Paper II
2015 February (2010 Scheme) · 40 marks · 120 min

Question

Fluconazole

Q43 marksShort Notes

Answer

Fluconazole is a triazole antifungal.

Mechanism of action

  • Inhibits fungal cytochrome P450-dependent enzyme (14-α-demethylase), blocking conversion of lanosterol to ergosterol
  • Ergosterol depletion disrupts fungal cell membrane integrity (fungistatic)

Pharmacokinetics

  • Good oral bioavailability, good CSF penetration (useful in fungal meningitis), water-soluble (can be given IV)

Uses

  • Cryptococcal meningitis
  • Candidiasis (oropharyngeal, oesophageal, vaginal, systemic)
  • Prophylaxis in immunocompromised patients

Adverse effects

  • Hepatotoxicity
  • GI upset, headache
  • QT prolongation (with high doses)
  • Fewer drug interactions than ketoconazole/itraconazole (still some CYP450 inhibition)

Other Years Asked


Revise MBBS
Preview