Pharmacology · patient case question

What is the mechanism of action of naloxone?

Patient case: Reviewing a long medication list

Patient: Female, 55 years old

Chief Complaint: Presents for a comprehensive examination.

Background: Graves disease, hypertension, asthma. She carries a naloxone kit because a family member has opioid use disorder.

Medications: Propylthiouracil · lisinopril · albuterol inhaler · naloxone (rescue kit)

Vital Signs: BP 132/84 mmHg · HR 84 bpm · RR 16

  1. Partial agonist at the mu opioid receptor
  2. Competitive antagonist at the benzodiazepine receptor
  3. Inhibits reuptake of noradrenaline and serotonin
  4. Competitive antagonist at the mu opioid receptor
Show answer and explanation

Correct answer: D. Competitive antagonist at the mu opioid receptor

  • A. Buprenorphine is the mu partial agonist; nalbuphine and butorphanol are agonist-antagonists. Naloxone has no agonist activity at all.
  • B. Benzodiazepine receptor antagonism is FLUMAZENIL — the reversal agent for midazolam and diazepam. Confusing the two reversal agents is a classic exam trap.
  • C. Monoamine reuptake inhibition describes the SNRI antidepressants, unrelated to opioid reversal.
  • D. CORRECT. Naloxone is a pure COMPETITIVE ANTAGONIST with high affinity for the mu opioid receptor. It displaces the agonist and reverses respiratory depression within minutes. The critical clinical caveat: naloxone's duration of action (roughly 30 to 90 minutes) is SHORTER than that of many opioids, so re-narcotisation can follow and the patient must be observed or transported.

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