Instructions Mosid MT tablets 5 mg No. 30
Composition
active ingredient: mosapride;
1 tablet contains mosapride citrate dihydrate equivalent to mosapride citrate 5 mg;
excipients: mannitol (E 421), colloidal anhydrous silicon dioxide, special orange powder, peppermint powder, aspartame (E 951), talc, crospovidone, magnesium stearate, yellow iron oxide (E 172), red iron oxide (E 172).
Dosage form
Pills.
Main physicochemical properties: round, flat tablets of pinkish-brown color with a fruity odor, inclusions of lighter and darker color are allowed.
Pharmacotherapeutic group
Peristaltic stimulants (propulsants). ATX code A03F A.
Pharmacological properties
Pharmacodynamics.
Mosapride is an upper gastrointestinal prokinetic agent that selectively acts as a 5-HT4 receptor agonist.
The pharmacological properties of mosapride can be summarized in its three important characteristics: 1) mosapride is a selective agonist of 5-HT4 receptors; 2) it stimulates the motility of the upper digestive tract; 3) it does not exhibit the properties of a dopamine D2 receptor antagonist.
There is evidence that the drug stimulates 5-HT4 receptors of neuronal plexuses in the digestive tract, which increases the release of acetylcholine, leading to increased gastrointestinal motility and gastric emptying. In addition, the main metabolite (M1) has a high affinity for 5-HT3 receptors and has been shown to be a potent 5-HT3 antagonist.
As a result of its action as a 5-HT4 agonist and 5-HT3 antagonist, mosapride increases gastric emptying, increases gastric and duodenal peristalsis, but does not increase lower gastrointestinal peristalsis. However, it can be used as an antiemetic.
Mosapride 5 mg once daily eliminated heartburn and vomiting associated with chronic gastritis in a double-blind comparative clinical trial involving 435 patients.
Mosapride at doses of 40 mg per day has demonstrated efficacy in reducing reflux of gastric contents into the esophagus in patients suffering from gastroesophageal reflux disease.
Pharmacokinetics.
Absorption: After oral administration, mosapride is rapidly absorbed and reaches a maximum concentration after 0.8 hours. The maximum concentration after administration of 5 mg mosapride in the fasted state in healthy volunteers was 30.7 ng/ml. The elimination half-life (t½) determined in healthy volunteers is 2 hours.
Distribution: Mosapride is highly bound to plasma proteins. 99% of the drug is bound to plasma proteins after oral administration.
Metabolism: Mosapride is metabolized primarily 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. The main metabolic enzyme involved is cytochrome P450 3A4. The main metabolite of mosapride, the des-4-fluorobenzyl compound, is a 5-HT3 receptor antagonist.
Excretion: 0.1% of mosapride is excreted as unchanged drug and 7% as the main metabolite is excreted in the urine within 48 hours in healthy volunteers. Partially excreted in the feces.
Indication
Treatment of gastroesophageal reflux disease, as well as elimination of dyspeptic symptoms of the gastrointestinal tract (heartburn, nausea) associated with diseases of the gastroduodenal zone.
Contraindication
Hypersensitivity to the active substance or to any of the excipients included in the preparation. Cases where stimulation of the motor activity of the gastrointestinal tract may be dangerous, for example, in gastrointestinal bleeding, mechanical obstruction or perforation.
Interaction with other medicinal products and other types of interactions
The gastrokinetic effect of the drug is achieved by activating cholinergic nerves. Therefore, when used simultaneously with anticholinergic agents (atropine sulfate, butylscopolamine bromide), the effect of the drug is reduced.
Since concomitant administration of anticholinergic agents may reduce the effect of this drug, precautions such as spacing the drugs should be taken when using it.
The gastric emptying effect of mosapride is inhibited by atropine, but not by naloxone, methysergide, propranolol, ritanserin, pyrilamine, indomethacin, phenoxybenzamine, yohimbine, or bicuculline.
No interaction was found between mosapride and antiulcer drugs such as cimetidine, famotidine and omeprazole.
Use with caution with nonsteroidal anti-inflammatory drugs (NSAIDs), histamine H2-receptor blockers. Concomitant use with erythromycin may increase blood concentrations of mosapride. There is a risk of QT prolongation with concomitant use with drugs that prolong the QT interval.
Application features
Use with caution in patients with a history of heart disease, including heart failure, conduction disorders, ventricular arrhythmias (including torsades de pointes), myocardial ischemia (potential risk of arrhythmia); in patients taking concomitant medications that prolong the QT interval (procaineamide, quinidine, flecainide, sotalol, tricyclic antidepressants, which can potentially increase the risk of arrhythmias, including torsades de pointes); in patients with electrolyte disturbances, especially hypokalemia, or concomitant medications that can rapidly cause hypokalemia (furosemide, which can potentially increase the risk of arrhythmias); in patients with hepatic and renal insufficiency (pharmacokinetic data are not available, but mosapride clearance may potentially be reduced).
In elderly patients, who often have decreased kidney and liver function, it is recommended to assess the patient's condition. In case of adverse reactions, take appropriate measures and reduce the dose of the drug.
If there is no improvement within 2 weeks of using the drug, further use is not recommended.
Use during pregnancy or breastfeeding
Data on the use of mosapride in pregnant women are limited, therefore the drug should be prescribed during pregnancy only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.
Mosapride passes into breast milk, so the drug should be avoided in women who are breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
Mosid MT in therapeutic doses does not affect the speed of motor reactions. In case of side effects, you should refrain from driving vehicles or working with complex mechanisms.
Method of administration and doses
The usual dose of Mosid MT is 5 mg 3 times a day before or after meals.
The Mosid MT tablet dissolves quickly in the mouth and can be washed down with water if necessary.
The maximum daily dose is 40 mg.
The course of treatment is determined by the doctor individually.
Children
The efficacy and safety of mosapride in children have not been established, so the drug should not be used in this category of patients.
Overdose
There is no information on overdose with mosapride, but it is possible to increase the manifestations of adverse reactions. There are no specific antidotes. Gastric lavage, use of activated charcoal, symptomatic treatment are recommended.
Adverse reactions
The total frequency of side effects with oral administration of the drug is no more than 7%. The following side effects are possible:
Gastrointestinal: diarrhea, constipation, nausea, dry mouth, abdominal pain, vomiting.
from the nervous system: general weakness, headache, insomnia, dizziness, impaired consciousness;
from the cardiovascular system: feeling of palpitations, tachycardia;
Skin: allergic reactions, including skin rashes, urticaria;
Laboratory changes: eosinophilia, increased triglyceride levels, aspartate aminotransferase, alanine aminotransferase, gammaglutamyltransferase.
Since Mocid MT lacks dopamine D2 receptor antagonist properties, it does not affect the central nervous system and does not cause extrapyramidal disorders.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging.
Keep out of reach of children.
Packaging
10 tablets in a strip, 3 strips in a cardboard box.
Vacation category
According to the recipe.
Producer
TORRENT PHARMACEUTICALS LTD.
Location of the manufacturer and its business address
Indrad Plant, Village Indrad, Taluka Kadi, Dist. Mehsana Gujarat 382721, India.
