Review of fluconazole: a new triazole antifungal agent.

Fluconazole is a new triazole antifungal agent with unique pharmacokinetic properties. It can be administered orally or parenterally and achieves rapid distribution by either route, and its absorption is not affected by the presence of food. It has a plasma half-life of approximately 25-30 hr and approximately 70% of dose is excreted in the urine unchanged. There is linearity of fluconazole plasma concentrations over the dose range and the elimination rate is independent of dose. No effect has been seen on basal or ACTH-stimulated cortisol or on testosterone, estrogen, progesterone, or other steroid hormones, and there is no interaction with an oral contraceptive. No interaction with concomitantly administered cyclosporine has been documented, and there are no clinically significant differences in absorption when fluconazole is given in the presence or absence of cimetidine or food. Patients who are concomitantly receiving coumarin anticoagulants should be monitored because there is an interaction between fluconazole and such anticoagulants. Patients taking oral hypoglycemics and fluconazole should be monitored, because fluconazole has been shown to inhibit the metabolism of tolbutamide. Fluconazole has been successfully used to treat a variety of fungal infections in a variety of contexts including vaginal candidiasis; oropharyngeal candidiasis in immunocompromised patients, those with malignancies, transplant recipients, and patients with systemic sclerosis; patients with cryptococcal meningitis; and patients with fungal infections who were also treated with chemotherapy or radiation therapy. In the treatment of all of these infections with doses ranging from 50 mg to 400 mg a day of fluconazole, there has been a very low incidence of side effects (9.3%) reported, and only 1.1% of all patients were withdrawn from therapy.