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

Question

Aprepitant

Q43 marksShort Notes

Answer

Aprepitant is a neurokinin-1 (NK1) receptor antagonist.

Mechanism of action

  • Blocks binding of substance P to NK1 receptors in the CNS (area postrema/chemoreceptor trigger zone), which mediates both the acute and, particularly, the delayed phase of nausea/vomiting

Uses

  • Prevention of chemotherapy-induced nausea and vomiting (CINV), especially with highly emetogenic regimens like cisplatin — typically combined with a 5-HT3 antagonist and dexamethasone
  • Postoperative nausea and vomiting prevention

Adverse effects

  • Fatigue, hiccups
  • GI upset
  • CYP3A4 interactions (moderate inhibitor — can affect metabolism of co-administered chemotherapy/other drugs)

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