It has anticholinesterase (Ache) activity as well as dopamine D2 receptor antagonistic activity. It is well established that M3 receptors exist on the smooth muscle layer throughout the gut and acetylcholine (Ache) released from enteric nerve endings stimulates the contraction of smooth muscle through M3 receptors. The enzyme Ache hydrolyses the released Ache, inactivates it and thus inhibits the gastric motility leading to various digestive disorders. Besides Ache, dopamine is present in significant amounts in the gastrointestinal tract and has several inhibitory effects on gastrointestinal motility, including reduction of lower esophageal sphincter and intragastric pressure. These effects appear to result from suppression of Ache release from the myenteric motor neurons and are mediated by the D2 subtype of dopamine receptors. Itopride, by virtue of its dopamine D2 receptor antagonism, removes the inhibitory effects on Ach release. It also inhibits the enzyme Ache which prevents the degradation of Ache. The net effect is an increase in Ache concentration, which in turn, promotes gastric motility, increases the lower esophageal sphincter pressure, accelerates gastric emptying and improves gastro-duodenal coordination. This dual mode of action of Itopride is unique and different from the actions of other prokinetic agents available in the market.
TargetActionsOrganismUD(2) dopamine receptor Not AvailableHumanUAcetylcholinesterase