When does the antiemetic shot metoclopramide start working? Metoclopramide: instructions, price, reviews

A drug metoclopramide is a peristalsis stimulant (propulsion).
Metoclopramide is a central dopamine antagonist that also exhibits peripheral cholinergic activity.
Two main effects of the drug are noted: antiemetic and the effect of accelerating gastric emptying and passage through the small intestine.
The antiemetic effect is caused by the action on the central point of the brain stem (chemoreceptors - the activating zone of the vomiting center), probably due to inhibition of dopaminergic neurons.
The increase in peristalsis is also partially controlled by higher centers, but a mechanism of peripheral action may also be partially involved, along with activation of postganglionic cholinergic receptors and, possibly, inhibition of dopaminergic receptors in the stomach and small intestine. Through the hypothalamus and parasympathetic nervous system, it regulates and coordinates the motor activity of the upper gastrointestinal tract: it increases the tone of the stomach and intestines, accelerates gastric emptying, reduces gastrostasis, prevents pyloric and esophageal reflux, stimulates intestinal motility. Normalizes the secretion of bile, reduces spasm of the sphincter of Oddi without changing its tone, eliminates dyskinesia of the gallbladder.
Side effects extend mainly to extrapyramidal symptoms, which are based on the mechanism of dopamine receptor-blocking action on the central nervous system.
Long-term treatment with metoclopramide can cause an increase in serum prolactin concentration due to the lack of dopaminergic inhibition of prolactin secretion. In women, cases of galactorrhea and menstrual irregularities are described, in men - gynecomastia. However, these symptoms disappeared after treatment was stopped.

Pharmacokinetics

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The onset of action on the gastrointestinal tract is noted 1-3 minutes after intravenous administration and 10-15 minutes after administration. Antiemetic action persists for 12:00. 13-30% of the drug binds to plasma proteins. The volume of distribution is 3.5 l / kg. Penetrates through the blood-brain and placental barriers, excreted in breast milk. Metabolized in the liver. The half-life is 4-6 hours. Part of the dose (about 20%) is excreted in the initial form, and the rest (about 80%) after metabolic transformations by the liver is excreted by the kidneys in compounds with glucuronic or sulfuric acid.
In patients with severe renal insufficiency, creatinine clearance is reduced to 70%, and the half-life of blood is increased (approximately 10:00 at CC 10-50 ml / min and 15 hours at CC<10 мл / мин).
In patients with cirrhosis of the liver, accumulation of metoclopramide was observed, which was accompanied by a decrease in blood clearance by 50%.

Indications for use

metoclopramide for adults: prevention of postoperative nausea and vomiting; nausea and vomiting caused by radiation; symptomatic treatment of nausea and vomiting, including those associated with acute migraine.
metoclopramide for children: as a second-line drug for the prevention of delayed nausea and vomiting caused by chemotherapy; treatment of postoperative nausea and vomiting.

Mode of application

Injection metoclopramide use intramuscularly or intravenously as a slow bolus injection for at least 3 minutes.
As a solvent, use 0.9% sodium chloride solution, 5% glucose solution.
Adults.
The drug is prescribed at a dose of 10 mg up to 3 times a day. The maximum daily dose is 30 mg or 0.5 mg/kg of body weight.
The use of injectable forms should be carried out for the shortest possible period of time with the transition to the use of oral or rectal forms of metoclopramide as soon as possible.
children.
When used to prevent postoperative nausea and vomiting, metoclopramide should be used after surgery.
The recommended dose of metoclopramide is 0.1-0.15 mg/kg body weight up to 3 times a day. The maximum daily dose is 0.5 mg/kg body weight. If it is necessary to continue the use of the medicinal product, at least 6-hour intervals should be observed.
Dosing schedule:

The maximum duration of use of metoclopramide for the treatment of established postoperative nausea and vomiting is 48 hours.
The maximum duration of the use of metoclopramide to prevent delayed nausea and vomiting caused by chemotherapy is 5 days.
Patients with impaired renal function
In patients with end-stage renal dysfunction (creatinine clearance ≤ 15 ml/min), the dose of metoclopramide should be reduced by 75%.
In patients with moderate to severe renal impairment (creatinine clearance 15-60 ml / min), the dose of metoclopramide should be reduced by 50%.
In patients with hepatic insufficiency due to an increase in the half-life, use half the dose.
Elderly patients.
Consideration should be given to reducing the dose in elderly patients due to age-related decline in renal and hepatic function.
duration of treatment.
In order to minimize the risks of adverse reactions from the nervous system and other adverse reactions, the drug should be used only for short-term treatment (up to 5 days).
Children. Metoclopramide is contraindicated in children under the age of 1 year.

Side effects

From the gastrointestinal tract: nausea, dyspepsia, dry mouth, constipation. When using metoclopramide in doses exceeding the daily dose, diarrhea may occur in patients.
From the nervous system: extrapyramidal reactions, usually dystonia (including very rarely cases of dyskinetic syndrome), especially in children and patients under the age of 30, the risk of which increases when a daily dose of 0.5 mg / kg of body weight is exceeded: muscle spasm, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of extraocular muscles, including oculogeric crises, involuntary spasmodic movements, in particular in the head, neck and shoulders, tonic blepharospasm, unnatural positions of the head and shoulders, opisthotonus, muscle hypertonicity; parkinsonism (tremor, muscle twitching, bradykinesia, muscle rigidity, akinesia, mask-like face) after long-term treatment with metoclopramide in some elderly patients, as well as in renal insufficiency elderly patients (especially women), in patients with diabetes mellitus and usually develops after discontinuation of the drug. Manifested by involuntary movements of the tongue, face, mouth, jaw, sometimes involuntary movements of the trunk and / or limbs;
neuroleptic malignant syndrome, including hyperpyrexia, altered consciousness, muscle rigidity, dysfunction of the autonomic nervous system and elevated serum CK levels. This syndrome is potentially lethal, if it occurs, you must immediately stop taking metoclopramide and urgently start treatment (dantrolene, bromocriptine); fever, headache, dizziness, drowsiness, fatigue, fear, confusion, asthenia, fatigue, depressed level of consciousness, tinnitus, akathisia.
There is also a risk of acute (short-term) neurological disorders, higher in children.
On the part of the psyche: depression, hallucinations, confusion, anxiety, restlessness.
From the side of the cardiovascular system: bradycardia, especially with intravenous use, cardiac arrest for a short time after injection, which may be due to bradycardia, AV block, blockade of the sinus node, especially with intravenous use, prolongation of the QT interval, supraventricular extrasystole, ventricular extrasystole , ventricular tachycardia of the "pirouette" type, arterial hypotension, shock, syncope with intravenous administration, acute arterial hypertension in patients with pheochromocytoma.
Separate reports have been registered on the possibility of developing severe cardiovascular reactions due to the use of metoclopramide, especially when administered intravenously.
On the part of the blood and lymphatic system: methemoglobinemia, which may be associated with a deficiency of NADH-cytochrome-b5-reductase, especially in infants, sulfhemoglobinemia, which is associated mainly with the concomitant use of high doses of drugs, release sulfur.
From the immune system: hypersensitivity reactions, including anaphylactic reactions, including Quincke's edema, anaphylactic shock. Due to the content of sodium sulfite in the dosage form, there may be isolated cases of hypersensitivity reactions, especially in patients with bronchial asthma, in the form of nausea, vomiting, wheezing, acute asthma attack, impaired consciousness or shock. These reactions may have an individual course.
From the skin and subcutaneous tissue: hypersensitivity reactions, in particular: skin rashes, flushing and itching of the skin, urticaria.
On the part of the reproductive system and the function of the mammary glands: after longer drug therapy, due to stimulation of prolactin secretion, hyperprolactinemia, gynecomastia, galactorrhea or menstrual irregularities may occur, amenorrhea with the development of these phenomena, the use of metoclopramide should be discontinued.
Laboratory indicators: increased levels of liver enzymes.
In adolescent patients with severely impaired renal function (renal failure), as a result of which the withdrawal of metoclopramide is weakened, the development of side effects should be monitored especially carefully. In case of their occurrence, the use of the drug should be stopped immediately.
The risk of developing adverse reactions from the nervous system increases with the use of the drug in high doses and with prolonged use.

Contraindications

Contraindications to the use of the drug metoclopramide are: hypersensitivity to metoclopramide or to any other component of the drug; gastrointestinal bleeding; mechanical intestinal obstruction; gastrointestinal perforation; confirmed or suspected pheochromocytoma (due to the risk of severe attacks of arterial hypertension); tardive dyskinesia caused by neuroleptics or metoclopramide in history; epilepsy (increased frequency and intensity of seizures); Parkinson's disease; simultaneous use with levodopa or dopaminergic agonists; installed?? methemoglobinemia with the use of metoclopramide or a history of NADH-cytochrome b5 reductase deficiency; prolactin deposits of the tumor; increased convulsive readiness (extrapyramidal movement disorders); the patient's age is up to 1 year (due to the risk of developing extrapyramidal disorders).
Due to the content of sodium sulfite, the drug should not be prescribed to patients with bronchial asthma with hypersensitivity to sulfite.

Pregnancy

A large amount of data in pregnant women (more than 1000 uses of the drug) indicates the absence of toxicity, which leads to malformations or fetotoxicity.

metoclopramide can be used during pregnancy if there is a clinical need. Through pharmacological properties (as in other antipsychotics), in the case of the use of metoclopramide at the end of pregnancy, the appearance of extrapyramidal syndrome in the newborn cannot be ruled out. It is necessary to avoid the use of metoclopramide in the final stages of pregnancy. When using metoclopramide, you need to monitor the newborn.
Metoclopramide passes into breast milk in small amounts. Therefore, it is not recommended to use metoclopramide during breastfeeding. Consideration should be given to discontinuing metoclopramide in women who are breastfeeding.

Interaction with other drugs

Combinations are contraindicated.
Levodopa or dopaminergic agonists and metoclopramide are characterized by mutual antagonism.
Combinations to avoid.
Alcohol enhances the sedative effect of metoclopramide.
Combinations to watch out for.
When used simultaneously with oral drugs, such as paracetamol, metoclopramide may affect their absorption due to the effect on gastric motility.
Anticholinergics and morphine derivatives: Anticholinergics and morphine derivatives are characterized by mutual antagonism with metoclopramide with respect to the effect on the motor activity of the digestive tract.
Central nervous system inhibitors (morphine derivatives, antipsychotics, sedative antihistamine H 1 receptor blockers, sedative antidepressants, barbiturates, clonidine and related drugs): potentiate the action of metoclopramide.
Antipsychotics: In the case of the use of metoclopramide in combination with other antipsychotics, a cumulative effect and the appearance of extrapyramidal disorders may occur.
Serotonergic drugs: The use of metoclopramide in combination with serotonergic drugs, such as selective serotonin reuptake inhibitors (SSRIs), may increase the risk of developing serotonin syndrome.
Digoxin: Metoclopramide may decrease the bioavailability of digoxin. Plasma concentrations of digoxin should be closely monitored.
Cyclosporine: metoclopramide increases the bioavailability of cyclosporine (Cmax by 46% and effect by 22%). It is necessary to carefully monitor the concentration of cyclosporine in plasma. The clinical implications of this phenomenon have not been definitively determined.
Mivacurium and suxamethonium: Metoclopramide injection may prolong the duration of neuromuscular block (by inhibiting plasma cholinesterase).
Strong inhibitors of CYP2D6: The level of metoclopramide exposure is increased when it is used simultaneously with strong inhibitors of CYP2D6, such as fluoxetine and paroxetine. Although the clinical significance of this is not exactly known, patients should be monitored for adverse reactions.
Metoclopramide may prolong the action of succinylcholine.
Due to the content of sodium sulfite in the injection solution, thiamine (vitamin 1), taken simultaneously with metoclopramide, can be quickly broken down in the body.

Overdose

Overdose symptoms metoclopramide: drowsiness, decreased level of consciousness, confusion, irritability, anxiety and its increase, convulsions, extrapyramidal-motor disorders, dysfunction of the cardiovascular system with bradycardia and an increase or decrease in blood pressure, hallucinations, respiratory and cardiac arrest, dystonic reactions. Isolated cases of methemoglobinemia have been reported.
Treatment: extrapyramidal disorders are eliminated by slow administration of the biperiden antidote. In the case of large doses of metoclopramide, it must be removed from the gastrointestinal tract by gastric lavage or activated charcoal and sodium sulfate should be taken. Observe the vital functions of the body until the symptoms of poisoning disappear completely.

Storage conditions

Keep out of the reach of children in the original packaging at a temperature not exceeding 25 ° C. Do not freeze.

Release form

Metoclopramide - solution for injection.
Packing: 2 ml in an ampoule; 5 ampoules in a blister pack, 1 or 2 blister packs in a pack.

Compound

1 ml metoclopramide hydrochloride 5 mg.
Excipients: sodium chloride, sodium edetate, anhydrous sodium sulfite (E 221), propylene glycol, dilute hydrochloric acid, water for injection.

Additionally

The drug should not be used for the treatment of chronic diseases such as gastroparesis, dyspepsia and gastroesophageal reflux disease or as an adjunct to surgical or radiological procedures.
Patients under 30 years of age are more likely to develop dystonic-dyskinetic disorders when treated with metoclopramide.
With caution, prescribe the drug to elderly patients due to the frequent occurrence of parkinsonism.
neurological disorders.
Extrapyramidal disorders may occur, especially in children, and/or at high doses. These reactions are usually observed at the beginning of treatment and may occur after a single application. If extrapyramidal symptoms develop, metoclopramide should be discontinued immediately. In general, these effects disappear completely upon discontinuation of treatment, but may require symptomatic treatment (benzodiazepines in children and/or anticholinergic antiparkinsonian drugs in adults).
Between each administration of metoclopramide, even in the case of vomiting and dose rejection, at least a 6-hour interval must be observed to avoid overdose.
Long-term treatment with metoclopramide can lead to tardive dyskinesia, which is potentially irreversible, especially in the elderly. Treatment should not be continued for more than 3 months due to the risk of tardive dyskinesia. Treatment should be discontinued if clinical signs of tardive dyskinesia appear.
Neuroleptic malignant syndrome has been reported with the use of metoclopramide in combination with neuroleptics, as well as with metoclopramide monotherapy. If symptoms of neuroleptic malignant syndrome occur, metoclopramide should be discontinued immediately and appropriate treatment instituted.
In patients with concomitant neurological diseases and in patients receiving treatment with other drugs acting on the central nervous system, it is necessary to be especially careful.
The use of metoclopramide may also increase the symptoms of Parkinson's disease.
Methemoglobinemia.
Cases of methemoglobinemia have been reported, which may be associated with a deficiency of NADH-cytochrome b5 reductase. In such cases, you should immediately permanently stop taking metoclopramide and take appropriate measures (for example, treatment with methylene blue).
Heart disorders.
Serious adverse reactions from the cardiovascular system have been reported, including cases of acute vascular insufficiency, severe bradycardia, cardiac arrest and prolongation of the QT interval, which were observed after taking metoclopramide in the form of injections, especially after administration.
The drug should be administered intravenously as a slow bolus injection (over at least 3 minutes) to reduce the risk of adverse reactions (eg, hypotension, akathisia).
Impaired kidney and liver function.
In patients with impaired renal function or severely impaired liver function, a dose reduction is recommended.
The drug should be used with caution in patients at risk, namely in elderly patients with cardiac conduction disorders, with uncorrected electrolyte imbalance or bradycardia, and patients taking other drugs that prolong the QT interval. The drug should not be used for the treatment of chronic diseases such as gastroparesis, dyspepsia and gastroesophageal reflux disease or as an adjunct to surgical or radiological procedures.
Ampoules taken from the package should not be left in the sun for a long time.

main parameters

Name:	METHOCLOPRAMIDE
ATX code:	A03FA01 -

The antiemetic drug metoclopramide is a drug that acts by blocking dopamine receptors. This leads to a decrease in the manifestations of nausea and vomiting, reduces the dysfunction of the digestive tract. The composition of the drug includes the active substance metoclopramide. Familiarize yourself with the effect of the medication from the instructions for use.

Composition and form of release

Instructions for use Metoclopramide contains information that the agent is presented in two formats. Their composition and description:

	Tablets
Description	White round pills	clear liquid
Metocoproamide hydrochloride concentration, mg		5 per 1 ml (10 per 1 ampoule)
Auxiliary components	Corn starch, sodium glycolate, magnesium stearate, talc, lactose, colloidal silica anhydrous	Water, sodium acetate, glacial acetic acid, ethylenediaminetetraacetic acid disodium salt, sodium metabisulphite
Package	Blisters of 10 pcs., 5 or 10 blisters in a pack	Ampoules of 2 ml, 5 pcs. in a pallet, 1 or 2 pallets in a pack

pharmachologic effect

Metoclopramide (Metoclopramide) reduces nausea, hiccups, stimulates the peristalsis of the gastrointestinal tract. The action of the drug is based on the blockade of dopamine D2 receptors, increasing the threshold of the trigger zone chemoreceptors. Also, the drug blocks serotonin receptors, inhibits the relaxation of the smooth muscles of the stomach, which is caused by dopamine and cholinesterase. This enhances cholinergic responses.

The use of the drug accelerates the emptying of the stomach by relaxing its body and increasing the activity of the antrum along with the upper sections of the small intestine. Metoclopramide reduces reflux (throwing) of contents into the esophagus, because it increases the pressure of its sphincter at rest, increases the clearance of acid from the esophagus by normalizing the amplitude of peristaltic contractions.

The drug promotes the production of prolactin, which leads to a transient increase in the level of circulating aldosterone - this can cause short-term fluid retention. After entering the body, the active component is rapidly absorbed, binds to plasma proteins by 30%, and undergoes biotransformation in the liver. The substance is excreted by the kidneys, the half-life is 4-6 hours.

Indications for use Metoclopramide

The instructions for use of the medication indicate the indications for use. These include:

vomiting, nausea, hiccups of various causes;
atony of the intestines, stomach, including postoperative cases;
biliary dyskinesia of the hypomotor type;
flatulence;
reflux esophagitis;
complex therapy of exacerbations of gastric or duodenal ulcers;
vomiting caused by cytostatics or radiation therapy;
functional pyloric stenosis;
facilitation of duodenal sounding for the study of the digestive tract.

Method of application and dosage

Depending on the form of release, the method of using the product differs. So, tablets are indicated for oral administration, and the solution is for parenteral administration. Dosages, frequency of administration and duration of the course of drug therapy are indicated in the instructions, but may vary depending on the individual characteristics of the patient, his age, type of disease.

According to the instructions, the tablets are taken orally 5-10 mg 3-4 times a day. The maximum single dose is 20 mg, daily - 60 mg. The average single dosage for children over six years old is 5 mg 1-3 times a day. Children under six years of age should not be given tablets, they are shown only parenteral administration of the solution, based on the dosages indicated below.

Metoclopramide solution

For intravenous or intramuscular administration, the use of a solution of metoclopramide is indicated. The maximum daily adult dose is 60 mg. In case of vomiting, the drug is administered intravenously at a dosage of 2 mg / kg of body weight half an hour before taking cytostatics or radiation, after 2-3 hours the dose is repeated. Before x-rays, adults are given 10-20 mg intravenously 5-15 minutes before the study.

For patients with hepatic or renal insufficiency, the dosage should be halved. With severe vomiting, the drug can be administered intramuscularly at a dose of 10 mg or dripped into the nose - into each nostril, 10-20 mg 2-3 times a day. The average single dosage for children over 6 years old is 5 mg 1-3 times a day, up to six years - 0.5-1 mg / kg of body weight 1-3 times a day.

special instructions

The drug should be used with caution in patients with arterial hypertension. Other special instructions from the instructions:

In young children, the use of the drug should be carried out with extreme caution.
In elderly patients, long-term use of metoclopramide in high doses can lead to extrapyramidal disorders, tardive dyskinesia, parkinsonism.
Against the background of treatment with the drug, distortions of the results of determining the level of prolactin and aldosterone in plasma are possible.
During therapy, driving and dangerous mechanisms should be avoided, because the concentration of attention decreases.
The composition of the solution includes sodium sulfite, so it should not be prescribed to patients with bronchial asthma and hypersensitivity to sulfites.
During therapy, the use of alcohol is prohibited.

metoclopramide during pregnancy

Metoclopramide tablets, according to the instructions, are contraindicated for use during pregnancy and breastfeeding, although studies have shown no adverse effect of the drug on fetal development. The solution is forbidden to use in the first trimester of pregnancy and lactation, but in the second and third trimesters it can be used for health reasons.

Metoclopramide for children

The drug is used with caution in young children due to the high risk of developing dyskinetic syndrome. Tablets are contraindicated for a child under 6 years old, solution - up to 2 years. The dosage of the drug is calculated according to the weight of the baby - 0.5-1 mg per kg of body weight 1-3 times a day, unless the doctor prescribes otherwise. Pediatrician approval must be obtained before use.

drug interaction

When combined with other drugs, adverse reactions of metoclopramide may occur. The instructions for use talk about these combinations and consequences:

Anticholinergics in combination with the drug weaken the effect of each other.
The combination of the drug with neuroleptics, phenothiazines, butyrophenone derivatives leads to the development of extrapyramidal reactions.
Metoclopramide enhances the absorption of ethanol, acetylsalicylic acid, Paracetamol, antibiotics, tetracyclines.
The combination of the drug with a slowly dissolving form of Digoxin leads to a reduction in its serum level by a third. No interactions have been observed between the liquid or instant dosage form.
Metoclopramide accelerates the degree of absorption of Zopiclone, Mefloquine, Morphine, Cyclosporine, Cimetidine and Mexiletine, reduces the effectiveness of Cabergoline, Nitrofurantoin and the bioavailability of Ketoprofen.
The drug exhibits antagonism against dopamine receptors, therefore, it reduces the anti-parkinsonic effect of Levodopa, increases its bioavailability.
Intravenous administration of the solution increases the rate of absorption of Diazepam, its maximum plasma concentration.
Dose reduction of Thiopental or Propofol is required when combined with metoclopramide.
The drug enhances and lengthens the effects of suxamethonium chloride.
The combination of the drug with Fluvoxamine or Fluoxetine leads to the development of extrapyramidal disorders.

Side effects

Most of the side effects occur within 36 hours after taking the drug and disappear within a day. Possible reactions, according to the instructions, are:

dyskinesia, parkinsonism;
akathisia, fatigue, depression, drowsiness, headache, dizziness;
spasm of the facial muscles, hyperkinesis, spastic torticollis;
agranulocytosis, leukopenia;
angioedema;
increased activity of sweat glands;
gynecomastia, amenorrhea, dysmenorrhea, menstrual disorders;
skin rash, allergy, hyperemia, urticaria.

Overdose

The instructions call hypersomnia, disorientation, extrapyramidal disorders as symptoms of an overdose of Metoclopramide. They can be eliminated by discontinuing drug therapy. Signs disappear within a day after cancellation. If necessary, treatment with antiparkinsonian and m-anticholinergic agents is possible.

Contraindications

The drug is used with caution in childhood and old age, with Parkinson's disease, bronchial asthma, renal or hepatic insufficiency, arterial hypertension. According to the instructions, contraindications for the use of the drug are:

hypersensitivity to the components of the composition;
combination with anticholinergics, m-anticholinergics;
perforation of the digestive tract;
lactation, pregnancy;
lockjaw;
mechanical obstruction of the intestine;
hypertensive crisis, hypotension;
av-blockade;
sulfagemoglobinemia;
pheochromocytoma;
glaucoma;
opisthotonus;
prolactin-dependent tumors;
epilepsy;
postoperative intervention on the gastrointestinal tract, pyloroplasty, intestinal anastomosis.

Terms of sale and storage

The drug is prescription, stored at temperatures up to 25 degrees for 4 years.

Analogues

The drug can be replaced by drugs with a similar effect and the same or a different composition. The analogues of the funds are:

Cerucal - antiemetic tablets and injections based on the same active substance;
Reglan - parenteral, oral solution and tablets for vomiting containing metoclopramide;
Metamol - tablets based on metoclopramide, blocking dopamine and serotonin receptors.

Metoclopramide price

The drug is sold on the Internet and through regular pharmacies, the cost depends on the form of release and the volume of the pack. Approximate prices in Moscow:

Release type	Manufacturer	Internet cost, rubles	Pharmacy price, rubles
Ampoules 2 ml 10 pcs.	Novosibkhimfarm, Russia
Ampoules 2 ml 10 pcs.	Sotex, Russia
Ampoules 2 ml 5 pcs.	Polpharma, Poland
Tablets 10 mg 50 pcs.	Polpharma, Poland
Tablets 10 mg 50 pcs.	Moscow Endocrine Plant, Russia
Tablets 10 mg 56 pcs.	Reneval, Russia

Metoclopramide Tablets 10 mg - blister pack 10, cardboard pack 1 - No. LS-002707, 2006-12-29 from NIOPIK SSC (Russia)

Latin name

Metoclopramide

Active substance

Metoclopramide*(Metoclopramide*)

ATX

A03FA01 Metoclopramide

Pharmacological group

Antiemetics

Nosological classification (ICD-10)

K21 Gastroesophageal reflux K22.4 Esophageal dyskinesia K31.8.0* Gastric atony K59.8.0* Intestinal atony K59.8.1* Intestinal dyskinesia K82.8.0* Gallbladder and biliary dyskinesia K92.9 Disease of the digestive system, unspecified K94* Diagnosis of diseases of the gastrointestinal tract21 Excessive vomitingR14 Nausea and vomitingR06.6 Hiccups Flatulence and related conditions T36 Poisoning with systemic antibiotics T40 Poisoning with narcotics and psychodysleptics [hallucinogens] T46.0 Poisoning with cardiac glycosides and similar drugs T50.9 Other and unspecified drugs, medicaments and biological substances

Composition and form of release

1 tablet contains metoclopramide 0.0105 g (in terms of anhydrous - 0.01 g), as well as excipients (milk sugar, corn starch, gelatin, calcium stearate) - in a blister pack 10 pcs., in a carton box 1, 2, 3, 4 or 5 packs.

Characteristic

Flat-cylindrical tablets with a beveled color from white to white with a yellow or cream tint.

pharmachologic effect

Pharmacological action - antiemetic.

It blocks dopamine (D2) and serotonin receptors, inhibits the chemoreceptors of the brain stem trigger zone, weakens the sensitivity of the visceral nerves that transmit impulses from the pylorus and duodenum to the vomiting center. Through the hypothalamus and parasympathetic nervous system, it has a regulating and coordinating effect on the tone and motor activity of the upper gastrointestinal tract (including the tone of the lower digestive sphincter at rest).

Pharmacodynamics

Increases the tone of the stomach and intestines, accelerates gastric emptying, reduces hyperacid stasis, prevents pyloric and esophageal reflux, stimulates intestinal motility. Normalizes the separation of bile, reduces spasm of the sphincter of Oddi without changing its tone, eliminates dyskinesia of the gallbladder. Stimulates the secretion of prolactin. Increases the sensitivity of tissues to acetylcholine (the action does not depend on vagal innervation, but is eliminated by anticholinergics). By stimulating the secretion of aldosterone, it enhances Na retention and K excretion. It does not have m-anticholinergic, antihistamine, antiserotonin and ganglioblocking effects; it does not affect the tone of the blood vessels of the brain, blood pressure, respiratory function, as well as the function of the kidneys and liver, hematopoiesis, secretion of the stomach and pancreas.

After oral administration, the effect is achieved after 20-40 minutes, manifested by an acceleration of the evacuation of the contents of the stomach (from about 0.5-6 hours) and an antiemetic effect (12 hours persist).

Pharmacokinetics

Rapidly and completely absorbed after oral administration. Due to partial destruction in the liver after absorption, bioavailability is 75%. Cmax is reached in 30-120 minutes. Plasma protein binding - 13-30%. The volume of distribution is 3.5 l / kg. It is metabolized in the liver. T1 / 2 - 4-6 hours, with chronic renal failure - 14 hours. Excreted by the kidneys within 24-72 hours (85%), unchanged - 30%. Easily passes through the BBB and the placental barrier, excreted in breast milk.

Indications for Metoclopramide

Treatment: vomiting and nausea (narcosis, radiation therapy, liver and kidney diseases, traumatic brain injury, migraine), Gilles de la Tourette syndrome (generalized tics and vocalisms in children), correction of side effects of drugs (digitis, cytostatics, antibiotics, morphine ), vomiting in pregnant women, hiccups of various origins, atony and hypotension of the stomach and duodenum (including postoperative, against diabetic neuropathy), reflux esophagitis, biliary dyskinesia, flatulence.

As part of complex therapy: chronic gastritis, peptic ulcer of the stomach and duodenum, cholelithiasis.

Acceleration of peristalsis during radiopaque studies of the gastrointestinal tract.

Contraindications

Hypersensitivity, bleeding in the gastrointestinal tract, intestinal obstruction, perforation of the gastrointestinal tract (including conditions when increased motor activity of the gastrointestinal tract is undesirable), pheochromocytoma (a hypertensive crisis is possible due to the release of catecholamines from the tumor), prolactin-dependent tumors, epilepsy, glaucoma, extrapyramidal disorders, Parkinson's disease, vomiting during treatment or overdose with antipsychotics, vomiting in patients with breast cancer, pregnancy (I trimester), breastfeeding, age up to 2 years.

Use during pregnancy and lactation

Contraindicated in the first trimester of pregnancy. At the time of treatment should stop breastfeeding.

Side effects

The drug is usually well tolerated. In rare cases, disorders are possible:

from the nervous system and sensory organs: extrapyramidal disorders (convulsive twitching of the facial muscles, trismus, muscle hypertonicity) - parkinsonism (hyperkinesis, muscle rigidity - 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 chronic liver failure), drowsiness, fatigue, anxiety, confusion, headache, tinnitus;

on the part of the digestive tract: constipation / diarrhea, dry mouth;

allergic reactions: urticaria

others: with prolonged use in high doses - gynecomastia, galactorrhea, menstrual disorders - asymptomatic mild hyperemia of the nasal mucosa, at the beginning of treatment - agranulocytosis.

Most side effects disappear 24 hours after withdrawal.

Interaction

Enhances the effect of ethanol on the central nervous system, the sedative effect of hypnotics, the effectiveness of therapy with H2-histamine blockers. Increases the absorption of acetylsalicylic acid, paracetamol, diazepam, levodopa, tetracycline, ampicillin (due to faster evacuation of the contents of the stomach), slows down - digoxin and cimetidine (acceleration of intestinal motility). When combined with neuroleptics (especially the phenothiazine series and butyrophenone derivatives), there is a risk of developing symptoms of extrapyramidal disorders.

Dosage and administration

Inside, before meals, without chewing, with a small amount of water, adults: 5-10 mg 3-4 times a day. The maximum single dose is 20 mg, the daily dose is 60 mg. Children over 6 years: 2.5-5 mg 1-3 times a day.

Before x-ray examination: inside, 5-15 minutes before the start of the study - 15-30 mg. With clinically pronounced hepatic and renal insufficiency, the initial dose is reduced by 2 times.

Precautionary measures

Prescribed with caution in renal failure, bronchial asthma, arterial hypertension, children (up to 14 years of age - parenteral administration).

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

It should not be used during work by drivers of vehicles and people whose profession is associated with increased concentration of attention.

During the period of treatment, you can not drink alcohol (risk of possible complications).

special instructions

Ineffective in vomiting of vestibular origin.

Do not prescribe after operations on the gastrointestinal tract (pyloroplasty or intestinal anastomosis), since muscle contractions prevent the healing of sutures.

Storage conditions of the drug Metoclopramide

In a place protected from light, in a tightly closed package, at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life of Metoclopramide

2 years.

Last update of the description by the manufacturer

31.07.2003

Other options for packaging the drug - Metoclopramide.

Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule, contour plastic packaging (pallets) 5, carton pack 1 - EAN code: 5903060000841 - No. P N013299 / 02, 2008-11-21 from Polpharma (Poland) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule with an ampoule knife, contour plastic packaging (pallets) 5, cardboard pack 1- No. P N002571 / 01, 2009-07-13 from Moscow Endocrine Plant (Russia) Metoclopramide Solution for intravenous and intramuscular administration 5 mg / ml - 2 ml ampoule with an ampoule knife, blister pack 5, cardboard box (box) 100 - No. P N002571 / 01, 2009-07-13 from Moscow Endocrine Plant (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule, cardboard pack 10 - EAN code: 4602212003532 - No. P N002157 / 01, 2007-11-26 from Novosibkhimfarm (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - ampoule 2 ml, packing contour cells kovy 10, cardboard pack 1- code EAN: 4602212003549- № R N002157/01, 2007-11-26 from Novosibkhimfarm (Russia) 5, cardboard pack 1- No. P N002571/01, 2009-07-13 from Moscow Endocrine Plant (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg/ml - 2 ml ampoule with ampoule knife, blister pack 5, carton pack 2- EAN code: 4602676006063- No. P N002571/01, 2009-07-13 from Moscow Endocrine Plant (Russia) Metoclopramide Solution for intravenous and intramuscular administration 5 mg/ml- 2 ml ampoule with ampoule knife, contour plastic packaging (pallets) 5, cardboard pack 1- code EAN: 4602509010007- No. LS-001657, 2011-11-30 from Biochemist (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule with ampoule knife, contour plastic packaging (pallets ) 5, cardboard pack 2- EAN code: 460 2509010021- No. LS-001657, 2011-11-30 from Biochemist (Russia) Metoclopramide Solution for intravenous and intramuscular administration 5 mg / ml - 2 ml ampoule with ampoule knife, cardboard box (box) 10 - EAN code: 4602509010045- No. LS -001657, 2011-11-30 from Biochemist (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule with ampoule knife, cardboard pack 5 - EAN code: 4602509010069 - No. LS-001657, 2011-11- 30 from Biochemist (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule with ampoule knife, cardboard pack 10 - EAN code: 4602509010083- No. LS-001657, 2011-11-30 from Biochemist (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule, blister pack 10, cardboard pack 2 - No. P N002157 / 01, 2007-11-26 from Novosibkhimfarm (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule, blister pack 5, cardboard pack 1 - No. P N002157 / 01, 2007-11-26 from Novosibkhimfarm (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule, blister pack 5, cardboard pack 2- No. P N002157 / 01, 2007-11-26 from Novosibkhimfarm (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule with an ampoule knife, blister pack 5, cardboard box (box) 50 - No. P N002571 / 01, 2009-07-13 from the Moscow Endocrine Plant ( Russia) Metoclopramide Solution for intravenous and intramuscular administration 5 mg / ml - 2 ml ampoule with ampoule knife, blister pack 5, cardboard box (box) 20- No. P N002571 / 01, 2009-07-13 from Moscow Endocrine Plant (Russia ) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule, blister pack 5, cardboard pack 1- No. LS-000393, 2010-05-04 from Sotex PharmFirma (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg/ml - 2 ml ampoule, pack vka contour cell 5, cardboard pack 2- code EAN: 4605964001153- No. LS-000393, 2010-05-04 from Sotex PharmFirma (Russia) pallets) 5, cardboard pack 1- No. LS-000393, 2010-05-04 from Sotex PharmFirma (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule, contour plastic packaging (pallets) 5, cardboard pack 2- No. LS-000393, 2010-05-04 from Sotex PharmFirma (Russia) Metoclopramide Solution for intravenous and intramuscular injection 5 mg / ml - 2 ml ampoule with ampoule knife, contour plastic packaging (pallets) 5, carton pack 2- code EAN: 4602676003369- No. R N002571/01, 2009-07-13 from Moscow Endocrine Plant (Russia) Metoclopramide Solution for intravenous and intramuscular administration 5 mg/ml - 2 ml ampoule with ampoule knife, blister pack 10, carton pack 2- No. Р N002571/01, 2009-07-13 dated

metoclopramide represents antiemetic drug, which suppresses hiccups , nausea and vomiting . Metoclopramide is able to influence dopamine and serotonin receptors located in the vomiting center and thereby suppress the gag reflex. This medication is effective for vomiting of various origins - with the side effects of various drugs, against the background of a violation of the diet, after traumatic brain injuries and in violation of the normal functioning of the kidneys and liver. It should also be noted that sometimes metoclopramide is used to treat migraine ( improves the absorption of anti-migraine drugs when taken orally).

Metoclopramide is a white crystalline substance that is almost insoluble in water and odorless. This drug is rapidly absorbed from the gastrointestinal tract after oral administration.

Types of medication, commercial names of analogues, release forms

Metoclopramide is available as a tablet or as a solution for intramuscular or intravenous injection.

Metoclopramide can be bought in pharmacies and under other names - Metamol, Ceruglan, Cerucal, Apo-Metoclops, Perinorm, Raglan.

Manufacturers of metoclopramide

Manufacturing firm	Commercial name of the drug	Country	Release form	Dosage
*NIOPIK SSC*	*metoclopramide*	Russia	Tablets	Tablets should be taken immediately before meals. *Adults* one-time prescribe to take 5 - 10 mg. The medication should be taken up to 3 times a day. It is not recommended to take more than 20 milligrams at a time, and more than 60 milligrams of the drug per day. *For children over six years old* a single dose is 5 mg. *Children under six years of age* appoint 0.5 - 1 milligram ( no more than 3 times a day).
*Borisov plant of medical preparations*	*metoclopramide*	Republic of Belarus
*Update*	*metoclopramide*	Russia
*North Star*	*metoclopramide*	Russia
*Chemical-Pharmaceutical Plant AKRIKHIN*	*Metoclopramide-ACRI*	Russia
*PharmFirma Sotex*	*metoclopramide*	Russia	Solution for the preparation of intramuscular or intravenous injections.	Injections are prescribed, as a rule, with severe nausea and vomiting. *Single dosage for adults* is 10 milligrams, which should be administered three times a day. *Children aged 6 and over* enter 5 milligrams. *Children under six years of age* appoint 0.5 - 1 milligram. The frequency of administration is 1 - 3 times a day.
*Armavir Biofactory*	*metoclopramide*	Russia
*Novosibkhimfarm*	*metoclopramide*	Russia
*Moscow Endocrine Plant*	*metoclopramide*	Russia
*Eskom*	*Metoclopramide-ESCOM*

The mechanism of the therapeutic action of the drug

Metoclopramide has antiemetic, anti-hiccup and prokinetic effects ( stimulates gastrointestinal motility). Metoclopramide is a blocker of central and peripheral dopamine D-2 receptors, which can have a significant effect on the center of vomiting. Metoclopramide normalizes and also enhances the motor activity of the esophagus, stomach and duodenum. The action of metoclopramide is aimed at increasing the tone and amplitude of contractions of the stomach, relaxing the pyloric sphincter ( circular muscle that separates the stomach from the duodenum), increased gastric emptying and relaxation of the duodenum. At the same time, there is a normalization of muscle contractions of the gallbladder, due to which the outflow of bile is normalized ( eliminates biliary dyskinesia). It is also worth noting that large doses of this antiemetic drug directly affect serotonin receptors, which also has an antiemetic effect ( suppressed gag reflex).

Metoclopramide is prescribed as an antiemetic in the following cases:

side effects of certain medications that can cause vomiting ( cytostatics, some antibiotics, morphine, and anti-tuberculosis drugs);
diet violation;
vomiting during pregnancy;
radiotherapy in the treatment of malignant tumors;
vomiting in traumatic brain injury;
vomiting in kidney and liver diseases;
uremia ( accumulation of urea in the blood against the background of chronic renal failure).

It should be noted that metoclopramide is not effective in the event of nausea and vomiting in violation of the function of the vestibular apparatus.

Metoclopramide can also be used in the treatment of migraine ( is part of complex therapy). Also, metoclopramide prevents stagnation of food in the stomach and thereby stimulates the absorption of anti-migraine drugs.

Metoclopramide is well absorbed through the mucosa of the digestive system and relatively quickly penetrates into the circulatory system. Metoclopramide passes quite easily through the placental barrier, the blood-brain barrier ( can enter nerve cells) and may pass into breast milk. The onset of action of metoclopramide with intravenous use is observed within a few minutes, after intramuscular injections - after 5-20 minutes, and when taking tablets - after 40-60 minutes. The duration of action of metoclopramide is usually 1 to 3 hours. It should be noted that metoclopramide is metabolized by the liver and excreted by the kidneys. If the function of the kidney tissue is impaired, there is a significant delay in the excretion of this medication from the body.

While taking metoclopramide, you should refrain from drinking alcohol because of the possibility of various side effects and complications. Also, under the influence of this medication, concentration of attention may decrease, which may affect work that requires quick reaction ( driving a car, as well as working with potentially dangerous production equipment).

For what pathologies is it prescribed?

Metoclopramide is able to effectively stop nausea and vomiting of various origins. It can also be prescribed in the treatment of migraine to improve the absorption of anti-migraine medications.

The use of metoclopramide

Indication for use	Mechanism of action	Dosage
*hiccup*	It blocks central as well as peripheral dopamine D-2 receptors and serotonin receptors, which stimulate the vomiting center. Normalizes the activity of the upper gastrointestinal tract. Increases the amplitude of contractions of the muscular layer of the end section of the stomach ( antrum). Improves the passage of food from the stomach to the intestines ( relaxes the sphincter that separates the stomach from the duodenum).	Can be used internally tablets), or intramuscularly or intravenously ( injections). Tablets are taken a few minutes before meals, 5 to 10 milligrams three times a day. No more than 20 mg should be taken at a time, and no more than 60 mg per day. *IV for adults* administered 10 mg up to three times a day. *For children six years of age and older* one-time it is necessary to take 5 milligrams. *Children under six years of age* , appoint 0.5 - 1 milligram. Use the drug in childhood should be from one to three times a day.
*Nausea*
*Vomit*
*indigestion*
*Gastroesophageal reflux* (reflux of food from the stomach into the esophagus)
*Atony and hypotension of the stomach and duodenum* (food retention in the stomach and duodenum, due to a decrease in muscle tone)
*Flatulence* (bloating due to accumulation of gases in the intestines)
*Period of exacerbation of gastric and duodenal ulcers* (metoclopramide is part of complex therapy)
*Biliary dyskinesia* (impaired motility of the bile ducts and gallbladder)	It normalizes the muscle contractions of the gallbladder, due to which the normal outflow of bile is restored. Eliminates biliary dyskinesia.
*As a preparation for diagnostic methods of examination of the gastrointestinal tract*	The same as in biliary dyskinesia.	Intravenously in the amount of 10 - 20 milligrams. The drug is administered 10-15 minutes before the start of the diagnostic procedure of the digestive tract.
*As a complex therapy in the treatment of migraine*	Promotes better absorption of anti-migraine drugs in the wall of the mucous membrane of the upper floors of the digestive tract.	The dosage is selected by the doctor.

How to apply the medication?

Metoclopramide can be administered both in the form of intramuscular and intravenous injections, and in the form of conventional tablets.

Metoclopramide tablets are taken immediately a few minutes before meals.

One-time adults should take 5-10 mg three times a day. The maximum single dose is 20 mg, and the maximum daily dose should not exceed 60 mg.

Children under six are prescribed metoclopramide in a single dose of 0.5-1 milligrams, and children over six years old are prescribed 5 milligrams ( apply 1-3 times a day). The course of therapy is selected individually.

To achieve a quick effect, this antiemetic is prescribed in the form of intravenous or intramuscular injections.

For adults, a single dosage is 10 mg. Injections should be done one to three times a day.

Children who are already six years old are injected with 5 milligrams of the drug, and children under six years old are given 0.5-1 milligrams 1 to 3 times a day.

The initial dosage should be halved for persons with impaired liver function.

Possible side effects

Sometimes taking metoclopramide causes serious disorders in various tissues and organs. As a rule, side effects occur with long-term oral use of this antiemetic medication.

The following adverse reactions may occur while taking metoclopramide:

disorders of the digestive system;
disorders of the nervous system;
violations of the hematopoietic system;
drug allergy;
violations of the organs of the endocrine system.

Digestive disorders

Adverse reactions from the digestive system occur most often against the background of long-term use of metoclopramide. Taking this antiemetic medication with other drugs that have hepatotoxicity ( negatively affect liver tissue) can interfere with the normal functioning of the liver. It should also be noted that metoclopramide can affect the frequency of bowel movements and lead to constipation or diarrhea.

There are the following disorders of the digestive system:

xerostomia;

Xerostomia manifested by a feeling of dryness in the mouth. Xerostomia is a direct consequence of decreased saliva production by the sublingual, parotid, submandibular, and small salivary glands ( hyposalivation). Against the background of prolonged xerostomia, other diseases of the oral cavity can often occur, since saliva contains a special antibacterial substance lysozyme, which inhibits the growth and reproduction of bacteria.

Jaundice is a pathological condition, which is characterized by staining of the skin and mucous membranes in a yellow tint. Jaundice occurs due to a malfunction of the liver, as a result of which the level of bilirubin in the blood, as well as in the tissues, increases significantly ( bile pigment). It is bilirubin that stains the skin and mucous membranes yellow. Jaundice can occur, as a rule, while taking another drug that is toxic to the liver tissue ( hepatotoxic effect).

Nervous System Disorders

Even a single dose of metoclopramide can lead to serious side effects from the nervous system. These reactions are observed most often in children and adolescents, as well as in the elderly. Violations of the nervous system occur due to the direct action of the drug on the nerve cells of the brain.

Metoclopramide can lead to the following disorders:

fatigue;
dizziness;
drowsiness;
akathisia;
spasm of the facial muscles;
hyperkinesis;
spastic torticollis;
parkinsonism;
dyskinesia.

Akathisia is a syndrome characterized by a recurring feeling of motor restlessness. With akathisia, people change their position very often, are unable to sit quietly in the same position for a long time or remain without any movement. This syndrome occurs due to blocking of dopamine receptors located in the central nervous system. Quite often, akathisia can occur along with a depressive state.

Spasm of the facial muscles(facial hemispasm) is manifested by unilateral and involuntary contractions of the facial muscles as a result of disruption of the facial nerve. Most often, facial hemispasm begins with single contractions of the circular muscle of the eye. In the future, the contractions progress and affect almost the entire half of the face. These clonic or tonic contractions ( in the form of involuntary twitches or significant muscle contractions) can significantly interfere with seeing with the eye on the affected side. Also, a spasm of the facial muscles can begin with contractions of the muscles of the cheek, and then spread upward.

Hyperkinesis are pathological contractions of different muscle groups that occur involuntarily. Hyperkinesis occurs as a result of damage to nerve cells of various brain structures ( thalamus, subthalamic nuclei, extrapyramidal system, etc.). Intensity and frequency can be reduced by volitional influence, change in posture or painful stimuli. It should be noted that in a dream these involuntary contractions completely disappear.

Spasmodic torticollis is a disease in which, due to tension in the muscles of the neck, the normal position of the head is disturbed. Painful sensations are less pronounced in the first half of the day and gradually increase in the evening. Often a stressful situation or physical activity exacerbates the pain. It should be noted that spastic torticollis is extremely difficult to treat.

parkinsonism is a neurological syndrome characterized by symptoms such as tremor ( rhythmic and rapid contractions of the muscles of the trunk or limbs), increased muscle tone ( muscle stiffness), slow pace of movements ( bradykinesia), difficulty in maintaining balance when walking ( postural instability), as well as muscle resistance during passive movements. Drug-induced parkinsonism is especially common in the elderly.

Dyskinesia, or tardive dyskinesia, are manifested by involuntary movements of the limbs that occur against the background of long-term use of medications that can block dopamine receptors. Dyskinesias can manifest as tremors, tics ( involuntary elementary and stereotypical movements), akathisia or other manifestations, which are often combined. A feature of dyskinesia is the persistence of this symptomatology after discontinuation of the drug ( several months to several years).

Hematopoietic system disorders

In rare cases, the use of metoclopramide may be accompanied by the occurrence of agranulocytosis. With this pathology in the blood, there is a decrease in the number of subspecies of white blood cells ( neutrophils, eosinophils and basophils). Agranulocytosis can lead to fever, chills, headache, nausea, and muscle and bone pain. Decrease in the number of neutrophils ( one of the subtypes of granulocytes) in the blood leads to the fact that the human body becomes vulnerable to fungal and bacterial infections. The occurrence of agranulocytosis is associated with the occurrence of an autoimmune process. Having contacted blood cells, half-life products ( metabolites) metoclopramide is perceived as a foreign substance ( antigen). The body then produces antibodies to them. special protein molecules), and when the drug is re-entered, the immune system attacks any cell that is bound to the antigen. It should be noted that agranulocytosis most often occurs only in the first few days after the start of treatment.

drug allergy

In rare cases, taking metoclopramide can lead to a skin rash. As a rule, red spots or small bubbles appear on various parts of the body, which can cause an unpleasant burning sensation to varying degrees. Also, in some cases, urticaria may occur. This allergic reaction is characterized by the appearance of rather large blisters on the skin, which visually resemble blisters from a nettle burn. These blisters are slightly pinkish in color and slightly raised above the surface of the skin. A rash with urticaria can be either solitary and appear only in one part of the body, or have a generalized character, covering the trunk and limbs.

Endocrine system disorders

Long-term use of high doses of metoclopramide can adversely affect the endocrine system, causing serious disorders. This is due to the fact that penetrating into the brain, the drug can affect the work of the higher centers of the endocrine system ( hypothalamus and pituitary gland).

Metoclopramide in rare cases can lead to the following adverse reactions:

galactorrhea;
violation of the menstrual cycle;
gynecomastia.

Galactorrhea is a spontaneous secretion of milk from the mammary gland, which is not associated with feeding the child. Galactorrhea can occur not only in women, but also in men. This pathological condition occurs due to increased production of the hormone prolactin ( synthesized by the anterior pituitary gland), which promotes the formation of breast milk.

Menstrual irregularity characterized by some deviation from the normal menstrual cycle, which is characterized by the duration of menstruation from 3 to 7 days, and the interval between cycles is, on average, 21 to 30 days. As a rule, these disorders are manifested by the irregularity of the menstrual cycle, heavy menstruation with blood clots ( menorrhagia) or, conversely, very scanty and spotting vaginal discharge that lasts less than 3 days ( oligomenorrhea). Also, menstrual disorders are often accompanied by moderate or severe pain in the lower abdomen ( algomenorrhea).

Gynecomastia is a pathological condition in men in which there is an increase in the mammary glands due to the growth of adipose tissue and the tissue of the glands themselves ( hypertrophy). Gynecomastia occurs when there is a decrease in the production of male sex hormones ( testosterone) or with an increase in the synthesis of female ( estrogen). With this pathology, the appearance of a feeling of heaviness in the chest, fullness and itching is characteristic. When probing the mammary gland, a relatively mobile formation with clear boundaries can be detected.

Approximate cost of medication

This antiemetic can be found in most pharmacies in Russia. It should be noted that depending on the form of release, the price of metoclopramide is somewhat different.

Average cost of metoclopramide

City	The average cost of a medicinal substance
City	Tablets	Solution for intramuscular or intravenous administration
*Moscow*	18 rubles	54 rubles
*Kazan*	17 rubles	53 rubles
*Krasnoyarsk*	17 rubles	52 rubles
*Samara*	16 rubles	52 rubles
*Tyumen*	19 rubles	57 rubles
*Chelyabinsk*	21 rubles	58 rubles

In this medical article, you can get acquainted with the drug Metoclopramide. The instructions for use will explain in which cases you can take injections or tablets, what the medicine helps with, what are the indications for use, contraindications and side effects. The annotation presents the form of release of the drug and its composition.

In the article, doctors and consumers can only leave real reviews about Metoclopramide, from which you can find out if the medicine helped in the treatment of nausea, vomiting and flatulence in adults and children, for which it is also prescribed. The instructions list analogues of metoclopramide, drug prices in pharmacies, as well as its use during pregnancy.

The antiemetic drug is metoclopramide. Instructions for use reports that 10 mg tablets, injections in ampoules for injection in solution stimulate the peristalsis of the digestive tract.

Release form and composition

Metoclopramide is available in the following dosage forms:

Tablets: flat-cylindrical, round, chamfered, almost white or white, marbling is allowed (50 pcs in blister packs, 1 pack in a carton box; 10 pcs in blister packs or blisters, 1-5, 10 packs or blisters in a carton pack, 14 pcs in blister packs, 4 packs in a carton pack, 50 pcs in plastic or dark glass jars, 1 jar in a carton pack).
Solution for intravenous and intramuscular administration (in ampoules of 2 ml, 5 or 10 ampoules in a carton pack or 5 or 10 ampoules in plastic or cell contour packs (pallets), 1 or 2 packs in a carton pack).

The composition of 1 tablet Metoclopramide includes - active substance: metoclopramide hydrochloride - 10 mg (in the form of metoclopramide hydrochloride monohydrate in terms of dry matter).

The composition of 1 ml of the injection solution Metoclopramide includes the active substance: metoclopramide hydrochloride - 5 mg.

pharmachologic effect

Metoclopramide has an antiemetic effect, has a stimulating effect on the peristalsis of the digestive tract, reduces the severity of hiccups and nausea. The mechanism of action is based on blocking dopamine D2 receptors, on increasing the threshold of chemoreceptors located in the trigger area, on blocking serotonin receptors.

There is an assumption that the active substance is able to inhibit the relaxation of the smooth muscle tissue of the stomach, which is caused by Dopamine.

The drug accelerates the emptying of the stomach by relaxing its body, increasing the activity of the upper sections of the small intestine and the antrum of the stomach. By increasing the pressure of the esophageal sphincter at rest, it reduces the reflux of contents into the lumen of the esophagus.

Increasing the amplitude of peristaltic contractions increases acid clearance. It is noticed that the active ingredient stimulates the production of prolactin, increases the level of aldosterone, which can lead to fluid retention in the body (the effect is reversible).

Indications for use

What does metoclopramide help with? Tablets are indicated for various pathological conditions, which are accompanied by the development of nausea and the appearance of vomiting, these include:

Complex therapy of peptic ulcer of the stomach or duodenum.
Reflux esophagitis is an inflammation of the esophageal mucosa, which is the result of the backflow of acidic gastric contents into it.
Vomiting, nausea or hiccups of various origins, including those associated with disorders in the structures of the central nervous system.
Atony or hypotension of the hollow structures of the digestive tract (stomach, small intestine) - a pronounced decrease in the tone of smooth muscles after surgery, taking or using certain drugs.
Biliary dyskinesia is a violation of the tone of the hollow structures of the hepatobiliary system (gall bladder, hepatic and bile ducts), which is accompanied by severe nausea and vomiting.
Flatulence - increased gas formation in the intestine, provoked by a decrease in its peristaltic movements.

Metoclopramide tablets are also used to enhance intestinal motility, which is necessary for certain diagnostic studies (X-ray examination using contrast agents).

Instructions for use

metoclopramide tablets

Take 30 minutes before meals with a small amount of water. Adults - 5-10 mg 3-4 times a day. The maximum single dose is 20 mg, the daily dose is 60 mg. Children over 6 years old - 5 mg 1-3 times a day.

Ampoules

Intravenously or intramuscularly. Adults at a dose of 10-20 mg 1-3 times a day (maximum daily dose - 60 mg). Children over 6 years old: 5 mg 1-3 times a day.

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 of body weight 30 minutes before the use of cytostatics or radiation; if necessary, the introduction is repeated after 2-3 hours.

Before an x-ray examination, adults are administered intravenously 10-20 mg 5-15 minutes before the start of the study.

Patients with clinically pronounced hepatic and / or renal insufficiency are prescribed a dose that is half the usual dose, the subsequent dose depends on the patient's individual response to the drug.

Contraindications

diagnosed glaucoma, suspicion of it;
bleeding in the digestive system;
individual hypersensitivity;
stenosis of the pylorus of the stomach;
Parkinson's disease;
perforation of the walls of the intestine, stomach;
prolactin-dependent neoplasms;
pheochromocytoma;
bronchial asthma in patients with hypersensitivity to sulfites;
epilepsy;
vomiting during treatment with antipsychotics in patients suffering from breast cancer;
extrapyramidal disorders;
mechanical intestinal obstruction.

The drug is not used in the postoperative period in patients with pyloroplasty and intestinal anastomosis, because. vigorous muscle contractions impair healing.

Relative contraindications:

old age (65 years and older);
bronchial asthma;
hypertonic disease;
Parkinson's disease;
diseases of the renal and hepatic system;
children's age (possible development of dyskinetic syndrome);

Side effects

Central nervous system: extrapyramidal disorders - trismus, facial muscle spasm, spastic torticollis, bulbar type of speech, rhythmic protrusion of the tongue, extraocular muscle spasm (including oculogiric crisis), muscle opisthotonus, hypertonicity.
Parkinsonism (muscle rigidity, hyperkinesis - a manifestation of dopamine-blocking action, the risk of development in children increases when the dose of 0.5 mg / kg per day is exceeded), dyskinesia (in chronic renal failure and in elderly patients), depression, headache, drowsiness, anxiety, fatigue, confusion, tinnitus.
Metabolism: porphyria.
Endocrine system: rarely (with prolonged therapy at high doses) - galactorrhea, gynecomastia, menstrual irregularities; Digestive system: diarrhea, constipation; rarely - dry mouth.
Allergic reactions: angioedema, bronchospasm, urticaria.
Hematopoietic system: leukopenia, neutropenia, sulfhemoglobinemia in adults.
Cardiovascular system: atrioventricular blockade.
Others: at the beginning of treatment - agranulocytosis; rarely (when using high doses) - hyperemia of the nasal mucosa. If the symptoms described above appear, they worsen, or other side effects develop, you should consult a doctor.

Children, during pregnancy and lactation

Metoclopramide is contraindicated for use in the 1st trimester of pregnancy. Application in the 2nd and 3rd trimesters of pregnancy is possible only for health reasons. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.

Use in children

Contraindicated in early childhood (children under 2 years of age - the use of metoclopramide in the form of any dosage forms is contraindicated, children under 6 years of age - parenteral administration is contraindicated). The use of the drug in children causes an increased risk of developing dyskinetic syndrome.

special instructions

With vomiting of vestibular origin, metoclopramide is not effective. When it is used, data on laboratory parameters of liver function and determination of the concentration of prolactin and aldosterone in plasma may be distorted. Side effects in most cases develop within 36 hours after the use of the drug and disappear without additional treatment within 24 hours after its withdrawal.

Therapy, if possible, should be short-term. It is not recommended to drink alcohol during the use of metoclopramide. During the period of treatment, care should be taken when working with potentially dangerous mechanisms that require increased concentration of attention and quick psychomotor reactions, as well as when driving.

drug interaction

Cholinesterase inhibitors weaken the effect of the drug. The risk of developing extrapyramidal disorders increases significantly with simultaneous therapy with antipsychotics.

Metoclopramide is able to increase the activity of histamine H2 receptor blockers, enhance the sedative effect of hypnotics, and aggravate the effect of ethanol on the nervous system. The drug enhances absorption:

Acetylsalicylic acid.
diazepam.
ethanol.
Levodopa.
Tetracycline (including tetracycline antibiotics).

Slows down the process of absorption of Cimetidine and Digoxin.

Analogues of the drug Metoclopramide

According to the structure, analogues are determined:

Apo Metoclops.
Tseruglan.
Cerucal.
Perinorm.
Metoclopramide Vial (Akri, Darnitsa, Promed, Escom).
Raglan.
Metamol.
Metoclopramide hydrochloride.

Antiemetics include analogues:

Perinorm.
Bonin.
Trifluoperazine Apo.
Etaperazine.
Avomit.
Ciel.
Granisetron.
Navoban.
Tseruglan.
Damelium.
Emetron.
Emeset.
Motijekt.
Onycite.
Lazaran.
Ondantor.
Passagex.
Ondansetron.
Metamol.
Vero Ondansetron.
Rondaset.
Setronon.
Kinedryl.
Aviaplant.
Domstal.
Bimaral.
Motinorm.
Aviomarin.
Notirol.
Zofran.
Motilium.
Cerucal.
Raglan.
Domperidone.
Validol.
Domegan.
Domet.
Sturgeon.
Motonium.
Emend.
Torekan.
Apo Metoclops.
Metoclopramide.
Triftazin.
Ondasol.
Tropindol.
Kytril.
Latran.

Holiday conditions and price

The average cost of Metoclopramide (tablets 10 mg No. 50) in Moscow is 29 rubles. The price of injections is 67 rubles for 10 ampoules. Released by prescription.

Store in a dark, dry place out of the reach of children at temperatures up to 25 C. Shelf life:

Tablets - 2 years.
Injection solution - 4 years.