Agonist of peripheral mu, kappa and delta opiate receptors
REVIEW Trimebutine is a spasmolytic with possible local anesthetic action used in gastrointestinal disorders. The compound is a antimuscarinic drug, with weak mu opioid agonist effects. The maleic acid salt of trimebutine is marketed under the trademark of Debridat, Recutin, Polybutin,] or Modulon for treatment of irritable bowel syndrome and other gastrointestinal disorders.. Trimebutine exerts its effects in part due to causing a premature activation of phase III of the migrating motor complex in the digestive tract. The actions of trimebutine] on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta opiate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. Recently, trimebutine has also been shown to decrease reflexes induced by distension of the gut lumen in animals and it may therefore modulate visceral sensitivity. Clinically, trimebutine has proved to be effective in the treatment of both acute and chronic abdominal pain in patients with functional bowel disorders, especially irritable bowel syndrome, at doses ranging from 300 to 600 mg/day. It is also effective in children presenting with abdominal pain.
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