Pharmacology · Opioids and Analgesics

Which pharmacokinetic property makes remifentanil uniquely suited to continuous infusion during anaesthesia without cumulative effect?

  • A It is exclusively eliminated by hepatic glucuronidation independent of blood flow
  • B It has a large volume of distribution that buffers changes in plasma concentration
  • C It undergoes rapid ester hydrolysis by nonspecific blood and tissue esterases to inactive metabolites
  • D It induces its own metabolism via CYP3A4 within hours of infusion
Correct answer: C. It undergoes rapid ester hydrolysis by nonspecific blood and tissue esterases to inactive metabolites

Explanation

Remifentanil is an ester-linked opioid degraded by widespread nonspecific plasma and tissue esterases, giving it a very short half-life of about 3 to 10 minutes and a context-insensitive half-time regardless of infusion duration. Its metabolite is essentially inactive. Hepatic elimination is irrelevant here, and there is no known autoinduction, which rules out options B, A and D.

Reference: Goodman and Gilman's The Pharmacological Basis of Therapeutics, 14th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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