Moscow ides of Mt

General characteristics. Structure:

Active ingredient: 2,5 mg or 5 mg of a mosaprid of citrate of a dihydrate that is equivalent to a citrate mosaprid.

Excipients: tablets on 2,5 mg: mannitol (Е 421), silicon dioxide colloid anhydrous, powder orange special, peppermint powder, aspartame (E 951), talc, кросповидон, magnesium stearate. tablets on 5 mg: mannitol (Е 421), silicon dioxide colloid anhydrous, powder orange special, peppermint powder, aspartame (E 951), talc, кросповидон, magnesium stearate, ferrous oxide yellow (Е 172), ferrous oxide red (Е 172).

Pharmacological properties:

Pharmacodynamics. Mosaprid is a pro-kinetic agent of an upper part of digestive tract, selectively acts as an agonist of 5-HT4 receptors.

Pharmacological properties the mosaprida can be generalized in three important characteristics: 1) мосаприд is a selective agonist 5-HT4, 2) stimulates mobility of an upper part of digestive tract, 3) D2 deprived of properties of the antagonist of a receptor of a dopamine.

There are data that drug stimulates 5-HT4 receptors in gastrointestinal neuroplex, and it increases allocation of acetylcholine that also gastric emptying leads to strengthening of a gastrointestinal vermicular movement. Besides, the main metabolite (M1) has big affinity with receptors 5-HT3 and confirmed the properties of the powerful antagonist 5-HT3.

Owing to the action as the agonist 5-HT4 and the antagonist 5-HT3, мосаприд increases gastric emptying, raises a peristaltics of a stomach and duodenum, but does not raise a peristaltics of lower parts of digestive tract. Has the use potential as antiemetic drug.

Reception to a mosaprid on 5 mg three times a day eliminating the heartburn and vomiting connected with chronic gastritis when performing double blind comparative clinical trial with involvement of 435 patients.

Mosaprid in doses of 40 mg a day showed efficiency in reduction of a reflux of gastric contents in a gullet of patients who had a gastroesophageal reflux disease.

Pharmacokinetics. Absorption. After oral administration мосаприд it is quickly soaked up and reaches the maximum concentration in 0,8 hours. The maximum concentration after reception of 5 mg анатощак healthy volunteers made 30,7 ng/ml. An elimination half-life (t½) established at healthy volunteers – 2 hours.

Distribution. Mosaprid has very big ability to contact proteins. 99% of drug contact proteins of plasma after oral administration.

Metabolism. Mosaprid is metabolized generally in a liver where the 4-ftorobenzilova group then there occurs oxidation of a morpholine ring in a position 5, and a gidroksilization of benzene ring – in a position 3 is removed. The main attracted metabolic enzyme – P450 ZA4 cytochrome. The main metabolite to a mosaprid – connection des-4-ftorobenzil is an antagonist 5-HT3.

Allocations. 0,1% are allocated to a mosaprid in the form of not changed drug, and 7% - in the form of the main metabolite are allocated together with urine within 48 hours at healthy volunteers. It is partially allocated with excrements.

Indications to use:

Treatment of a gastroesophageal reflux disease, and also elimination of the dispeptic symptoms of digestive tract (heartburn, nausea) connected with diseases of a gastroduodenal zone.

Route of administration and doses:

The usual dose of Mosidu of MT makes 5 mg three times a day to or after food.

The tablet Mosid is quickly dissolved by MT in a mouth and therefore it can be accepted both with water, and without. The maximum daily dose – 40 mg.

The average duration of primary course of treatment – 4 weeks. After that it is necessary to estimate a condition of the patient and to define need of further use of drug.

Features of use:

Use during pregnancy or feeding by a breast. As the uses by pregnant women given relatively are limited, it is possible to appoint drug during pregnancy only when the expected advantage for mother exceeds potential risk for a fruit.

Mosaprid gets into breast milk therefore women who nurse should avoid drug use.

Children. Efficiency and safety of use of drug are not established to children therefore drug should not be used at this category of patients.

Features of use. Moscow ides of MT contains aspartame therefore it should not be applied at a fenilketonuriya.

With care to apply to patients with a heart disease in the anamnesis, including heart failure, conductivity disturbances, ventricular arrhythmias (including torsades de pointes), myocardium ischemia (potential risk of emergence of arrhythmia), at a concomitant use of the drugs extending QT interval (procaineamide, quinidine, флекаинид, соталол, tricyclic antidepressants which can potentially increase risk of emergence of arrhythmias including torsades de pointes) at patients with disturbance of level of electrolytes, especially a hypopotassemia or a concomitant use of drugs which can quickly cause a hypopotassemia (furosemide which potentially increase risk of emergence of arrhythmia), at patients with a liver and renal failure (data on pharmacokinetics are absent, but the clearance to a mosaprid can potentially decrease).

At patients of advanced age at whom reduced function of kidneys and a liver is often noted it is recommended to estimate a condition of patients. In case of side reactions – to take the appropriate measures, to reduce a drug dose.

Ability to influence speed of response at control of motor transport or work with other mechanisms. MT Moscow ides in therapeutic doses do not influence the speed of motor reactions. In case of side effects it is necessary to refrain from control of vehicles or work with difficult mechanisms.

Side effects:

Total frequency of side effects at oral administration of drug makes no more than 7%. Such side reactions are possible:

- from a digestive tract: diarrhea, dryness in a mouth, abdominal pain,

- from a nervous system: general weakness, dizziness, consciousness disturbance,

- from cardiovascular system: heart consciousness, tachycardia,

- from skin: allergic reactions, such as skin rashes, a small tortoiseshell are very seldom observed,

- changes: eosinophilia, increase in level of triglycerides, aspartate aminotransferases (nuclear heating plant), alaninaminotrasferaza (ALT), gammaglutamiltransferaza (GGT).

As Mosid of MT of the deprived properties of the antagonist of a receptor of a dopamine D2, it does not influence the central nervous system and does not cause extrapyramidal disturbances.

Interaction with other medicines:

Considering that the gastrokinetichesky effect of this drug happens by activation of cholinergic nerves, simultaneous use to anticholinergic agents (Atropini sulfas, butylscopolaminum bromide) reduces it. As the concomitant use of anticholinergic agents can reduce effect of this drug, at its use it is necessary to take security measures, such as bucketed administration of drugs.

Gastric emptying enhancement effect that is provided thanks to a mosaprid, antagonizirutsya by atropine, but not Naloxonum, metisergidy, propranoly, ritanseriny, pyrilamine, indometacin, phenoxybenzamine, yohimbine or bikukuliny.

No interaction was revealed between mosapridy and antiulcerous agents, such as Cimetidinum, famotidine and омепразол.

With care to apply along with non-steroidal anti-inflammatory drugs (NPVP), blockers histamine H2 receptors. At use with anticholinergic medicines decrease in efficiency to a mosaprid is possible.

Contraindications:

The established hypersensitivity to this drug. Cases when stimulation of motor activity of digestive tract can be dangerous, for example, at gastrointestinal bleeding, mechanical impassability or perforation.

Overdose:

There is no information concerning overdose mosapridy, however at overdose strengthening of manifestations of side reactions is possible. Specific antidotes do not exist. The gastric lavage, use of absorbent carbon, a symptomatic treatment is recommended.

Storage conditions:

Period of validity - 3 years. To store in the place protected from light at ^{a temperature not higher than 25 ° C}. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a strip, on 3 strips in a cardboard pack.