Paper II
2018 July (Supplementary) (2010 Scheme) · 40 marks · 120 min

Question

Itraconazole

Q73 marksShort Notes

Answer

Itraconazole is a triazole antifungal.

Mechanism of action

  • Inhibits fungal cytochrome P450-dependent 14-α-demethylase, blocking conversion of lanosterol to ergosterol, disrupting fungal cell membrane synthesis (fungistatic)

Uses

  • Dermatophytosis, onychomycosis
  • Aspergillosis
  • Histoplasmosis, blastomycosis
  • Candidiasis (oral/oesophageal/vaginal)

Adverse effects

  • Requires acidic gastric environment for absorption (reduced with PPIs/H2 blockers)
  • Hepatotoxicity
  • GI upset
  • Significant CYP450 inhibitor — multiple drug interactions
  • Negative inotropic effect — caution/avoid in heart failure

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