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Antifungal agents. Part II. The azoles

C L Terrell1

  • 1Division of Allergy and Outpatient Infectious Disease and Internal Medicine, Mayo Clinic Rochester, Minnesota 55905, USA.

Mayo Clinic Proceedings
|February 13, 1999
PubMed
Summary
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New antifungal drugs like fluconazole and itraconazole have largely replaced older treatments for systemic fungal infections, offering improved efficacy and safety profiles. Research continues for even newer antifungal agents.

Area of Science:

  • Mycology
  • Pharmacology
  • Infectious Diseases

Background:

  • Systemic fungal infections were primarily treated with amphotericin B and flucytosine before 1978.
  • The introduction of imidazoles (miconazole, ketoconazole) marked advancements in antifungal therapy.
  • Ketoconazole was a widely used oral antifungal for a decade due to limited alternatives.

Purpose of the Study:

  • To review the evolution of antifungal drug therapy for systemic fungal infections.
  • To compare the efficacy and safety profiles of older and newer antifungal agents.
  • To highlight the therapeutic roles of triazoles (fluconazole, itraconazole).

Main Methods:

  • Literature review of antifungal drug development and clinical use.
  • Comparative analysis of pharmacologic properties, efficacy, and toxicity.

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  • Examination of treatment guidelines and therapeutic outcomes.
  • Main Results:

    • Fluconazole offers improved safety and efficacy over ketoconazole, with better cerebrospinal fluid penetration.
    • Itraconazole, despite drug interactions, is valuable for specific infections like sporotrichosis and aspergillosis.
    • Itraconazole has replaced ketoconazole for certain endemic mycoses and is effective in cryptococcosis and coccidioidomycosis.

    Conclusions:

    • The development of triazoles (fluconazole, itraconazole) has significantly advanced systemic fungal infection treatment.
    • Fluconazole and itraconazole represent major improvements over older antifungal agents.
    • Ongoing research aims to develop novel antifungal agents to combat resistant fungal strains.