Universal reference book for medicines

Active substance: metoclopramide

Type: Antiemetic drug of central action blocking dopamine receptors

Manufacturer: IPCA LABORATORIES (India)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

Antiemetic, helps to reduce nausea, hiccups;
stimulates the peristalsis of the gastrointestinal tract. Antiemetic effect is due to blockade of dopamine D 2 receptors and an increase in the threshold of chemoreceptors of the trigger zone, is a blocker of serotonin receptors. It is believed that metoclopramide inhibits the relaxation of the smooth muscle of the stomach caused by dopamine, thereby enhancing cholinergic reactions of the smooth muscles of the gastrointestinal tract. Promotes the acceleration of gastric emptying by preventing the relaxation of the body of the stomach and increasing the activity of the antrum of the stomach and upper parts of the small intestine. Reduces the reflux of the contents in the esophagus by increasing the pressure of the sphincter of the esophagus at rest and increases the clearance of acid from the esophagus due to an increase in the amplitude of its peristaltic contractions.
Metoclopramide stimulates the secretion of prolactin and causes a transient increase in the level of circulating aldosterone, which may be accompanied by a short-term fluid retention.

After oral administration, it is rapidly absorbed from the digestive tract.
Binding to plasma proteins is about 30%. Biotransformatsya in the liver. It is excreted mainly by the kidneys both in unchanged form and in the form of metabolites. T 1/2 is from 4 to 6 hours.
Vomiting, nausea, hiccough of different genesis.
Atony and hypotension of the stomach and intestines (including postoperative); biliary dyskinesia; reflux esophagitis;flatulence; in the complex therapy of exacerbations of peptic ulcer of the stomach and duodenum; acceleration of peristalsis during radiocontrast studies of the gastrointestinal tract.
Adults inside - 5-10 mg 3-4 times / day.
When vomiting, severe nausea, metoclopramide is given in / m or IV in a dose of 10 mg. Intranasal - 10-20 mg in each nostril 2-3 times / day.
Maximum doses: one-time with oral administration - 20 mg;
daily - 60 mg (for all modes of administration).
The average single dose for children over 6 years is 5 mg 1-3 times / day inward or parenterally.
For children under 6 years of age, the daily dose for parenteral administration is 0.5-1 mg / kg, the frequency of reception is 1-3 times / day.
From the digestive system: at the beginning of treatment, constipation, diarrhea;
rarely dry mouth.
From the side of the central nervous system: at the beginning of treatment there may be a feeling of fatigue, drowsiness, dizziness, headache, depression, akathisia.Perhaps the emergence of extrapyramidal symptoms in children and young people (even after a single application of metoclopramide): spasm of facial muscles, hyperkinesis, spastic torticollis (usually immediately after stopping metoclopramide).
With prolonged use, more often in elderly patients, there may be phenomena of parkinsonism, dyskinesia.
From the hemopoietic system: at the beginning of treatment, agranulocytosis is possible.

On the part of the endocrine system: rarely, with prolonged use in high doses - galactorrhea, gynecomastia, menstrual irregularities.

Allergic reactions: rarely - skin rash.

Bleeding from the digestive tract, mechanical intestinal obstruction, perforation of the stomach or intestines, pheochromocytoma, extrapyramidal disorders, epilepsy, prolactin-dependent tumors, glaucoma, pregnancy, lactation, simultaneous use of anticholinergic drugs, hypersensitivity to metoclopramide.

Contraindicated in pregnancy.

When used during lactation (breastfeeding), it should be borne in mind that metoclopramide penetrates into breast milk.

In experimental studies, no adverse effect of metoclopramide on the fetus has been established.

Use with caution in patients with impaired renal function.

Use with caution in patients with impaired hepatic function.

With extreme caution should be used in children, especially the early age, t.
they have a significantly higher risk of dyskinetic syndrome.
When used in elderly patients, it should be borne in mind that with prolonged use of metoclopramide in high or medium doses, the most common side effect is extrapyramidal disorders, especially parkinsonism and tardive dyskinesia.

With caution apply in patients with bronchial asthma, arterial hypertension, impaired liver and / or kidney function, with Parkinson's disease.

With extreme caution should be used in children, especially the early age, t.
they have a significantly higher risk of dyskinetic syndrome. Metoclopramide in some cases can be effective in vomiting caused by the use of cytotoxic drugs.
When used in elderly patients, it should be borne in mind that with prolonged use of metoclopramide in high or medium doses, the most common side effect is extrapyramidal disorders, especially parkinsonism and tardive dyskinesia.

Against the background of the use of metoclopramide, there may be distortions in these laboratory parameters of liver function and determination of the concentration of aldosterone and prolactin in the blood plasma.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, potentially dangerous activities requiring increased attention, rapid psychomotor reactions should be avoided.

With simultaneous use with anticholinergic agents, mutual weakening of effects is possible.

When used simultaneously with neuroleptics (especially the phenothiazine series and butyrofenone derivatives), the risk of extrapyramidal reactions increases.

With simultaneous use, absorption of acetylsalicylic acid, paracetamol, ethanol is enhanced.

Metoclopramide with IV introduction increases the rate of absorption of diazepam and increases its maximum concentration in the blood plasma.

When used simultaneously with a slowly dissolving dosage form of digoxin, it is possible to reduce the digoxin concentration in serum by 1/3.
With simultaneous use with digoxin in liquid dosage form or in the form of a rapidly dissolving drug, no interaction was observed.
With simultaneous application with zopiclone, zopiclone absorption is accelerated;
with cabergoline - possibly reducing the effectiveness of cabergoline; with ketoprofen - the bioavailability of ketoprofen decreases.
Due to the antagonism of dopamine receptors, metoclopramide can reduce the antiparkinsonian action of levodopa, while increasing the bioavailability of levodopa due to the acceleration of its evacuation from the stomach under the influence of metoclopramide.
The results of the interaction are ambiguous.
With simultaneous application with mexiletine, the absorption of mexiletine is accelerated;
with mefloquine - increases the rate of absorption of mefloquine and its concentration in the blood plasma, while reducing its side effects.
When used simultaneously with morphine, the absorption of morphine is accelerated when ingested and its sedative effect is enhanced.

At simultaneous application with nitrofurantoin absorption of nitrofurantoin decreases.

When metoclopramide is used immediately before administration of propofol or thiopental, their induction doses may need to be reduced.

In patients receiving metoclopramide, the effects of suxamethonium chloride are enhanced and prolonged.

With simultaneous application with tolterodine, the effectiveness of metoclopramide decreases;
with fluvoxamine - the case of development of extrapyramidal disorders has been described; with fluoxetine - there is a risk of developing extrapyramidal disorders; with cyclosporine - increases the absorption of cyclosporine and increases its concentration in the blood plasma.
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