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Fluconazole: a new triazole antifungal agent
M T Pasko1, S C Piscitelli, A D Van Slooten
1School of Pharmacy, State University of New York, Buffalo 14260.
DICP : the Annals of Pharmacotherapy
|September 1, 1990
Summary
Fluconazole, a bis-triazole antifungal, effectively treats fungal infections by disrupting fungal membranes. It is well-tolerated and suitable for oral or intravenous administration in various patient populations.
Area of Science:
- Pharmacology
- Mycology
- Infectious Diseases
Background:
- Fluconazole is a fluorine-substituted bis-triazole antifungal agent.
- Its mechanism involves inhibiting fungal cytochrome P-450, disrupting ergosterol synthesis and fungal membranes.
Purpose of the Study:
- To review the pharmacological properties, clinical applications, and safety profile of fluconazole.
- To highlight its efficacy in treating candidiasis and cryptococcal meningitis.
Main Methods:
- Review of animal models demonstrating activity against various fungi.
- Analysis of pharmacokinetic data including serum concentrations, protein binding, and elimination.
- Summary of clinical trial outcomes and reported therapeutic uses.
Main Results:
- Demonstrated activity against Aspergillus spp., Candida spp., Cryptococcus neoformans, and others in animal models.
- Favorable pharmacokinetics with long serum half-life and good penetration into cerebrospinal fluid.
- Clinical efficacy supported for oropharyngeal/esophageal candidiasis and cryptococcal meningitis.
Conclusions:
- Fluconazole is a well-tolerated antifungal agent with established efficacy for specific fungal infections.
- Potential drug interactions exist, requiring careful consideration of co-administered medications.
- Further trials will define its role in broader systemic fungal infection management.