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Racecadotril demonstrates intestinal antisecretory activity in vivo
1Department of Pharmacology, Institut National de la Recherche Agronomique, Toulouse, France. lbueno@toulouse.inra.fr
Alimentary Pharmacology & Therapeutics
|January 26, 2000
Summary
Racecadotril, an enkephalinase inhibitor, effectively reduces cholera toxin-induced intestinal hypersecretion. This antisecretory effect is mediated by opioid pathways, as shown by naloxone suppression.
Area of Science:
- Pharmacology
- Gastroenterology
Background:
- Racecadotril is a potent enkephalinase inhibitor that protects endogenous enkephalins.
- It exhibits antidiarrhoeal activity with selective antisecretory effects, not affecting intestinal motility.
Purpose of the Study:
- To directly assess the antisecretory effect of racecadotril.
- To investigate the role of opioid pathways in racecadotril's antisecretory activity.
Main Methods:
- A jejunal Thiry-Vella loop model was used in mongrel dogs.
- Water and ionic fluxes were measured during cholera toxin infusion.
- The effects of racecadotril, naloxone, and phentolamine were evaluated.
Main Results:
- Racecadotril significantly reduced cholera toxin-induced hypersecretion of water, sodium, and potassium.
- Basal absorption remained unaffected by racecadotril.
- The antisecretory effect was blocked by naloxone but not by phentolamine.
Conclusions:
- Racecadotril demonstrates direct antisecretory activity.
- This activity is linked to the protection of endogenous enkephalins and involves opioid pathways.