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Trimebutine maleate effect on the small intestine

Time:2015/9/30 7:25:13

In fasted dogs, Trimebutine maleate - given either intravenously or orally - delays the appearance of phase III of the MMC in the stomach and duodenum by increasing the duration 

of phase II of the MMC in the intestine and by inducing a premature phase III, migrating along the entire intestine. 53 The motor effects of Trimebutine maleate on the small 

Trimebutine maleate

intestine are prevented by previous intravenous injection of naloxone, but not by intracerebroventricular injection of naloxone,

indicating that Trimebutine maleate acts peripherally to induce these effects.' In the same study, Trimebutine maleate itself was shown to be ineffective when administered 

centrally. It has recently been shown that the effect of Trimebutine maleate on dog intestine is dependent on the phase of MMC at the time of drug injection."

In stressed rats, Trimebutine maleate prevented stress-induced changes in intestinal motility,which consisted of a decreased duration of phase III of the MMC; diazepam did not 

reverse the effects of stress on small-intestine motility in this study." In man, Trimebutine maleate stimulates intestinal motility in both fed and fasted states." In the 

fasted state, intravenous injection ofTrimebutine maleate (100 mg) induced a premature phase III of the MMC, which was very similar in duration and propagation velocity to a 

spontaneous phase I1I.71 When the injection of Trimebutine maleate was performed immediately after a spontaneous phase III or after the injection of naloxone, Trimebutine 

maleate did not induce additional phase III activity. In the fed state, intravenous Trimebutine maleate (100 mg) interrupted the fed pattern of intestinal motility and induced 

cyclical activity similar to that observed in the fasted state." In an otherstudy, Trimebutine maleate (600 mg) injected intraduodenally 20 min after a spontaneous phase III, 

also induced a premature phase III,

which was related to the peak plasma Trimebutine maleate concentration.P:"In man, unlike the dog," Trimebutine maleate does not increase blood levels of motilin.":"

Moreover, Trimebutine maleate was found to abolish the increase in plasma motilin observed in fasted subjects. In the same study, plasma levels of cholecystokinin and pancreatic 

polypeptide were not altered by the injection of Trimebutine maleate, while the prolactin level increased. By contrast, in another study, the plasma level of pancreatic 

polypeptide was

increased following injection of Trimebutine maleate." Finally, Trimebutine maleate seemed to lower the plasma gastrin level in patients with chronic active gastritis."