Pharmacology: Pharmacodynamics: Mosapride is a substituted benzamide used for its prokinetic properties. Mosapride is the selective 5-HT4 receptors agonist. It stimulates 5-HT4 receptors in the gastrointestinal enteric plexus. Mosapride is increasing acetylcholine release and stimulating gastrointestinal motility, as well as the main active metabolite (M1 also known as des-4-fluorobenzyl) is reported to have 5-HT3 receptor antagonist activity.
Moreover Mosapride enhances the gastric emptying.
Pharmacokinetics: Absorption: Mosapride is rapidly absorbed with time to peak plasma concentrations occurring about 0.5 to 1.4 hours, and time to peak plasma concentrations of M1 is 0.5 hours.
Distribution: Mosapride's volume of distribution is 1.7 to 3.5 L/kg. 97% of Mosapride is bound to plasma protein.
Metabolism: Mosapride is metabolized by the liver via CYP3A4 (minor) and the principal metabolite is M1.
Elimination: Mosapride is excreted in the urine and faeces. Approximately 1% of an administered dose was excreted in urine as unchanged drug and 10% was excreted in urine as active metabolite. The mean elimination half-life of Mosapride is 1.4-2.5 hours and M1 is 4.3 hours.