Effect of Itopride Hydrochloride on the Ileal and Colonic Motility in Guinea Pig In Vitro

Abstract

PurposeItopride hydrochloride (itopride) inhibits acetylcholinesterase (AChE) and antagonizes dopamine D2 receptor, and has been used as a gastroprokinetic agent. However, its prokinetic effect on the small bowel or colon has not yet been thoroughly investigated. The aim of this study was to investigate the effects of itopride on motor functions of the ileum and colon in guinea pigs.Materials and MethodsThe distal ileum was excised and the activity of peristaltic contraction was determined by measuring the amplitude and propagation velocity of peristaltic contraction. The distal colon was removed and connected to the chamber containing Krebs-Henseleit solution (K-H solution). Artificial fecal matter was inserted into the oral side of the lumen, and moved toward the anal side by intraluminal perfusion via peristaltic pump. Colonic transit times were measured by the time required for the artificial feces to move a total length of 10 cm with 2-cm intervals.ResultsIn the ileum, itopride accelerated peristaltic velocity at higher dosage (10-10-10-6 M) whereas neostigmine accelerated it only with a lower dosage (10-10-10-9 M). Dopamine (10-8 M) decelerated the velocity that was recovered by itopride infusion. Itopride and neostigmine significantly shortened colonic transit at a higher dosage (10-10-10-6 M). Dopamine (10-8 M) delayed colonic transit time that was also recovered after infusion of itopride.ConclusionItopride has prokinetic effects on both the ileum and colon, which are regulated through inhibitory effects on AChE and antagonistic effects on dopamine D2 receptor.

PillCam colon capsule endoscopy versus conventional colonoscopy for the detection of severity and extent of ulcerative colitis

“…In previous studies, domperidone, tegaserod or mosapride have been used as prokinetics to reduce gastrointestinal transit time. In our study, itopride hydrochloride was used as it can increase the contractility of the entire digestive tract and propel substances from the ileum to the colon, which was chosen to shorten the gastrointestinal transit time . Moreover, NaP has regularly been regarded as a safe osmotic agent.…”

“…In our study, itopride hydrochloride was used as it can increase the contractility of the entire digestive tract and propel substances from the ileum to the colon, which was chosen to shorten the gastrointestinal transit time. 37,38 Moreover, NaP has regularly been regarded as a safe osmotic agent. The oral administration of a small volume of NaP draws fluid from the intravascular space and causes transient hyperphosphatemia.…”

Functional Gastrointestinal Disorders: Select From the Point Prokinetic Comorbidity, Clinical Efficacy and Drug Safety

“…Итоприда гидрохлорид стимулирует контрактильную активность ЖКТ от желудка до толстой кишки, что позволяет исполь-зовать его для лечения функционального запора [66]. В обзоре исследований новых препаратов для лечения запора итоприда гидрохлорид рассматривается в каче-стве одного из наиболее перспективных препаратов [67].…”

Constipation – a difficult therapeutic problem

“…Wyjątkiem jest itopryd, będący antagonistą acetylocholinesterazy oraz inhibitorem receptora dopaminowego D 2 , dla którego w badaniach na zwierzętach wykazano działanie prokinetyczne i propulsywne w jelicie cienkim i grubym. Być może okaże się on pomocny w leczeniu ZZP -wymaga to weryfikacji w badaniach klinicznych [35,36].…”