Review of fluconazole: a new triazole antifungal agent. 1989

H Washton
Pfizer International, Inc., New York, New York 10017-5703.

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of fluconazole, there has been a very low incidence of side effects (9.3%) reported, and only 1.1% of all patients were withdrawn from therapy.

UI MeSH Term Description Entries
D009181 Mycoses Diseases caused by FUNGI. Fungus Diseases,Fungal Diseases,Fungal Infections,Fungus Infections,Disease, Fungal,Disease, Fungus,Diseases, Fungal,Diseases, Fungus,Fungal Disease,Fungal Infection,Fungus Disease,Fungus Infection,Infection, Fungal,Infection, Fungus,Infections, Fungal,Infections, Fungus
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000042 Absorption The physical or physiological processes by which substances, tissue, cells, etc. take up or take in other substances or energy.
D015725 Fluconazole Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS. Apo-Fluconazole,Béagyne,Diflucan,Fluc Hexal,FlucoLich,Flucobeta,Fluconazol AL,Fluconazol AbZ,Fluconazol Stada,Fluconazol von ct,Fluconazol-Isis,Fluconazol-ratiopharm,Flunazul,Fungata,Lavisa,Loitin,Neofomiral,Oxifungol,Solacap,Triflucan,UK-49858,Zonal,Apo Fluconazole,Fluconazol Isis,Fluconazol ratiopharm,UK 49858,UK49858

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