Introduction
Itopride is a dopamine D2 antagonist with acetylcholinesterase inhibitory actions.
Uses
Itopride is an acetylcholine esterase inhibitor and dopamine D2 receptor antagonist used to treat symptoms of functional dyspepsia such as nausea and vomiting.
Investigated for use/treatment in gastrointestinal diseases and disorders (miscellaneous).
Associated Conditions
Mechanism of Action
Itopride 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 (ACh) released from enteric nerve endings stimulates the contraction of smooth muscle through M3 receptors. The enzyme AChE hydrolyses the released ACh, inactivates it and thus inhibits the gastric motility leading to various digestive disorders. Besides ACh, 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 ACh 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 ACh. The net effect is an increase in ACh 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.
Dosage
Use in the elderly: Since the elderly often have a physiological hypo function, they are prone to adverse reactions and should thus be closely monitored. If adverse reactions are evident, appropriate measures such as reduction or cessation of the drug should be implemented.
Use in pediatric population: The safety and efficacy of Itogut Tablet 50 mg in children and adolescents have not been established. Therefore, the administration of Itogut Tablet 50 mg is not recommended in children and adolescents below 18 years of age.
Shock and anaphylactoid reactions: Shock and anaphylactoid reactions may occur, and close observation should be made. If hypotension, dyspnoea, larynx edema, urticaria, pallor and diaphoresis etc. occur, the drug should be discontinued and appropriate measures implemented.
Hepatic function disorder and Jaundice: Hepatic function disorder and jaundice with increased AST(GOT), ALT(GPT) and g-GTP etc., may occur, and close observation should be made. If abnormalities occur, the drug should be discontinued and appropriate therapeutic measures implemented.
