Opiate Modulation of Gastrointestinal Motility and the Actions of Trimebutine

Abstract

Trimebutine is an opiate ligand that interacts with the μ, σ and κ receptor subclasses with approximately equal affinity. Since opiate receptors are widely distributed in the gut, and because opiate receptor subtypes may be involved in excitatory or inhibitory control mechanisms, trimebutine has an unusual profile of action that cannot be predicted on the basis of experience with other synthetic opiates such as codeine, morphine or loperamide. Trimebutine influences motility throughout the gastrointestinal tract. The effect of trimcbutine on the lower esophageal sphincter raises the possibility of a beneficial role in the treatment of gastroesophageal reflex disease. The ability of trimebutine to promote propulsive activity in the fasting and postprandial small intestine offers novel therapeutic approaches to the treatment of motility disorders, including postoperative ileus and pseudo-obstruction. Finally, the effect of the drug on the colon supports the use of trimcbutine in irritable bowel syndrome patients who have constipation due to colonic inertia.