MIMS Class : GIT Regulators, Antiflatulents & Anti-inflammatories

Other Precautions: When 100-330 times of the recommended clinical dose (30-100 mg/kg/day) of mosapride citrate was orally administered in rodents for long period (104 weeks in rats, 92 weeks in mice), increased incidence of hepatocellular adenoma and thyroid follicular cell adenoma were observed.

Use in pregnancy & lactation: Safety of Gasmotin in pregnant women has not been established. It should not be used in pregnant women or to women who may possibly be pregnant. Gasmotin can only be used if the expected therapeutic benefits outweigh the possible risks associated with the treatment.

Animal (rat) experiments have shown that this drug is excreted in breast milk. Administration of Gasmotin to nursing mothers should be avoided. If administration is essential, nursing mothers should discontinue breastfeeding during the treatment.

Use in children: Safety of this drug in children has not been established [no clinical experience].

Use in the elderly: Since the physiological function of the kidneys and liver are generally reduced in the elderly patients, Gasmotin should be administered with care by monitoring patients’ condition. If any adverse reactions are found, appropriate measures eg, reducing the dose (eg, to 7.5 mg daily) should be given.

Clinically Significant Adverse Reactions: Fulminant hepatitis, hepatic dysfunction and jaundice (<0.1%, each). Since fulminant hepatitis, serious hepatic dysfunction accompanied with marked elevations of AST (GOT), ALT (GPT) and g-GTP, etc. and jaundice may occur and some of them were fatal, the patient should be monitored carefully. If any abnormalities are found, discontinue the administration immediately and give appropriate measures.

Other Adverse Reactions: See Table 2.

The doctor must be informed in case any adverse reactions related to drug use is observed.
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Mechanism and Risk Factors: As gastroprokinetic effect of mosapride citrate is exerted by activation of the cholinergic nerves, concomitant use of anticholinergic agents may decrease the effect of Gasmotin.
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Shelf-Life: 3 years.

Mosapride citrate is (±)-4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methyl] benzamide citrate dihydrate. Molecular formula: C21H25ClFN3O3·C6H8O7·2H2O. Molecular weight: 650.05. Partition coefficient: 9.1 x 102 (chloroform/water solvent, pH 7, at room temperature).

Mosapride citrate occurs as white to yellowish white crystalline powder. It is odorless and has a slightly bitter taste. It is freely soluble in N, N-dimethylformamide, in pyridine and in acetic acid (100), sparingly soluble in methanol, slightly soluble in ethanol (95) and acetic anhydride, and practically insoluble in water and in diethyl ether.

Pharmacology: Clinical Pharmacology: In the gastric emptying test for healthy adults and patients with chronic gastritis, single administration of mosapride citrate 5 mg enhanced gastric emptying.

Gastroprokinetic Effect: Mosapride citrate increased gastric and duodenal motility after meals in conscious dogs.

Gastric Emptying Enhancing Effect: Mosapride citrate enhances gastric emptying of liquid (in mice and rats) and solid (in rats) content. The gastric emptying enhancing effect was decreased after 1-week repeated administration (in rats).

Mechanism of Action: Mosapride citrate 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: Plasma Concentration Results (5 healthy adults under fasting conditions, single administration of mosapride citrate 5 mg): Tmax: 0.8 ± 0.1 hr; Cmax: 30.7 ± 2.7 ng/mL; t½: 2 ± 0.2 hr.

Plasma Protein Binding Rate: 99% (in vitro, human serum, at a concentration of 1 mcg/mL, methods of ultrafiltration or equilibrium dialysis).

Main Metabolites and Metabolic Pathway: Main Metabolite: Des-4-fluorobenzyl compound. Metabolic Pathway: Mosapride citrate is metabolized mainly in the liver, where the 4-fluorobenzyl group is removed, followed by oxidation of the morpholine ring at position 5, and hydroxylation of the benzene ring at position 3.

Excretion Route and Excretion Rate: Excretion Route: In urine and feces. Excretion Rate: In urine collected for 48 hrs after administration, 0.1% was excreted as unchanged compound and 7% was excreted as the main metabolite (des-4-fluorobenzyl compound). (Healthy adults, single administration of mosapride citrate 5 mg under fasting conditions).

Metabolic Enzyme: Cytochrome P-450 sub-family: Mainly CYP3A4.

Drug Interactions: When erythromycin at 1200 mg/day was concomitantly administered with mosapride citrate at 15 mg/day, in comparison with a single administration of mosapride, maximum blood concentration of mosapride increased from 42.1-65.7 ng/mL, the half-life was prolonged from 1.6-2.4 hrs and AUC0-4 increased from 62-114 ng·hr/mL. (Healthy adult).

Clinical Studies: The results of clinical studies on 435 cases in total including a double-blind comparative study are summarized in Table 1. (See Table 1.)