Remifentanil is preferred for infusion during short neurosurgical procedures because its offset of action after prolonged high-dose infusion is rapid and predictable. This property is due to:

• A Very small volume of distribution allowing fast redistribution
• B Hydrolysis by nonspecific blood and tissue esterases to inactive metabolites ✓
• C Metabolism exclusively by CYP3A4 with high clearance
• D Renal filtration of unchanged drug with negligible tubular reabsorption

Explanation

Remifentanil is an ester-linked opioid rapidly hydrolysed by widespread nonspecific plasma and tissue esterases to a virtually inactive metabolite. Because elimination does not depend on redistribution, liver or kidney function, its context-sensitive half-time stays short even after hours of infusion, giving predictable rapid recovery. Its volume of distribution is not unusually small, and CYP enzymes play no significant role in its clearance.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.