Expiration date: 04/2025
Pharmachologic effect
Antiemetic, reduces nausea, hiccups, stimulates peristalsis of the digestive tract. Antiemetic effect due to blockade of dopamine D2-receptors and increase the threshold of the chemoreceptor trigger zone, is a blocker of serotonin receptors. It is believed that metoklopramidingibiruet relaxation of smooth muscles of the stomach caused by dopamine, thereby enhancing cholinergic reaction gastrointestinal smooth musculature. It helps accelerate gastric emptying of the stomach by preventing the relaxation of the body and increase the activity of the antrum and upper sections of the small intestine. Decreases content reflux into the esophagus by increasing the pressure of the esophagus sphincter at rest and improves the esophageal acid clearance due to the increase of its peristaltic amplitude.
Metoclopramide stimulates prolactin secretion and causes a transient increase in circulating levels of aldosterone, which may be accompanied by short-term fluid retention.
Pharmacokinetics
After intake of rapidly absorbed from the gastrointestinal tract. Plasma protein binding is about 30%. Biotransformed in the liver. Write mainly kidneys in an unmodified form or in the form of metabolites. T1 / 2 is from 4 to 6 hours.
Testimony
Vomiting, nausea, hiccups of various origins. Atony and hypotonia of the stomach and intestines (including postoperative), biliary dyskinesia, reflux esophagitis, flatulence, complex therapy relapse of gastric ulcer and duodenal ulcers, accelerating peristalsis during gastrointestinal radiocontrast studies.
dosage
Adults inside - 3-4raza 5-10 mg / day. Vomiting, nausea strong administered metoclopramide / m or / in a dose of 10 mg. Intranasal - 10-20 mg in each nostril 2-3 times / day.
Maximum dose: single ingestion - 20 mg daily - 60 mg (for all routes of administration).
The average single dose for children over 6 years of age is 5 mg 1-3 times / day. orally or parenterally. For children under 6 years of daily dose for parenteral administration is 0.5-1 mg / kg, the frequency of reception - 1-3 times / day.
Side effect
From the digestive system: at the beginning of treatment may be constipation, diarrhea, rarely - dry mouth.
CNS: the beginning of treatment may be a feeling of tiredness, sleepiness, dizziness, headache, depression, akathisia. Perhaps the emergence of extrapyramidal symptoms in children and young adults (even after a single application of metoclopramide): spasm of facial muscles, hyperkinesis, spasmodic torticollis (usually held immediately after the discontinuation of metoclopramide). With prolonged use, more frequently in elderly patients, possible symptoms of parkinsonism, dyskinesia.
From hemopoiesis system: at the beginning of the treatment is possible agranulocytosis.
From endocrine system: rarely, long-term use at high doses - galactorrhea, gynecomastia, menstrual irregularities.
Allergic reactions: seldom - skin rash.
Contraindications
Bleeding from the gastrointestinal tract, mechanical intestinal obstruction, perforation of the stomach or intestines, pheochromocytoma, extrapyramidal disorders, epilepsy, prolaktinozavisimye tumors, glaucoma, pregnancy, lactation, the simultaneous use of anticholinergic drugs, hypersensitivity to metoclopramide.
Pregnancy and breast-feeding
Contraindicated during pregnancy.
If used during lactation (breastfeeding) should be borne in mind that metoclopramide passes into breast milk.
In experimental studies have found adverse effects of MCP on the fruit.
Application for violations of liver function
To use caution in patients with impaired hepatic function.
Application for violations of renal function
To use caution in patients with impaired renal function.
Use in elderly patients
When applied in elderly patients should be borne in mind that the long-term use of metoclopramide at high or moderate doses of most common side effect is extrapyramidal disorders, especially Parkinson's disease and tardive dyskinesia.
Use in children
With extreme caution should be used in children, especially young children, because they have much higher risk of dyskinetic syndrome.
special instructions
To use caution in patients with asthma, hypertension, disorders of the liver and / or kidney disease, in Parkinson's disease.
With extreme caution should be used in children, especially young children, because they have much higher risk of dyskinetic syndrome. Metoclopramide in some cases it may be effective for vomiting induced by cytostatic reception.
When applied in elderly patients should be borne in mind that the long-term use of metoclopramide at high or moderate doses of most common side effect is extrapyramidal disorders, especially Parkinson's disease and tardive dyskinesia.
Against the background of the use of metoclopramide may be corruption of data in laboratory parameters of liver function and determine the concentration of aldosterone and prolactin in the blood plasma.
Effects on ability to drive vehicles and management mechanisms
During treatment should avoid potentially hazardous activities that require attention, fast psychomotor reactions.
Drug interactions
In an application with anticholinergics possible mutual weakening effects.
In an application with neuroleptics (especially phenothiazine series and butyrophenone derivatives) increased risk of extrapyramidal reactions.
In an application enhances the absorption of acetylsalicylic acid, paracetamol, ethanol.
Metoclopramide at / in the introduction of diazepam increases the rate of absorption and increases its maximum concentration in the blood plasma.
In an application with a slowly dissolving dosage form may be reduced digoxin digoxin serum concentrations of 1/3. not noted an application with digoxin in a liquid dosage form or in the form of a rapidly dissolving dosage form of interaction.
In an application with accelerates the absorption of zopiclone zopiclone with cabergoline - may decrease the effectiveness of cabergoline, ketoprofen - reduced bioavailability of ketoprofen.
Because dopamine antagonism may reduce retseptorovmetoklopramid antiparkinsonian effects of levodopa, thus, may increase the bioavailability of levodopa due to accelerated gastric emptying its influenced metoclopramide. interaction results are mixed.
At simultaneous application with Valium accelerated absorption of mexiletine, with mefloquine - increases the absorption rate of mefloquine and its concentration in the blood plasma, with possible reduction of its side effects.
In an application with accelerates the absorption of morphine morphine ingestion and enhanced its sedative effect.
In an application with reduced absorption of nitrofurantoin nitrofurantoin.
In the application of metoclopramide immediately before administration of thiopental or propofol may require a reduction of the induction dose.
Patients receiving metoclopramide, enhanced effects are prolonged and suxamethonium chloride.
While the use of tolterodine reduces the effectiveness of metoclopramide with fluvoxamine - described a case of extrapyramidal disorders, with fluoxetine - there is a risk of extrapyramidal disorders, with cyclosporine - increases the absorption of cyclosporin and increase its concentration in the blood plasma.
