Paper II
2024 December (Supplementary) (2019 Scheme) · 100 marks · 180 min

Question

Compare and contrast: loperamide and racecadotril.

Q104 marksShort Answers

Answer

Compare and contrast: Loperamide and Racecadotril

FeatureLoperamideRacecadotril
ClassOpioid-receptor agonist (peripherally restricted)Enkephalinase inhibitor
MechanismActivates mu-opioid receptors in the gut wall, reducing peristalsis and increasing transit timeInhibits enkephalinase, prolonging the action of endogenous enkephalins, which reduces intestinal hypersecretion without slowing motility
Effect on motilityReduces motility (antimotility)Antisecretory, motility largely unaffected
CNS penetrationMinimal (P-glycoprotein substrate, excluded from CNS at normal doses)Minimal
Risk in invasive/infective diarrheaCan worsen outcomes by delaying pathogen clearance and increasing toxin dwell time (risk of toxic megacolon in some infections)Considered safer in infective diarrhea, since motility (and hence clearance) is not slowed
Typical useAcute non-infective/traveler’s diarrhea, chronic diarrheaAcute diarrhea, including in children, as an adjunct to oral rehydration

Shared feature: both provide symptomatic relief in acute diarrhea without being antimicrobial agents themselves, and neither substitutes for oral rehydration, which remains the priority.

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