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Pharmacology: Pharmacodynamics: Mosapride is a selective 5-HT4 receptor agonist. It is considered that this drug stimulates 5-HT4 receptors in the gastrointestinal nerve plexus, which increases the release of acetylcholine, resulting in enhancement of gastrointestinal motility and gastric emptying.
Pharmacokinetics: After oral administration of single doses of Mosapride 5 mg, peak Mosapride concentrations (Cmax) were reached after approximately 1 hour. Mosapride mean Cmax values after a single dose of Mosapride 5 mg was 30.7 ng/mL. Mean AUC∞ value was 67 ng·h/mL. Mean elimination half-life (t1/2) were 1.4-2.0 hours.
The protein binding rate in human plasma was 97%.
Mosapride is primarily metabolized in the liver by Cytochrome P450 3A4 to the active metabolite, a des-4-fluorobenzyl compound.
Mosapride is excreted in the urine and feces. In the 48 hours after administration of a single dose of Mosapride 5 mg, 0.1% of the total administered dose was excreted in the urine as the parent drug and 7.0% was excreted in the urine as the active metabolite.
The apparent total body clearance of Mosapride is estimated to be 56.2-80.00 L/h and the apparent volume of distribution was 1.7-3.5 L/kg.
The pharmacokinetic profile of a single dose of Mosapride 7.5 mg in elderly volunteers (aged 65-72 years) was generally similar to that in younger volunteers (aged 20-27 years).
There were no significant differences in the pharmacokinetic profiles of Mosapride administered as single or multiple doses.
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