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Fluconazole: pharmacokinetics and indications

F Montero-Gei1

  • 1Escuela de Ciencias Médicas, Universidad Autónoma de Centro América (UCA), San José, Costa Rica.

Archives of Medical Research
|January 1, 1993
PubMed
Summary

Fluconazole, a new triazole antifungal, offers improved water solubility and extensive tissue distribution for treating fungal infections. Its favorable pharmacokinetic profile supports once-daily dosing for conditions like mycoses and AIDS-related fungal infections.

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Area of Science:

  • Pharmacology
  • Mycology
  • Infectious Diseases

Background:

  • Fluconazole represents a novel systemic azole antifungal agent.
  • It features a triazole substitution for reduced lipophilicity and enhanced water solubility.
  • The drug exhibits weak plasma protein binding and is available in various formulations.

Purpose of the Study:

  • To describe the pharmacokinetic properties of fluconazole.
  • To outline its clinical indications, particularly in immunocompromised patients.
  • To highlight its advantages over older antifungal agents.

Main Methods:

  • Pharmacokinetic analysis of fluconazole's absorption, distribution, metabolism, and excretion.
  • Review of clinical trial data for efficacy and safety.
  • Assessment of drug interactions and formulation characteristics.

Main Results:

  • Fluconazole achieves steady-state plasma concentrations within approximately 7 days of once-daily dosing.
  • The drug distributes extensively and evenly into tissues, circulating primarily as free drug.
  • Elimination half-life is approximately 30 hours, facilitating convenient dosing regimens.

Conclusions:

  • Fluconazole demonstrates favorable pharmacokinetic properties, including good oral bioavailability and tissue penetration.
  • It is indicated for the treatment of various fungal infections, including those in patients with Acquired Immunodeficiency Syndrome (AIDS).
  • The agent's characteristics make it a valuable option for managing mycoses.

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