Gastiin CR

Each controlled-release tablet contains Mosapride Citrate Dihydrate 15.87 mg (As Mosapride Citrate 15 mg).

Drug for Functional Gastrointestinal Disorders (Propulsive).
Pharmacology: Pharmacodynamics: Mechanism of Action: Mosapride Citrate is a selective 5-HT4 receptor agonist. It is considered that mosapride citrate stimulates 5-HT4 receptors in the gastrointestinal nerve plexus, which increases the release of acetylcholine (ACh), resulting in enhancement of gastrointestinal motility and 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) contents. The gastric emptying enhancing effect was decreased after 1-week repeated administration (in rats).
Pharmacokinetics: After oral administration of single dose of Mosapride 5-40 mg, peak Mosapride concentration (Cmax) was reached after ~1 hour. Mean elimination half-lives (t) were 1.4-2.0 hours.
Plasma Cmax (52.0 ng/mL) of the active M 1 metabolite occurred 0.5 hours after a single dose of mosapride 40 mg. Elimination of M 1 (t = 4.3 hours).
Mosapride is excreted in urine and feces in 48 hours after administration of a single dose of Mosapride 5 mg.

Treatment of gastrointestinal symptoms associated with functional dyspepsia (heartburn, nausea, vomiting).

Adults: 15 mg of mosapride citrate is orally administered once a day.
Mosapride Citrate (GASTIIN CR) should be taken on an empty stomach.
Tablet must be swallowed without chewing or crushing.

No data available.

Mosapride Citrate (GASTIIN CR) contains lactose monohydrate and should not be taken by patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption.

If any improvement of gastrointestinal symptoms is not observed after the administration for a given period of time (usually for 2 weeks), Mosapride Citrate (GASTIIN CR) should not be administered for a long period of time.
Administering this drug with food may raise the blood concentration of this drug, so it shall be administered in an empty stomach. When this drug was administered on a single dose after a high-fat diet, Cmax, AUC were increased by 78% and 39% respectively compared to when administered on an empty stomach.
Others: 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 Children: Safety in children has not been established (no clinical experience).
Use in the Elderly: Since the physiological function in the kidneys and liver are generally reduced in the elderly patients, Mosapride Citrate (GASTIIN CR) should be administered with care by monitoring patients' condition. If any adverse reactions are found, appropriate measures e.g., reducing the dose (e.g. to 7.5 mg/day) should be given.

1) Mosapride Citrate (GASTIIN CR) should not be used in pregnant women, women who may possibly be pregnant, only if the expected therapeutic benefits outweigh the possible risks associated with the treatment. (Safety in pregnant women has not been established.)
2) Administration of Mosapride Citrate (GASTIIN CR) to nursing mothers should be avoided. If administration is essential, nursing mothers should discontinue breastfeeding during the treatment. (Animal (rat) experiments have shown that Mosapride citrate is excreted in breast milk.)

Adverse reactions of Mosapride citrate controlled-release tablets: From the randomized, double-blind, active-controlled, parallel-group clinical trial on 138 functional dyspepsia patients, adverse reactions occurred in 12 patients, where the expression rate was found to be 13.24% (9/68, 10 cases) in the test group (controlled-release tablet), and 4.29% (3/70, 3 cases) in the control group (immediate-release tablet). No serious adverse reactions were reported in both the test group and the control group. As the result of analyzing adverse drug reaction expression rate that cannot exclude the causal relation with the clinical drug, diarrhea and nausea were reported in 1.47% each (1/68, 1 case) for total of 2.94% (2/68, 2 cases) from the test group, and none were reported from the control group.
Adverse reactions of Mosapride citrate immediate-release tablets (3 times a day): Adverse reactions were found in 40 of 998 cases (4%) in clinical trials. The main adverse reactions were diarrhea/loose stools (1.8%), dry mouth (0.5%), malaise (0.3%), etc.
Abnormal clinical laboratory test values were observed in 30 of 792 cases (3.8%), which were mainly eosinophilia (1.1%), elevations of triglyceride (1%), AST (GOT), ALT (GPT), ALP and γ-GTP (0.4% each) (at the time of approval).
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 γ-GTP, etc and jaundice may occur, and the patient should be monitored carefully as some of these reactions were fatal. If any abnormalities are found, discontinue the administration immediately and give appropriate measures.

Store at temperatures not exceeding 30°C.
Special Precautions for Storage: Do not preserve in other containers in order to avoid accident or quality control problem.

GIT Regulators, Antiflatulents & Anti-Inflammatories

A03FA09 - mosapride ; Belongs to the class of propulsives. Used in the treatment of functional gastrointestinal disorders.

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