Question:

All are true about Aprepitant except?

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Antiemetics block substance P; is aprepitant really an agonist?
Updated On: Jun 24, 2026
  • Agonist at NK1
  • Crosses blood brain barrier
  • Ameliorates nausea and vomiting of chemotherapy
  • Metabolized by CYP3A4
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The Correct Option is A

Solution and Explanation

Step 1: Identify the drug. Aprepitant is an antiemetic used to prevent chemotherapy-induced and postoperative nausea and vomiting.
Step 2: Recall its true mechanism. Aprepitant is a neurokinin-1 (NK1) receptor antagonist; it blocks the action of substance P in the vomiting centre. Therefore calling it an NK1 agonist is false.
Step 3: Verify the remaining statements. It is lipophilic and crosses the blood brain barrier to act centrally (B true). It clearly reduces chemotherapy-related nausea and vomiting, especially the delayed phase (C true). It is a substrate of CYP3A4 and also inhibits CYP3A4, leading to drug interactions (D true).
Step 4: Select the exception. Since the stem asks for the false statement, the NK1 agonist claim is the exception.
Answer: Option A, Agonist at NK1.
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