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Pharmacology: Pharmacodynamics: Itopride is acetylcholinesterase inhibitor and dopamine D2 receptor antagonism. The effect of itopride is an increase in acetylcholine concentration, which increases the lower oesophageal sphincter (LOS) pressure, promotes gastric motility, accelerates gastric emptying, and improves gastroduodenal coordination.
Pharmacokinetics: Absorption: Itopride hydrochloride is rapidly and almost completely absorbed from the gastrointestinal tract. Relative bioavailability is calculated to be 60%. There is no effect of food on bioavailability.
The peak plasma concentration is achieved within 35 minutes of oral administration.
Distribution: Approximately 96% of itopride hydrochloride is bound to plasma proteins. Albumin accounts for most of the binding. itopride has extensive tissue distribution, except in the tissues of CNS. As itopride is highly polar molecule, it does not cross the blood brain barrier readily.
Metabolism: Itopride undergoes extensive hepatic metabolism in humans. It is metabolized in the liver by N-oxidation to inactive metabolites by a flavin-dependent monooxygenase (FMO3).
Biotransformation of itopride does not involve the cytochrome P450 enzyme.
Excretion: Itopride hydrochloride and its metabolites are primarily excreted in the urine. The urinary excretions of itopride and its N-oxide were 3.7% and 75.4%, respectively.
The plasma half-life of itopride is about 6 hours.
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