Question 1 · Medium
Aprepitant is added to ondansetron and dexamethasone before highly emetogenic chemotherapy. It works by blocking:
- ANK1 (substance P) receptors
- B5-HT3 receptors
- CDopamine D2 receptors
- DHistamine H1 receptors
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Answer: A · NK1 (substance P) receptors
Aprepitant is a neurokinin-1 receptor antagonist that blocks substance P in the brainstem vomiting centre. It is especially effective against delayed nausea and vomiting 24 hours to 5 days after cisplatin, which 5-HT3 antagonists control poorly. The three-drug combination is standard for highly emetogenic regimens. Aprepitant inhibits CYP3A4, so the dexamethasone dose is reduced.
- B: 5-HT3 receptors are blocked by ondansetron, already in the regimen.
- C: D2 receptors are blocked by metoclopramide and domperidone.
- D: H1 receptors are blocked by antihistamines such as promethazine.