Pharmacology · single question

Naloxone's mechanism of action is:

  1. Mu-opioid receptor agonist
  2. NMDA receptor antagonist
  3. GABA-A receptor antagonist
  4. Competitive mu-opioid receptor ANTAGONIST (reverses opioid toxicity)
Show answer and explanation

Correct answer: D. Competitive mu-opioid receptor ANTAGONIST (reverses opioid toxicity)

  • A. Mu-opioid receptor agonists (morphine, oxycodone, fentanyl) cause opioid effects — the opposite of naloxone.
  • B. NMDA antagonism is the mechanism of ketamine and memantine — not naloxone.
  • C. GABA-A antagonism (flumazenil reverses benzodiazepines, not opioids) — wrong receptor system.
  • D. Correct. Naloxone (Narcan) is a PURE competitive mu-opioid receptor ANTAGONIST. It has higher affinity for mu receptors than opioids, rapidly displacing them and reversing opioid-induced: respiratory depression, sedation, miosis, and analgesia. Duration of action is 30–90 minutes (shorter than most opioids), requiring repeat dosing or infusion for long-acting opioid overdoses.

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