Metoclopramide pills 10mg №56

Mechanism of action

Antiemetic, helps reduce nausea, hiccups; stimulates gastrointestinal peristalsis. Antiemetic effect due to blockade of dopamine D₂-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 muscles of the stomach caused by dopamine, thus enhancing the cholinergic reactions of the smooth muscles of the gastrointestinal tract. It contributes to the acceleration of gastric emptying by preventing the relaxation of the body of the stomach and increasing the activity of the antrum and the upper small intestine. It reduces the reflux of the contents into 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 short-term fluid retention.

Pharmacokinetics

After ingestion is rapidly absorbed from the gastrointestinal tract. Plasma protein binding is about 30%. Biotransforming in the liver. It is excreted mainly by the kidneys both in unchanged form and in the form of metabolites. T_1/2 ranges from 4 to 6 h.

Indications

Vomiting, nausea, hiccups of various origins. Atony and hypotonia of the stomach and intestines (including postoperative); biliary dyskinesia; reflux esophagitis; flatulence; as part of complex therapy of acute gastric and duodenal ulcers; acceleration of peristalsis during radiopaque studies of the gastrointestinal tract.

Dosage and administration

Adults inside by 5-10 mg 3-4 times / day. With vomiting, severe nausea metoclopramide administered in / m or / in a dose of 10 mg. Intranasal - 10-20 mg in each nostril 2-3 times / day.

Maximum doses: single intake - 20 mg; daily - 60 mg (for all routes of administration).

The average single dose for children older than 6 years is 5 mg 1-3 times / day. inside or parenterally. For children under the age of 6, the daily dose for parenteral administration is 0.5–1 mg / kg, the frequency of administration — 1–3 times / day.

Side effect

Gastrointestinal: at the beginning of treatment, constipation, diarrhea; 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. Extrapyramidal symptoms may occur in children and young people (even after a single use of metoclopramide): spasm of the facial muscles, hyperkinesis, spastic torticollis (as a rule, they disappear immediately after stopping metoclopramide). With prolonged use, often in elderly patients, parkinsonism and dyskinesia are possible.

Hemic and lymphatic: 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 disorders.

Allergic reactions: rarely a skin rash.

Contraindications

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

Use during pregnancy and lactation

Contraindicated for use in pregnancy.

When used during lactation (breastfeeding) 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.

Application for violations of the liver

With caution used in patients with impaired liver function.

Application for violations of kidney function

It is used with caution in patients with impaired renal function.

Use in elderly patients

When used in elderly patients, it must be borne in mind that with prolonged use of metoclopramide in high or medium doses, the most frequent side effects are extrapyramidal disorders, especially parkinsonism and tardive dyskinesia.

Use in children

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

Special notes

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

With extreme caution should be used in children, especially young children, because they have a significantly higher risk of dyskinetic syndrome. Metoclopramide in some cases it may be effective in vomiting caused by the administration of cytostatics.

When used in elderly patients, it must be borne in mind that with prolonged use of metoclopramide in high or medium doses, the most frequent side effects are extrapyramidal disorders, especially parkinsonism and tardive dyskinesia.

Against the background of the use of metoclopramide, data may be distorted by laboratory parameters of liver function and determine the concentration of aldosterone and prolactin in the blood plasma.

Influence on ability to drive motor transport and control mechanisms

During treatment, you should avoid potentially hazardous activities that require increased attention, quick psychomotor reactions.

Drug interaction

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

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

With simultaneous use increases the absorption of Acetylsalicylic acid, Paracetamol, ethanol.

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

With simultaneous use with a slowly dissolving Digoxin dosage form, it is possible to reduce the concentration of digoxin in serum by 1/3. With simultaneous use of digoxin in a liquid dosage form or in the form of an instant dosage form of the interaction is not marked.

When applied simultaneously with zopiclone, zopiclone absorption is accelerated; with cabergoline - may decrease the effectiveness of cabergoline; with Ketoprofen - decreases the bioavailability of ketoprofen.

Due to antagonism of dopamine receptors metoclopramide may reduce the anti-Parkinsonian effect of levodopa, while it may increase 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.

At simultaneous use with meksiletinom absorption of meksiletin accelerates; with mefloquine - the rate of absorption of mefloquine and its concentration in the blood plasma increases, while its side effects can be reduced.

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

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

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

In patients receiving metoclopramide, the effects of Suxamethonia Chloride are enhanced and prolonged.

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