Azoles

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Summary

Azoles are drugs recognized by their common ending of -conazole, like fluconazole and miconazole. These drugs act as antifungals, and are used to treat fungal infections like candidiasis and tinea infections. Side effects include GI upset, hepatotoxicity, and headache.

Key Points

  • Azoles
    • Key Drugs (Ending “-conazole”)
      • Fluconazole
      • Miconazole
      • Ketoconazole
      • Itraconazole
    • Mechanism
      • Antifungal
        • Inhibits the cytochrome P450 (CYP450) in fungal cells, increasing the cell permeability and killing the cell
    • Clinical Uses
      • Candidiasis
        • Vaginal or topical cream or oral formulations are available
        • Most common use is as a one-time topical application to treat vaginal candidiasis; sexual intercourse should be avoided until the inflammation is resolved, in order to prevent reinfection
        • Oral formulations are typically used to treat oral or esophageal thrush
      • Tinea infections
        • E.g. Tinea cruris (“jock itch”) or tinea corporis
        • Also known as ringworm
      • Prophylaxis against fungal infections in immunocompromised patients
    • Side Effects and Adverse Reactions
      • GI upset
        • Nausea, vomiting, diarrhea
      • Hepatotoxicity
        • Closely monitor liver enzymes (AST, ALT)
      • Headache
      • Drug-drug interactions
        • Including certain antidiabetic drugs
        • Closely monitor blood glucose in diabetic patients
      • Gynecomastia (ketoconazole)
      • Rash
      • Hypokalemia
      • Nephrotoxicity