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Fluconazole: a new antifungal agent.

S F Kowalsky1, D M Dixon

  • 1Department of Pharmacy Practice, Albany College of Pharmacy, NY 12208.

Clinical Pharmacy
|March 1, 1991
PubMed
Summary

Fluconazole is a triazole antifungal effective for candidiasis and cryptococcal meningitis. While generally safe and well-tolerated, its superiority over other antifungals requires further study.

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Area of Science:

  • Pharmacology
  • Mycology
  • Clinical Medicine

Background:

  • Fluconazole is a triazole antifungal agent.
  • It is used to treat oropharyngeal and esophageal candidiasis and cryptococcal meningitis.
  • Fluconazole inhibits lanosterol C-14 demethylation, with minimal impact on mammalian cytochrome P-450 enzymes.

Purpose of the Study:

  • To review the chemistry, activity, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, and administration of fluconazole.
  • To assess fluconazole's role in treating systemic mycoses.

Main Methods:

  • Literature review of fluconazole's properties and clinical applications.
  • Analysis of in vitro activity versus in vivo effectiveness.
  • Examination of pharmacokinetic data, including tissue distribution and cerebrospinal fluid penetration.
  • Review of clinical trial data for efficacy and safety.

Main Results:

  • Fluconazole exhibits water solubility, excellent bioavailability, low protein binding, and wide tissue distribution.
  • It penetrates the cerebrospinal fluid effectively.
  • Adverse effects are infrequent and mainly gastrointestinal.
  • Drug interactions with tolbutamide, warfarin, rifampin, cyclosporine, and phenytoin are noted.
  • Efficacy in candidiasis and cryptococcal meningitis is demonstrated, but superiority over other antifungals is not yet proven.

Conclusions:

  • Fluconazole is an effective antifungal with a favorable pharmacokinetic profile and a low incidence of adverse effects.
  • Further research is needed to establish fluconazole as a first-line therapy for systemic mycoses.
  • Its efficacy appears comparable to other antifungals for certain infections.

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