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

Pharmacodynamics: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 pylorus 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 duodenopiloric and gastroesophageal 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. Does not affect the tone of the blood vessels of the brain, blood pressure, respiratory function, as well as kidney and liver, on hematopoiesis, gastric and pancreatic secretion. Stimulates the secretion of prolactin. Increases the sensitivity of tissues to acetylcholine (the action does not depend on vagal innervation, but is eliminated by m-holinoblokatorami). Stimulating the secretion of aldosterone, enhances the retention of sodium ions and the excretion of potassium ions.

Pharmacokinetics:Quickly absorbed from the gastrointestinal tract. In connection with partial destruction in the liver after absorption, bioavailability is 75%. The time to reach the maximum concentration in the blood plasma is 1-2 hours. Connection with plasma proteins - 13 - 30%. The half-life period is from 2.5 to 6 hours, with kidney failure - up to 14 hours. The excretion of metoclopramide occurs mainly through the kidneys for 24 hours in unchanged form and in the form of conjugates. Passes through the placental and blood-brain barrier and penetrates into the mother's milk.

Indications:Vomiting, nausea, hiccough of various genesis (in some cases can be effective in vomiting caused by taking 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:

Hypersensitivity to the drug components, lactase deficiency, lactose intolerance,glucose-galactose insufficiency, bleeding from the gastrointestinal tract, stenosis of the pylorus, mechanical intestinal obstruction, perforation of the wall of the stomach or intestine, pheochromocytoma, epilepsy, glaucoma, extrapyramidal disorders, Parkinson's disease, prolactin-dependent tumors, vomiting during treatment or overdose with antipsychotics and patients with breast cancer, pregnancy (I trimester), lactation period, children under 14 years.

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

Carefully:Children and old age, renal / hepatic insufficiency, bronchial asthma, arterial hypertension, pregnancy II and III trimester.

Pregnancy and lactation:

The drug is contraindicated in the first trimester of pregnancy. In the II and III trimester of pregnancy, the use of the drug is possible in the event that the intended benefit to the mother exceeds the potential risk to the fetus.

For the duration of treatment, breastfeeding should be discontinued. the drug is excreted in breast milk.

Dosing and Administration:

Inside, 30 minutes before eating, squeezed a little water.

For adults, the recommended single dose is 10 mg, the maximum daily dose is 30 mg (10 mg 3 times a day) or 0.5 mg per 1 kg of body weight, the duration of treatment should not be more than 5 days.

For children older than 14 years, the recommended dose of 0.1-0.15 mg per 1 kg of body weight, the maximum daily dose of 0.5 mg per 1 kg of body weight, the maximum duration of use of 5 days.

In renal failure: in patients with terminal renal failure (creatinine clearance less than 15 ml / min), the daily dose should be reduced by 75%; in patients with moderate and severe renal insufficiency (CC 15-60 ml / min) - the dose should be reduced by 50%.

For hepatic insufficiency: in patients with severe hepatic insufficiency, the dose should be reduced by 50%.

Side effects:

The drug is usually well tolerated. Disorders are possible:

From the central nervous system: extrapyramidal disorders, drowsiness, fatigue, anxiety, headache, tinnitus, depression, anxiety, malignant neuroleptic syndrome; in children,may develop a dyskinetic syndrome (convulsive twitching of the muscles of the face, neck or shoulders); tardive dyskinesia (with severe renal failure and in elderly people); after long-term treatment in some elderly patients, Parkinsonism (hyperkinesis, muscle stiffness) can develop;

From the digestive system: constipation or diarrhea, dry mouth;

From the endocrine system: (with long-term admission in high doses) - gynecomastia, galactorrhea, menstrual cycle disorder;

From the cardiovascular system: supraventricular tachycardia, increase or decrease of blood pressure.

Allergic reactions: hypersensitivity reactions, urticaria;

From the hematopoiesis: agranulocytosis;

Other: when used in high doses - hyperemia of the mucous membrane of the nasal cavity;

Most side effects occur within 36 hours of the start of treatment and disappear within 24 hours after cancellation.

Overdose:

Symptoms of overdose: drowsiness, confusion, irritability, anxiety, seizures, extrapyramidal movement disorders,disorders of the cardiovascular system. Typically, the symptoms disappear after stopping the drug after 24 hours.

Treatment: symptomatic. Extrapyramidal disorders are eliminated by the slow administration of biperidene; it is possible to use diazepam.

Interaction:

Strengthens the action of ethanol on the central nervous system, the sedative effect of hypnotics, increases the effectiveness of therapy with blockers H₂ -gistaminovyh receptors.

Increases the absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol, bioavailability of bromocryptine and cyclosporine (control of its concentration in the blood is necessary); slows the absorption of digoxin and cimetidine; reduces the effectiveness of pergolide.

It is not recommended simultaneous use with tricyclic antidepressants, MAO inhibitors, sympathomimetics (metoclopramide promotes the release of catecholamines from nerve endings) because of the possibility of a mutual increase in side effects and the unpredictability of changes in the severity of the action of antidepressants and sympathomimetics.

When used simultaneously with serotonin reuptake inhibitors, as with neuroleptics, the risk of developing extrapyramidal symptoms increases.

The action of metoclopramide may weaken the anticholinesterase drugs.

Special instructions:

It is not effective for vomiting of vestibular genesis.

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

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

Effect on the ability to drive transp. cf. and fur:When taking the drug should be avoided potentially dangerous activities that require increased concentration of attention, rapid mental and motor reaction (driving vehicles, etc.).

Form release / dosage:Tablets 10 mg.

Packaging:

10 tablets per contour cell packaging made of polyvinylchloride film and flexible packaging on the basis of aluminum foil for medicines or aluminum foil or foil-based composite material.

For 1, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002367

Date of registration:11.02.2014

Expiration Date:11.02.2019

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp09.05.2018

Illustrated instructions

Instructions

Metoclopramide (Metoclopramide)