Pharmacology · Opioids and Analgesics

A patient maintained on high-dose morphine for cancer pain is given nalbuphine for breakthrough pain. Within minutes he becomes agitated, tachycardic and complains of diffuse pain. The most likely mechanism is:

  • A Nalbuphine's mu-antagonist activity displacing morphine from receptors and precipitating withdrawal
  • B Allergic reaction to nalbuphine causing catecholamine release
  • C Additive respiratory depression leading to hypercapnic encephalopathy
  • D Nalbuphine-induced histamine release causing a pseudo-withdrawal syndrome
Correct answer: A. Nalbuphine's mu-antagonist activity displacing morphine from receptors and precipitating withdrawal

Explanation

Nalbuphine is a mixed agonist-antagonist: it is a kappa agonist and a competitive mu-receptor antagonist. In a physically dependent patient its mu antagonism displaces morphine from receptors and abruptly precipitates an abstinence syndrome with agitation, tachycardia and pain. Mixed agonist-antagonists such as nalbuphine, pentazocine and butorphanol must be avoided in opioid-dependent patients for this reason. Histamine release and allergy do not reproduce the specific withdrawal picture.

Reference: Katzung Basic and Clinical Pharmacology, 15th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.

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