chapter  27
4 Pages

Fluconazole

WithJames L. Schardein, Orest T. Macina

Fluconazole is a synthetic triazole chemical used therapeutically as an antifungal drug, given orally for the treatment of vaginal candidiasis, or given parenterally at higher doses for other mycotic infections or for other drug-resistant organisms. It acts by interfering with cytochrome P450 activity, decreasing ergosterol synthesis, and inhibiting cell membrane formation. The drug is available by prescription as Diflucan® or as several other trade names. Fluconazole has a pregnancy category of C. Indicated on the package label is that fluconazole in the rat at oral doses in the range of 80 to 320 mg/kg/day during organogenesis resulted in cleft palate, wavy ribs, and abnormal craniofacial ossification, all teratogenic responses; embryolethality was also recorded, and developmental variations were observed at lower doses of 25 mg/kg/day and higher. The usual therapeutic doses of fluconazole inhumans recommended range from 150 to 800 mg/day depending upon the seriousness of the infection.