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Antifungal Drugs
Azoles 
Blocks formation of ergosterol
Azoles
(inhibits fungal CYP450 3A)
Imidazoles Ketoconazole
Clotrimazole
Miconazole
Systemic and superficial infections
Wide coverage
Triazoles Fluconazole
Itraconazole
Voriconazole
Systemic and superficial infections
Wide coverage
 
Introduction
  • Classification
    • antifungal
      • blocks formation of ergosterol
        • azoles
  • Drugs
    • imidazoles
      • ketoconazole
      • clotrimazole
      • miconazole
    • triazoles
      • fluconazole
      • itraconazole
      • voriconazole
Mechanism
  • Action
    • fungicidal
    • inhibit synthesis of ergosterol, found in the fungal cell membrane
      • via inhibition of 14-α-demethylase, a fungal P450 enzyme
      • enzyme converts lanosterol to ergosterol
  • Resistance
    • via ↓ accumulation of azoles within the cell
Uses
  • Fluconazole
    • Candida (both superficial and disseminated)
    • Cryptococcal meningitis
      • in AIDS
      • crosses blood-brain barrier
  • Ketoconazole
    • Coccidioides
    • Histoplasma
    • Blastomyces
    • Candida albicans
    • hypercortisolism
  • Clotrimazole and miconazole
    • topical fungal infections
    • too toxic for systemic use
  • Itraconazole and voriconazole
    • Blastomyces
    • Sporothrix
    • Aspergillus
Adverse effects
  • Inhibition of testosterone synthesis 
    • CYP450 system plays a role in testosterone synthesis
    • results in gynecomastia, ↓ libido, etc.
  • Hepatoxicity
  • GI upset
  • Fever/chills
 

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