in urine unchanged. Excreted in milk. 30 hr.
Toxicity/S.E.s: Rare hepatotoxicity. Rare exfoliative skin disorders (can be fatal). GI irritation, rash. Affects rat fetal development. Increases metabolite levels of some terfenadine metabolits (not terf. itself). May slow metab. of long-acting antihistamines and cyclosporines.
Utility: Candidiasis (oropharyngeal, esophageal, UTI, vaginal, systemic), Cryptococcal meningitis in AIDS patients and otherwise healthy patients. Coccidiodal meningitis. Chronic suppresion of Crypt. meningitis in AIDS patients. Single-dose therapy for vaginal yeast infections.
Special Features: Oral absorption @ IV absorption. Only causes minor changes in plasma testosterone and corticosteroid concentrations.