Metoclopramide tablets 10mg, No. 56

• Vomiting

• nausea,

• hiccups of various origins.

• Atony and hypotension of the stomach and intestines (including postoperative);

• biliary dyskinesia; reflux esophagitis;

• flatulence;

• as part of the complex therapy of exacerbations of gastric ulcer and duodenal ulcer; acceleration of peristalsis during radiopaque studies of the gastrointestinal tract.

For adults inside - 5-10 mg 3-4 times / day. With vomiting, severe nausea, metoclopramide is administered intramuscularly or intravenously at a dose of 10 mg. Intranasally - 10-20 mg in each nostril 2-3 times / day.

Maximum doses: single ingestion - 20 mg; daily - 60 mg (for all modes 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 age, the daily dose for parenteral administration is 0.5-1 mg / kg, the frequency of administration is 1-3 times / day.

Pills

1 tab. metoclopramide 10 mg

• Bleeding from the gastrointestinal 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.

pharmachologic effect

Antiemetic, helps to reduce nausea, hiccups; stimulates gastrointestinal motility. The antiemetic effect is due to the blockade of dopamine D2 receptors and an increase in the threshold of the trigger zone chemoreceptors; it is a blocker of serotonin receptors. It is believed that metoclopramide inhibits dopamine-induced relaxation of gastric smooth muscles, thereby enhancing the cholinergic responses of gastrointestinal smooth muscles. Helps to accelerate gastric emptying by preventing relaxation of the stomach body and increasing the activity of the antrum and upper small intestine. Reduces the reflux of the contents into the esophagus by increasing the pressure of the esophageal sphincter 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 circulating aldosterone levels, which may be accompanied by short-term fluid retention.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract. Plasma protein binding is about 30%. Biotransformed in the liver. It is excreted mainly by the kidneys both unchanged and in the form of metabolites. T1 / 2 is from 4 to 6 hours.

Side effect

From the digestive system: at the beginning of treatment, constipation, diarrhea are possible; rarely dry mouth.

From the side of the central nervous system: at the beginning of treatment, a feeling of fatigue, drowsiness, dizziness, headache, depression, akathisia are possible. It is possible that extrapyramidal symptoms occur in children and young people (even after a single use of metoclopramide): spasm of the facial muscles, hyperkinesis, spastic torticollis (usually disappear immediately after stopping metoclopramide). With prolonged use, more often in elderly patients, the phenomena of parkinsonism, dyskinesia are possible.

On the part of the hematopoietic system: at the beginning of treatment, agranulocytosis is possible.

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

Allergic reactions: rarely - skin rash.

Application during pregnancy and lactation

Contraindicated in pregnancy.

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

In experimental studies, no adverse effects of metoclopramide on the fetus have been established.

Application for violations of liver function

Use with caution in patients with impaired liver function.

Application for impaired renal function

Use with caution in patients with impaired renal function.

Application in children

It should be used with extreme caution in children, especially young children. they have a significantly higher risk of dyskinetic syndrome.

Use in elderly patients

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 effects are extrapyramidal disorders, especially parkinsonism and tardive dyskinesia.

special instructions

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

It should be used with extreme caution in children, especially young children. they have a significantly higher risk of dyskinetic syndrome. In some cases, metoclopramide can be effective in vomiting caused by taking cytostatics.

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 effects are extrapyramidal disorders, especially parkinsonism and tardive dyskinesia.

Against the background of the use of metoclopramide, distortions of the data of laboratory indicators of liver function and determination of the concentration of aldosterone and prolactin in blood plasma are possible.

Influence on the ability to drive vehicles and use mechanisms

During the period of treatment, you should avoid potentially hazardous activities that require increased attention, rapid psychomotor reactions.

Drug interactions

With simultaneous use with anticholinergics, mutual weakening of the effects is possible.

With simultaneous use with antipsychotics (especially the phenothiazine series and butyrophenone derivatives), the risk of extrapyramidal reactions increases.

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

When administered intravenously, metoclopramide increases the rate of absorption of diazepam and increases its maximum concentration in blood plasma.

With simultaneous use with a slowly dissolving dosage form of digoxin, a decrease in the concentration of digoxin in the blood serum by 1/3 is possible. With simultaneous use with digoxin in a liquid dosage form or in the form of a rapidly dissolving dosage form, no interaction was noted.

When used simultaneously with zopiclone, the absorption of zopiclone is accelerated; with cabergoline - a decrease in the effectiveness of cabergoline is possible; with ketoprofen - the bioavailability of ketoprofen decreases.

Due to antagonism against dopamine receptors, metoclopramide can reduce the antiparkinsonian effect of levodopa, while it is possible to increase the bioavailability of levodopa due to the acceleration of its evacuation from the stomach under the influence of metoclopramide. Interaction results are mixed.

With simultaneous use with mexiletine, the absorption of mexiletine is accelerated; with mefloquine - the rate of absorption of mefloquine and its concentration in the blood plasma increase, while its side effects may decrease.

With simultaneous use with morphine, the absorption of morphine when taken orally is accelerated and its sedative effect is enhanced.

With simultaneous use with nitrofurantoin, the absorption of nitrofurantoin decreases.

When using metoclopramide immediately before the introduction of propofol or thiopental, it may be necessary to reduce their induction doses.

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

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