Metoclopramide - instructions for use, dose, side effects, contraindications

A specific blocker of dopamine (D2) and serotonin (5-HT3) receptors, inhibits the chemoreceptors of the trigger zone of the brainstem,weakens the sensitivity of the visceral nerves that transmit impulses from the pyloric and duodenum to the vomiting center. Through the hypothalamus and the parasympathetic nervous system (innervation of the gastrointestinal tract) has a regulating and coordinating effect on the tone and motor activity of the upper gastrointestinal tract (including the tone of the lower sphincter of the esophagus). Increases the tone of the stomach and intestines, accelerates the emptying of the stomach, reduces the hyperacid stasis, prevents pyloric and esophageal reflux, stimulates intestinal peristalsis. Normalizes the separation of bile, reduces the spasm of the sphincter of Oddi. Without changing its tone, it eliminates dyskinesia of the gallbladder. It has no M-holinoblokiruyuschim, antihistamine, antiserotoninovym and (ganglioblokiruyuschim action, does not affect the tone of the blood vessels of the brain, blood pressure, respiratory function, as well as kidney and liver, on the blood, the secretion of the stomach and pancreas. Increases the sensitivity of tissues to acetylcholine (the action does not depend on vagal innervation, but is eliminated by holinoblokatorami).Stimulating the secretion of aldosterone, increases the delay of Na⁺ and the selection of K⁺.

The onset of action on the digestive tract (gastrointestinal tract) occurs 1-3 minutes after intravenous administration and 10-15 minutes after intramuscular injection and is manifested by accelerating the evacuation of the stomach contents and antiemetic effect.

Pharmacokinetics:Bioavailability of 60-80%. Cmax in the blood is observed 1-2 hours after the administration of the drug. T1 / 2 - 3-5 hours, with renal dysfunction - up to 14 hours. It is metabolized in the liver. Removal of the drug occurs mainly through the kidneys for 24-72 hours (85% of the dose) in unchanged form (30%) and in the form of conjugates. Easily penetrates through the placental and blood-brain barrier, penetrates into the mother's milk.

Indications:Vomiting, nausea, hiccough of various genesis (in some cases can be effective in vomiting caused by radiation therapy or the use of cytotoxic drugs). Atony and hypotension of the stomach and intestines (in particular, postoperative); biliary dyskinesia; reflux esophagitis; flatulence; in the complex therapy of exacerbations of gastric ulcer and duodenal ulcer. It is used to enhance peristalsis during radiocontrast studies of the gastrointestinal tract.

Contraindications:Bleeding from the gastrointestinal tract, pyloric stenosis, mechanical intestinal obstruction, perforation of the stomach or intestine, pheochromocytoma, epilepsy, glaucoma, extrapyramidal disorders, Parkinson's disease, prolactin-dependent tumors, vomiting during treatment or overdose with antipsychotics and in breast cancer patients, early childhood age (up to 2 years), hypersensitivity to metoclopramide or other components of the drug.

Carefully:Children's age (increased risk of dyskinetic syndrome), hepatic and / or renal failure, bronchial asthma, hypertension, advanced age.

Pregnancy and lactation:Application during pregnancy and during lactation is contraindicated.

Dosing and Administration:

Introduce intravenously or intramuscularly adults at a dose of 10-20 mg 1-3 times a day (maximum daily dose - 60 mg); children older than 6 years of 5 mg 1-3 times a day; for children aged 2 to 6 years, the daily dose is 0.5-1 mg / kg body weight, the frequency of administration is 1-3 times.

For the prevention and treatment of nausea and vomiting caused by the use of cytostatics or radiation therapy,the drug is administered intravenously at a dose of 2 mg / kg body weight 30 minutes before the use of cytostatics or irradiation; if necessary, repeat the introduction after 2-3 hours.

Before the X-ray study, adults are administered intravenously 10-20 mg for 5-15 minutes before the study.

Patients with clinically expressed hepatic / renal insufficiency initially receive a dose twice as low as usual, the subsequent dose depends on the patient's individual response to metoclopramide.

Side effects:

From the nervous system: extrapyramidal disorders - spasm of facial musculature, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of extraocular muscles (including oculogic crisis), spastic torticollis, opisthotonus, muscular hypertonia; Parkinsonism (hyperkinesis, muscle rigidity is a manifestation of dopamine-blocking action, the risk of development in children and adolescents increases when the dose is exceeded 0.5 mg / kg / day); dyskinesia (in the elderly, with CRF (chronic renal failure), drowsiness, fatigue, anxiety, confusion, headache, dizziness, depression, tinnitus.

From the digestive system: constipation or diarrhea, rarely dry mouth. Allergic reactions: urticaria, bronchospasm (especially in patients with a history of bronchial asthma).

From the endocrine system: rarely (with long-term admission in high doses) gynecomastia, galactorrhea, menstrual irregularity.

Other: at the beginning of treatment, agranulocytosis is possible, rarely (when used in high doses) - hyperemia of the nasal mucosa.

Overdose:Symptoms: hypersomnia, disorientation and extrapyramidal disorders. Symptomatology disappears after discontinuation of the drug within 24 hours.

Interaction:

Strengthens the action of ethanol on the CNS (central nervous system), sedative effect of hypnotics, the effectiveness of therapy with H2-histamin blockers. Increases the absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol; slows the absorption of digoxin and cimetidine. Do not prescribe simultaneously with neuroleptics, because the risk of extrapyramidal reactions increases.

The action of metoclopramide may weaken the anticholinesterase drugs.

Special instructions:

It is not effective for vomiting of vestibular genesis.

Do not appoint after operations on the digestive tract (gastrointestinal tract) (like pyloroplasty or anastomosis of the intestine), because vigorous muscle contractions inhibit healing.

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

Most side effects occur within 36 hours of the start of treatment and disappear within 24 hours after cancellation. Treatment should be as short as possible.

During the treatment with the drug, alcohol is not recommended.

Effect on the ability to drive transp. cf. and fur:When the drug is administered, potentially dangerous activities that require increased attention, rapid mental and motor reaction (vehicle management, etc.) should be avoided.

Form release / dosage:Solution for intravenous and intramuscular injection 5 mg / ml in ampoules of 2 ml.

Packaging:

5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil (or without foil); for 1 or 2 contour squares with instructions for use in a pack of cardboard.

For 20, 50 or 100 contour mesh packages with 10, 25 or 50 instructions for use, respectively, in a cardboard box or a box of corrugated cardboard (for hospital).

In a pack, box or box, knives or scarifier ampoules are put. When packing ampoules with notches, rings or break points, knives or scarifier ampoules do not.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002571 / 01

Date of registration:10.06.2008 / 05.08.2014

Expiration Date:Unlimited

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Information update date: & nbsp09.05.2018

Illustrated instructions

Instructions

Metoclopramide (Metoclopramide)