Mimosa 5

White, oblong, biconvex, bevelled edge film coated tablet with engraved M5 on one side and plain on the other.
Each film coated tablet contains Mosapride citrate dihydrate 5.30 mg eq. to Mosapride citrate anhydrous 5 mg.

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 (C_max) were reached after approximately 1 hour. Mosapride mean C_max 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 (t_1/2) 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.

Mosapride is indicated for the treatment of gastrointestinal symptoms associated with functional dyspepsia, (chronic gastritis, heartburn, nausea, vomiting).

Adults: 15 mg of mosapride citrate as anhydrous form is usually administered in 3 divided oral doses before or after meals.

When 100 to 330 times of the recommended clinical dose (30 to 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.

Mosapride citrate is contraindicated in patients with a history of hypersensitivity to this product or any other 5-HT₄ receptor agonists.

If any improvement in gastrointestinal symptoms does not occur after approximately 2 weeks of therapy, then this agent should not be continued without supervision.
Mosapride should be administered with care in elderly patients. Safety of this drug in children has not been established.
Severe (including fatal) hepatotoxicity has been rarely reported with use. Discontinue immediately if early signs/symptoms of hepatic toxicity or elevated liver enzymes occur.
Use with caution in situations where stimulated gastrointestinal (GI) motility may be dangerous, including mechanical GI obstruction, perforation, or hemorrhage.
Some prokinetic agents (eg, cisapride, domperidone, levosulpride, metoclopramide) are contraindicated. Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy.
Use in Pregnancy & Lactation: Mosapride use during pregnancy and lactation should be avoided.
Use in Children: Safety of this drug in children has not been established.
Use in the Elderly: Since in the elderly patients their physiological function in the kidneys and the liver are reduced in general, this drug should be administered with care by monitoring patients' condition. If any adverse reactions are found, appropriate measures such as reducing the dose (e.g. to 7.5 mg daily) should be given.

Pregnancy: Safety of this drug in pregnant women has not been established. This drug should 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.
Lactation: Animal (rat) experiments have shown that this drug is excreted in breast milk. Administration of this drug to nursing mothers should be avoided. If administration is essential, nursing mothers should discontinue breast feeding during the treatment.

Mosapride was well tolerated in clinical trials, with only minor adverse events such as diarrhoea/loose stools, dry mouth, malaise and headache being most commonly reported (<5% of patients).
According to physician-rated assessments in phase III trials, Mosapride was considered to be safe in 96.6% of patients with gastro-oesophageal reflux disease and 97.5% of patients with chronic gastritis.
Adverse events occurred in 2.71% (23 of 848) of patients with dyspepsia who had received Mosapride for more than 2 weeks, according to data from the post-marketing surveillance study. The most common adverse events were abdominal pain and loose stools (both 0.35%). No serious adverse events were reported.
Abnormal laboratory test values reported in clinical trials included eosinophilia (1.1%), elevated triglycerides (1.0%), and elevated AST, ALT and gamma glutamyl transpeptidase levels (all 0.4%).
There were no reports of QT interval prolongation associated with Mosapride treatment. However, there has been a single case report of Torsades de pointes ventricular tachycardia in a patient with hypokalemia who was receiving combination therapy with Mosapride and flecainide.

Mosapride should be administered with caution when co-administered with anticholinergic agents (atropine sulfate and butyl-scopolamine bromide, etc.) As gastroprokinetic effect of Mosapride is exerted by activation of the cholinergic nerves, concomitant use of anticholinergic agents may decrease the effect Mosapride. Therefore, in the case of the concomitant use of anticholinergic agents, precautions such as taking the drugs at intervals should be taken.
When erythromycin at 1,200 mg/day was concomitantly administered with this drug at 15 mg/day, in comparison with a single administration of Mosapride, maximum blood concentration of Mosapride increased from 42.1 ng/mL to 65.7 ng/mL, the half-life was prolonged from 1.6 hours to 2.4 hours and AUC_0-4 increased from 62 ng·hr/mL to 114 ng·hr/mL (Healthy adult).

Store below 30°C.

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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