ATX code: A03FA01
Trade name: Metoclopramide International generic name: Metoclopramide/Metoclo-pramide. Release form: solution for injection 5 mg/ml. Composition: one ampoule (2 ml of solution) contains - active substance: metoclopramide hydrochloride – 10 mg; excipients: sodium chloride, sodium sulfite anhydrous E 221, disodium edetate, propylene glycol, hydrochloric acid, water for injection. Description: transparent colorless liquid. Pharmacotherapeutic group: drugs for the treatment of functional disorders gastrointestinal tract; prokinetics.
For adults. For the prevention of postoperative nausea and vomiting.
For symptomatic treatment nausea and vomiting, including nausea and vomiting in acute migraine.
For the prevention of nausea and vomiting induced radiation therapy.
The injection course of treatment should be as short as possible. The patient should be transferred to the oral or rectal route of administration as soon as possible.
Children aged 1 to 18 years. For the prevention of delayed (non-acute) nausea and vomiting caused by chemotherapy, as a second-line drug. The maximum course of treatment is 5 days.
For the treatment of established postoperative nausea and vomiting, as a second-line drug. The maximum course of treatment is 48 hours.
Hypersensitivity to metoclopramide or components of the drug, gastrointestinal bleeding, pyloric stenosis, mechanical intestinal obstruction, perforation of the stomach or intestines, 3–4 days after surgery on the stomach and/or intestines, pheochromocytoma (confirmed or suspected due to the risk of severe hypertensive complications), Parkinson's disease, extrapyramidal disorders (including neuroleptic or metoclopramide-induced tardive dyskinesia history), epilepsy, prolactin-dependent tumors, episodes of methemoglobinemia in a history of taking metoclopramide or with NADP-cytochrome-b5 deficiency, concomitant use of levodopa or dopamine receptor stimulants, pregnancy, childhood up to 1 year, lactation period.
Due to the sodium sulfite content, metoclopramide solution should not be administered to patients bronchial asthma With hypersensitivity to sulfite.
Maximum duration of use medicine no more than 5 days!
The injection solution is administered intramuscularly or intravenously as a bolus over at least 3 minutes. Adults at a dose of 10 mg up to 3 times a day (maximum single dose– 10 mg, maximum daily dose– 30 mg or 0.5 mg/kg).
For children. The dose is calculated in accordance with the table or based on the calculation of 0.10 - 0.15 mg/kg body weight up to 3 times a day. The maximum daily dose is 0.5 mg/kg body weight.
| Age (in years) | Weight, kg) | Dose (mg) | Frequency |
| 1 - 3 | 10 - 14 | 1 | up to 3 times a day |
| 3 - 5 | 15 - 19 | 2 | up to 3 times a day |
| 5 - 9 | 20 - 29 | 2,5 | up to 3 times a day |
| 9 - 18 | 30 - 60 | 5 | up to 3 times a day |
| 15 - 18 | More than 60 | 10 | up to 3 times a day |
The maximum duration of therapy is 5 days. In case of repeated vomiting, the minimum interval between administrations of metoclopramide should not be less than 6 hours.
For decreased kidney function, the drug is prescribed:
- with creatinine clearance less than 15 ml/min - in doses reduced by 75%;
- with creatinine clearance from 15 to 60 ml/min - in doses reduced by 50%.
In severe liver failure, the dose of metoclopramide should be reduced by 50%.
In elderly patients, dosing is carried out taking into account changes in liver and kidney function, as indicated above.
Metoclopramide
International nonproprietary name
Metoclopramide
Dosage form
Solution for injection 0.5% 2 ml
Compound
2 ml of solution contain
active substance - metoclopramide hydrochloride 10 mg,
Excipients: sodium pyrosulfite, sodium chloride, water for injection.
Description
Transparent solution, odorless.
Pharmacotherapeutic group
Drugs for the treatment of functional gastrointestinal disorders.
Gastrointestinal motility stimulants. Metoclopramide.
ATX code A03FA01
Pharmacological properties
Pharmacokinetics
Suction
The action of metoclopramide hydrochloride begins within 1-3 minutes after intravenous administration, and then intramuscular injection after 10-15 minutes.
The pharmacological effect lasts for 1-2 hours after administration.
Distribution
Metoclopramide hydrochloride is slightly bound to plasma proteins (13 - 30%), mainly to albumin.
The volume of distribution is 3.5 l/kg, indicating a wide distribution medicinal product in tissues.
Metoclopramide hydrochloride crosses the placental barrier and is excreted in breast milk. Drug concentration in breast milk 2 hours after administration is higher than in plasma.
Metoclopramide hydrochloride penetrates the blood-brain barrier.
Metabolism
Metoclopramide hydrochloride is biotransformed only to a small extent. Binds to sulfuric and glucuronic acid.
Elimination
The half-life (T1/2) of metoclopramide hydrochloride in adults with normal renal function is 5 to 6 hours and is longer in patients with impaired renal function.
About 85% of an oral dose of the drug is excreted in the urine, mostly unchanged or bound to sulfuric and glucuronic acid, within 72 hours. The remaining amount is excreted in feces.
Renal dysfunction
The clearance of metoclopramide is reduced by 70% in patients with severe renal impairment, while the plasma half-life is prolonged (approximately 10 hours for creatinine clearance 10-50 ml/min and 15 hours for creatinine clearance<10 мл/мин).
Liver dysfunction
In patients with cirrhosis, metoclopramide accumulation was observed, associated with a 50% decrease in plasma clearance.
Pharmacodynamics
Metoclopramide is a dopamine receptor antagonist. It also exhibits an antagonistic effect on 5-HT3 receptors and a weak stimulating effect on the ganglia. Blocks presynaptic dopamine receptors and promotes the release of acetylcholine from cholinergic motor neurons in the intestinal wall. Due to this, metoclopramide increases the release of acetylcholine from neurons, which induces spasm by stimulating muscarinic M2 receptors in the smooth muscle cells of the digestive tract. By increasing physiological conductance in cholinergic neurons, metoclopramide inhibits dopamine-induced relaxation of gastric smooth muscle, thereby enhancing cholinergic responses of gastrointestinal smooth muscle. The drug also stimulates the motility of the upper gastrointestinal tract (including increasing the static tone of the lower esophageal sphincter). In addition, gastroduodenal coordination between pyloric function and proximal duodenal motility is improved. Almost no effect on the motility of the colon and gall bladder. Does not affect the secretion of gastric juice, bile and pancreatic enzymes.
Metoclopramide penetrates the blood-brain barrier, producing effects on the central nervous system (CNS) that are typical of a dopamine receptor blocker. Has a sedative and antiemetic effect, eliminates nausea.
Indications for use
Use in adults:
Prevention of postoperative nausea and vomiting
Symptomatic treatment of nausea and vomiting, including nausea and vomiting in acute migraine
Prevention of nausea and vomiting induced by radiation therapy
Prevention of delayed chemotherapy-induced nausea and vomiting
Use in children:
Prevention of delayed chemotherapy-induced nausea and vomiting as a second-line treatment option
Treatment of postoperative nausea and vomiting as a second-line treatment option
Directions for use and doses
Metoclopramide is administered intramuscularly (IM) or intravenously (IV).
IV injections should be administered as a slow bolus (at least 3 minutes).
Dosage regimen for adults:
To eliminate postoperative nausea and vomiting, the recommended single dose is 10 mg. For the symptomatic treatment of nausea and vomiting, including nausea and vomiting in acute migraine, as well as for the prevention of nausea and vomiting induced by radiation therapy and the prevention of delayed nausea and vomiting induced by chemotherapy: The recommended single dose is 10 mg up to three times daily.
Dosage regimen for children and adolescents (1-18 years):
When prescribing the drug, a minimum six-hour interval between administration of the drug must be observed.
The maximum recommended treatment duration is 48 hours for the treatment of postoperative nausea and vomiting. The maximum recommended treatment duration is 5 days for the management of delayed chemotherapy-induced nausea and vomiting. In some cases, the duration of treatment is determined by the doctor, assessing the potential benefits and risks for the child. For children aged 1-14 years, metoclopramide is prescribed only in case of a confirmed diagnosis.
Elderly
Dose reduction should be considered in elderly patients based on renal and liver function and general condition.
Kidney failure
In patients with end-stage renal failure (creatinine clearance ≤ 15 ml/min), the daily dose should be reduced by 75%.
In patients with moderate to severe renal failure (creatinine clearance 15-60 ml/min), the daily dose should be reduced by 50%.
Liver failure
In patients with severe liver failure, the daily dose should be reduced by 50%
Side effects
Often (≥ 1/100,< 1/10)
Asthenia
Extrapyramidal disorders (especially in children and young people and/or when the recommended dose is exceeded, even after one dose of the drug), parkinsonism, akathisia
Depression
Hypotension, especially with intravenous administration
Not often (≥ 1/1000,< 1/100)
Bradycardia (especially with intravenous administration)
Amenorrhea, hyperprolactinemia
Hypersensitivity
Dystonia, dyskinesia, depression of consciousness
Hallucinations
Rarely (≥ 1/10,000,< 1/1000)
Insomnia, headaches, dizziness, visual disturbances, confusion
Swelling of the tongue or larynx
Galactorrhea
Seizures, especially in patients with epilepsy
Very rarely (< 1/10 000)
Neutropenia, leukopenia, agranulocytosis without a definite connection with the use of Metoclopramide
Bronchospasm, especially in patients with a history of asthma
Rash, hives
Unknown
Methemoglobinemia
Cardiac arrest occurring shortly after injection, atrioventricular block, QT prolongation
Gynecomastia, impotence
Porphyria
Inflammation and local phlebitis at the injection site
Anaphylactic reactions (including anaphylactic shock), especially with intravenous administration
Tardive dyskinesia, which may be permanent, during or after long-term treatment, especially in elderly patients, neuroleptic malignant syndrome
Shock, fainting after injections, acute arterial hypertension in patients with pheochromocytoma
Urinary incontinence, frequent urination
* Endocrine disorders during long-term treatment associated with hyperprolactinemia (amenorrhea, galactorrhea, gynecomastia).
The following reactions, sometimes associated, occur more often when using the drug in large doses:
Extrapyramidal symptoms: acute dystonia and dyskinesia, parkinsonian syndrome, akathisia, even after a single dose of the drug, especially in children and young adults
Drowsiness, depression of consciousness, confusion, hallucinations.
Contraindications
Hypersensitivity to any component of the drug
Bleeding from the gastrointestinal tract
Pyloric stenosis
Mechanical intestinal obstruction
Perforation of the stomach or intestines
Confirmed or suspected pheochromocytoma due to risk of severe episodes of hypertension
Epilepsy (increased frequency and intensity of seizures)
Parkinson's disease
Concomitant use of anticholinergic drugs, levodopa and dopaminergic agonists.
History of tardive dyskinesia induced by antipsychotics or metoclopramide
A history of methemoglobinemia when combined with metoclopramide or NADH-cytochrome b5 reductase deficiency.
Prolactinoma or prolactin-dependent tumor
Children's age up to 1 year
III trimester of pregnancy and lactation period
Drug interactions
The combination is contraindicated
Levodopa or dopaminergic agonists and Metoclopramide are antagonists.
Combination to avoid
Alcohol enhances the sedative effect of Metoclopramide.
Combination to be taken into account
Metoclopramide increases the absorption of diazepam, tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol; slows down the absorption of digoxin and cimetidine.
Anticholinergic drugs and morphine derivatives
Anticholinergic drugs and morphine derivatives may have mutual antagonism with metoclopramide in their effect on gastrointestinal motility.
Depressants that inhibit the activity of the central nervous system (morphine derivatives, tranquilizers, sedative H1 histamine receptor blockers, sedative antidepressants, barbiturates, clonidine and the like)
Metoclopramide potentiates the sedative effect of sedatives affecting the central nervous system.
Neuroleptics
When metoclopramide is used simultaneously with antipsychotics, the risk of developing extrapyramidal disorders increases.
Serotonergic drugs
Using metoclopramide with serotonergic drugs such as SSRIs may increase the risk of developing serotonin syndrome.
Digoxin
Metoclopramide may reduce the bioavailability of digoxin. Careful monitoring of plasma digoxin concentrations is required.
Cyclosporine
Metoclopramide increases the bioavailability of cyclosporine (Cmax by 46% and effect by 22%). Careful monitoring of cyclosporine plasma concentrations is required.
Mivacurium and suxamethonium
Metoclopramide injections may prolong the duration of neuromuscular blockade (by inhibiting plasma cholinesterase).
Strong inhibitorsCYP2 D6
Metoclopramide exposure is increased when coadministered with strong CYP2D6 inhibitors such as fluoxetine and paroxetine.
MAO inhibitors
In patients with hypertension treated with MAO inhibitors (monoamine oxidase inhibitors), metoclopramide potentiates the effect of MAO inhibitors.
special instructions
Neurological disorders
Extrapyramidal disorders may occur, especially in children and young people, and/or when using high doses of metoclopramide. These reactions usually occur at the beginning of treatment and may appear after a single dose. Metoclopramide should be discontinued immediately if symptoms of extrapyramidal disorders occur. These symptoms are usually completely reversible after cessation of treatment, but symptomatic treatment (benzodiazepines in children and/or antiparkinsonian anticholinergic drugs in adults) may be required.
Long-term treatment with metoclopramide may lead to tardive dyskinesia, which is potentially irreversible, especially in the elderly. Treatment should not exceed three months due to the risk of tardive dyskinesia. Treatment should be discontinued if clinical signs of tardive dyskinesia appear.
Neuroleptic malignant syndrome may occur when taking metoclopramide in combination with antipsychotics, as well as when taking metoclopramide alone. The drug should be stopped immediately if symptoms of neuroleptic malignant syndrome occur and appropriate treatment should be initiated.
When prescribing the drug, special attention should be paid to patients with concomitant neurological diseases and patients receiving other centrally acting drugs.
Cardiovascular diseases
Use intravenously with caution in elderly patients, patients with cardiac conduction abnormalities (including prolongation of the QT interval), patients with uncorrected electrolyte imbalances, those with bradycardia, and those taking other drugs that prolong the QT interval.
IV metoclopramide should be administered slowly (over at least 3 minutes) to reduce the risk of side effects (eg, hypotension, akathisia).
Metoclopramide is used with caution in patients with bronchial asthma, arterial hypertension, and impaired liver and/or kidney function.
Patients with impaired renal and liver function
When using the drug in patients with impaired renal function and in patients with severe liver dysfunction, a dose reduction is recommended.
Hypokalemia
In patients with impaired renal function, hypokalemia may occur during treatment with metoclopramide because the drug increases plasma aldosterone concentrations and decreases sodium excretion.
Depression
In patients with a history of depression, especially moderate or severe depression, accompanied by suicidal tendencies, a relapse of the disease may occur during treatment with metoclopramide. Before starting treatment, it is necessary to weigh the ratio of the potential benefits of treatment to the possible risks.
Endocrine system disorders
Metoclopramide causes a transient increase in aldosterone levels in
plasma. This can lead to fluid retention in the body, especially in patients with cirrhosis or congestive heart failure.
Application in pediatrics
For children aged 1-14 years, metoclopramide is prescribed only in case of a confirmed diagnosis.
Application in geriatrics
When used in elderly patients, it must be borne in mind that with long-term use of the drug in high or medium doses, the most common side effect is extrapyramidal disorders, especially parkinsonism and tardive dyskinesia.
Pregnancy and lactation
Numerous data obtained on the use of metoclopramide in pregnant women (more than 1000 described cases) indicate the absence of fetotoxicity and the ability to cause malformations in the fetus. But embryotoxic data do not indicate complete safety of the drug. Therefore, metoclopramide can be used during pregnancy (I-II trimesters of pregnancy) only if the potential benefit to the mother outweighs the potential risk to the fetus. It is not used in the third trimester of pregnancy, since the possibility of developing extrapyramidal symptoms in the newborn cannot be excluded. Metoclopramide is excreted in breast milk and is not recommended for use during breastfeeding.
Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
When taking the drug, you should avoid potentially hazardous activities that require increased attention, rapid mental and motor reactions (driving vehicles, etc.).
Overdose
Symptoms: drowsiness, confusion, hallucinations, irritability, convulsions, extrapyramidal movement disorders, dysfunction of the cardiovascular system with bradycardia and arterial hypo- or hypertension.
Treatment: drug withdrawal, symptomatic therapy. If symptoms of extrapyramidal disorders occur, symptomatic treatment is carried out (benzodiazepines in children and/or antiparkinsonian anticholinergic drugs in adults).
Release form and packaging
2 ml in ampoules made of colorless transparent glass.
5 ampoules are placed in a plastic container. 1 container, along with instructions for medical use in the state and Russian languages, is placed in a cardboard box.
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25°C. The drug should be stored out of the reach of children!
Shelf life
Do not use the drug after the expiration date indicated on the package.
Conditions for dispensing from pharmacies
On prescription
Manufacturer
Pharmaceutical plant "Polpharma" JSC
st. Pelplinska 19, 83-200 Starogard Gdanski, Poland
Registration Certificate Holder
"Khimpharm" JSC, Republic of Kazakhstan
Address of the organization that accepts claims from consumers regarding the quality of products (products) on the territory of the Republic of Kazakhstan
JSC "Khimpharm", Shymkent, Republic of Kazakhstan,
st. Rashidova, 81
Phone number 7252 (561342)
Fax number 7252 (561342)
E-mail address [email protected]
Photo of the drug
Latin name: Metoclopramide
ATX code: A03FA01
Active substance: Metoclopramide
Manufacturer: BORISOV MEDICAL PREPARATION PLANT (Republic of Belarus); PROMED EXPORTS (India); Moscow Endocrine Plant (Russia)
Description is valid on: 30.10.17
Metoclopramide is an antiemetic drug.
Release form and composition
Available in the form of tablets for oral administration and solution for injection.
Indications for use
Indications for use include conditions such as nausea, vomiting and hiccups. The drug can be prescribed for biliary dyskinesia, atony and hypotension of the stomach and intestines, flatulence, reflux esophagitis, exacerbation of gastric and duodenal ulcers (as part of complex therapy). Another indication is X-ray contrast examination of the gastrointestinal tract: in this case, this drug is used to accelerate intestinal motility.
Contraindications
- glaucoma;
- epilepsy;
- pheochromocytoma;
- prolactin-dependent tumors;
- perforation of the stomach or intestines;
- bleeding from the gastrointestinal tract;
- extrapyramidal disorders;
- intestinal obstruction of mechanical origin.
Contraindications for use are also hypersensitivity to the components of the drug, pregnancy and breastfeeding. Do not prescribe with simultaneous use of anticholinergic drugs.
Instructions for use Metoclopramide (method and dosage)
Pills
The tablets are taken orally half an hour before meals with a small amount of liquid.
Children over 6 years of age are prescribed 5 mg 1-3 times a day.
Injection
The solution can be administered intravenously or intramuscularly.
The dosage for adults is 10-20 mg 2-3 times a day (no more than 60 mg per day). For children over 6 years of age, the recommended dose is 5 mg, administered 1-3 times a day. Children from 2 to 6 years old are advised to administer a solution in the amount of 0.5-1 mg per kilogram of body weight per day.
In order to prevent and treat vomiting and nausea that occurs during radiation therapy or taking cystostatic drugs, it is administered intravenously at a dosage of 2 mg per kilogram of weight half an hour before taking the medication or performing the procedure. In case of urgent need, the drug can be re-administered after 2-3 hours.
Before conducting an X-ray examination with contrast, intravenous administration of a solution in the amount of 10-20 mg is recommended 15 minutes before the start of the procedure.
Side effects
Side effects usually appear at the beginning of treatment in the form of constipation, diarrhea, dizziness, headache, drowsiness, fatigue, depression, akathisia and agranulocytosis. In rare cases, dry mouth and skin rash may occur. With prolonged use, the drug can provoke the development of gynecomastia, galactorrhea and menstrual irregularities.
In children, Metoclopramide can cause hyperkinesia, spasms of the facial muscles and spasmodic torticollis. These side effects usually go away on their own immediately after stopping the drug.
In elderly patients, with prolonged use of the drug, tardive dyskinesia and parkinsonism may develop.
Overdose
There are no data on overdose.
Analogs
Analogs by ATC code: Metamol, Perinorm, Raglan, Cerucal, Ceruglan.
Do not decide to change the drug on your own; consult your doctor.
pharmachologic effect
Has an antiemetic effect. It reduces the symptoms of hiccups, nausea and vomiting, alleviating the patient's condition. The drug stimulates peristalsis of the gastrointestinal tract, reduces the reflux of stomach contents into the esophagus by increasing sphincter pressure.
Metoclopramide, the active ingredient of the drug, stimulates the production of prolactin and causes a transient increase in the level of circulating aldosterone, which may be accompanied by short-term fluid retention.
special instructions
For patients with severe renal or liver dysfunction, it is recommended to reduce the dosage by 2 times from the usual one. Further dose adjustment depends on the patient's response to the therapy.
Use with caution in patients with arterial hypertension, bronchial asthma and Parkinson's disease. When treating children, the drug should also be used with caution, as they are much more likely to develop dyskinetic syndrome. If there are strict indications, Metoclopramide can be used in children over the age of 2 years (in the form of injections) and over the age of 6 years (in the form of tablets).
During pregnancy and breastfeeding
Contraindicated during pregnancy and breastfeeding.
In childhood
The injection solution is contraindicated in children under 2 years of age, tablets up to 6 years of age. At older ages, it is used with extreme caution and in compliance with the recommended dosage regimen.
In old age
It is used with extreme caution for the treatment of elderly people due to the high risk of developing dyskinesia and parkinsonism.
For impaired renal function
It is prescribed with extreme caution for severe renal dysfunction.
For liver dysfunction
It is prescribed with extreme caution for severe liver dysfunction.
Drug interactions
- When used simultaneously with anticholinergic drugs, a mutual weakening of the therapeutic effects occurs. The drug can also reduce the bioavailability of ketoprofen, the effectiveness of cabergoline and the antiparkinsonian effect of levodopa.
- When taking Metoclopramide in combination with zopiclone, paracetamol, acetylsalicylic acid, ethanol, diazepam, mefloquine, morphine, mexiletine and cyclosporine, the absorption of these drugs is accelerated.
- Antipsychotic drugs, as well as fluvoxamine and fluoxetine, increase the risk of developing extrapyramidal conditions during treatment. The effectiveness of the drug may be reduced when tolterodine is used concomitantly. If it is necessary to use Metoclopramide before injecting thiopental or propofol, it may be necessary to reduce the dosage of these drugs.
– a medicinal drug that can cope with the syndrome of nausea and vomiting, as well as paroxysmal headaches – migraines. The chemical composition of the medicine is close to dimethpramide and sulpiride, but not similar to them.
Release form
Metoclopramide is manufactured and sold in different dosage forms.
- In tablets– round, flat-cylindrical, chamfered, white (option: almost white) color with a marble tint. Packed: 50 pcs. into a blister and then into a cardboard box (each box contains 1 blister). Another packaging option is 10 pcs. in blisters (1-5 or 10 blisters are packed in one cardboard box). Possible packaging of 50 pcs. in glass bottles or jars made of safe polymer material (one such bottle is placed in a cardboard box). The packaging allows you to choose the optimal number of tablets for treatment without unnecessary expenses.
- In ampoules for injection, 2 ml of solution each, administered intramuscularly or intravenously. Ampoules are packed in 5 or 10 pcs. or 5-10 pcs. in a plastic tray; 1 box contains 1 or 2 pallets. Different packaging options allow you to carry out an individually prescribed course of treatment without the cost of extra ampoules. Naturally, the drug, as befits an injection solution, is sterile.
Compound
Each metoclopramide tablet contains:
- active ingredient – metoclopramide hydrochloride monohydrate – 10 mg (in terms of dry matter);
- excipients: lactose monohydrate – 60 mg, potato starch “Extra” – 28.47 mg, enterosorbent – 0.53 mg, calcium stearate (calcium salt chemically combined with stearic acid) – 1 mg.
One dose of solution for injection includes:
- active ingredient: metoclopramide hydrochloride – 5 mg.
Pharmacological properties
Acts as a substance capable of blocking serotonin and dopamine receptors.
- It helps to suppress the activity of receptors in the trigger zone of the brain stem, which is responsible for the body’s susceptibility to chemicals (including medications). It also reduces the sensitivity of the nerves of the autonomic nervous system, which transmit impulses from the duodenum and pylorus of the stomach to the vomiting center in the medulla oblongata.
The medicine has a significant effect on the hypothalamus and parasympathetic nervous system, which helps to activate the nerves leading to the gastrointestinal tract, as well as regulate and coordinate the tone of its upper section.
- Metoclopramide enhances the muscle activity of the stomach and intestines, activates peristalsis, prevents disruption of the lower esophageal sphincter, and reduces high acidity. The drug regulates the production of bile in an optimal amount, eliminates spasm of the sphincter of Oddi and problems with bile excretion, and does not affect the tone of the gallbladder.
The effect of metoclopramide on the gastrointestinal tract begins 10-15 minutes after an intramuscular injection and 1-3 minutes after an intravenous injection. This manifests itself in the form of increased movement of stomach contents into the duodenum for further digestion, abundant passage of fecal matter and a decrease in nausea and vomiting.
- Metoclopramide is freely broken down in the liver and excreted in the urine within 72 hours. Approximately 30 percent of the total metoclopramide hydrochloride is excreted unchanged. The active substance easily penetrates the placenta and the blood-brain barrier and can pass into breast milk.
It is worth remembering that due to its high ability to be absorbed and penetrate the placenta, the drug can affect the fetus.
When taking metoclopramide, it should be borne in mind that in patients with severe kidney disease, the rate of clearance of biological fluids and tissues from the active substance of the drug is reduced by 70 percent. An increase in its half-life from blood plasma was also noted (approximately 15 hours with a creatinine clearance of less than 10 ml/min and 10 hours with a creatinine clearance of 10‒50 ml/min).
In liver cirrhosis, accumulation of metoclopramide is possible, associated with a decrease in the plasma clearance rate by 50 percent.
Indications
- Nausea, hiccups, vomiting of various origins with the simultaneous undesirability of the vomiting process (the latter is possible, for example, when taking anticancer drugs or undergoing radiation therapy for malignant tumors).
- Flatulence is excessive gas formation in the intestines.
- Functional pathological narrowing of the pylorus.
- Decreased tone of the gastric and intestinal muscles, including those occurring as a consequence of surgery performed on it.
- Damage to the lower esophagus due to the entry of stomach contents into it.
- Hypomotor dyskinesia of the biliary tract and, as a consequence, bile stagnation.
- Exacerbation of stomach or duodenal ulcers.
Metoclopramide is taken to activate intestinal motility, which is necessary before X-rays of the digestive system, as well as to facilitate diagnostic probing (to empty the stomach and enhance the movement of digested food through the small intestine).
Directions for use and dosage
Metoclopramide tablets are taken orally. The dosage of the drug depends on several factors: the patient’s age, diagnosis, and general health.
- For adults the drug is usually prescribed in a dose of 5-10 mg 3-4 times a day.
- In case of severe nausea and indomitable vomiting, when taking in tablet form is not always possible, it is recommended to administer the drug by intramuscular or intravenous injection at a dose of 10 mg, it is also possible to instill the drug into the nose (12-20 mg in each nostril 2-3 times a day ).
- The maximum single dose of metoproclamide for adults is 20 mg, the maximum daily dose is 60 mg (regardless of the form of administration of the drug).
- For children over 6 years of age, the drug is prescribed at a dose of 5 mg 1-3 times a day orally or by injection.
- For children under 6 years of age, metoclopramide is administered only by injection, the daily dose is 0.5-1 mg/kg (this dose is taken 1-3 times a day, that is, completely and simultaneously, or the daily amount of the drug is divided into 2 or 3).
- To suppress unwanted nausea and vomiting that may occur when taking anticancer drugs or radiation, metoclopramide is administered intravenously half an hour before the start of procedures at a dose of 2 mg/kg body weight. If necessary, the injection can be repeated after 2-3 hours to prevent vomiting, which is unwanted in this case, which can be caused by taking medications and medical procedures.
- For X-ray contrast examination of the gastrointestinal tract, intravenous injection of metoclopramide at a dose of 10-20 mg is recommended 15 minutes before the start of the procedure.
- In case of liver or kidney failure, the usual dose of metoclopramide should be halved when first taking the medicine. The subsequent dosage will be calculated by a medical specialist based on the patient’s individual tolerance of the active substance.
Contraindications
- hypersensitivity to one or more components of the drug;
- bleeding from the gastrointestinal tract;
- narrowing of the lumen of the pylorus of the stomach (stenosis);
- intestinal obstruction of a mechanical nature;
- a through defect in the wall of the stomach or intestines;
- glaucoma;
- epilepsy (there is a serious risk of increased frequency and severity of seizures);
- Parkinson's disease (metoclopramide can cause an exacerbation of its symptoms);
- prolactin-dependent tumors (pituitary prolactinoma, breast cancer);
- children under 2 years of age.
The use of metoclopramide must be limited when:
- bronchial asthma due to the possibility of provoking bronchospasm by the drug;
- hypertension;
- liver or kidney failure;
- children under 14 years of age;
- elderly patient.
Side effects
- From the cardiovascular system: arrhythmia and disturbances in the movement of blood through blood vessels.
- From the side of the central nervous system: spasm of the facial muscles, trismus of the jaws, torticollis of a spastic nature, bulbar speech impairment, parkinsonism (in children the risk of its development increases when the dosage is exceeded), spasm of the extraocular muscles, hypertonicity and opisthotonus of the muscles, dyskinesia (with renal failure and in elderly patients), frequent headaches, increased anxiety, fatigue, depression, hearing loss - tinnitus.
- From the endocrine system: disturbances in the frequency of the menstrual cycle and the duration of menstruation, spontaneous release of breast milk from the mammary glands, gynecomastia in men (usually due to a systematic overdose of the drug).
- From the digestive system: constipation, diarrhea, dry mouth (sometimes).
- From the hematopoietic system: decrease in the number of leukocytes per unit volume of blood, decrease in the number of neutrophils per unit volume of blood, sulfohemoglobinemia in adults.
- From the side of metabolism: porphyrin disease.
As a consequence of taking metoclopramide, allergic reactions are possible, including severe conditions provoked by allergies: urticaria, bronchospasm, Quincke's edema (the so-called “giant urticaria”).
If these symptoms occur, you must immediately contact a medical specialist and prescribe appropriate treatment.
Use during pregnancy and lactation
- Metoclopramide should not be taken by a woman in the third trimester of pregnancy, as this can lead to the development of neurological disorders in the newborn, manifested by motor disorders.
If a pregnant woman needs to take the drug for objective reasons, the newborn will subsequently need to be registered with a pediatric neurologist.
- According to the instructions for use of Metoclopramide, the drug should not be taken by a woman during lactation, since the active substance is found in breast milk and can harm the baby. If there is an objective need to take the drug, breastfeeding should be stopped.
Prescription for children
According to the instructions for taking metoclopramide, the drug is prescribed to children (especially young children) with great caution, since there is a risk of developing dyskinetic syndrome.
Drug interactions
Use of metoclopramide:
- enhances the effect of sedatives and hypnotics;
- enhances the effects of alcohol on the central nervous system, therefore combining metoclopramide with alcohol is prohibited;
- increases the absorption of paracetomol,
Name:
Metoclopramide.
INN:
Metoclopramide
ATX code: A03FA01.
Dosage form:
solution for injection 5 mg/ml.
Compound:
One ampoule (2 ml solution) contains
Active substance:
Metoclopramide hydrochloride - 10 mg;
Excipients:
Sodium chloride, sodium sulfite anhydrous, disodium edetate, propylene glycol, hydrochloric acid, water for injection.
Description:transparent colorless liquid.
Pharmacotherapeutic group:
Antiemetics are blockers of central D2 - dopamine receptors. Stimulants of gastrointestinal motility.
Pharmacological properties
Pharmacodynamics
Antiemetic, helps reduce nausea, hiccups; stimulates peristalsis of the upper gastrointestinal tract. The antiemetic effect is due to the blockade of dopamine receptors and an increase in the threshold for excitation of trigger zone chemoreceptors. Metoclopramide is believed to inhibit dopamine-induced relaxation of gastric smooth muscle, thereby enhancing the cholinergic responses of gastrointestinal smooth muscle. Helps accelerate gastric emptying by preventing relaxation of the body of the stomach and increasing the phase activity of the antrum of the stomach. In this case, the upper parts of the small intestine relax, which leads to improved coordination of peristalsis of the body and the antrum of the stomach and the upper parts of the small intestine. Reduces reflux of contents into the esophagus by increasing the pressure of the lower esophageal sphincter at rest and increases the clearance of acid from the esophagus by increasing the amplitude of its peristaltic contractions.
Metoclopramide stimulates prolactin secretion and causes a transient increase in circulating aldosterone levels, which may be accompanied by short-term fluid retention
Pharmacokinetics
Protein binding is about 30%. Passes through the placental barrier and blood-brain barrier, penetrates into breast milk. The effect begins to develop 10 - 15 minutes after intramuscular administration and 1 - 3 minutes after intravenous administration. T1/2 - 3-5 hours, in case of renal dysfunction - up to 14 hours. The drug is excreted mainly through the kidneys (85% within 72 hours) unchanged and in the form of sulfate and glucuronide conjugates.
Indications for use
Vomiting, nausea, hiccups of various origins (in some cases it can be effective for vomiting caused by radiation or chemotherapy), atony and hypotension of the stomach and intestines (in particular, postoperative); biliary dyskinesia; reflux esophagitis, flatulence, exacerbation of gastric and duodenal ulcers (as part of complex therapy).
X-ray contrast studies of the gastrointestinal tract (to enhance peristalsis).
Contraindications
Hypersensitivity, gastrointestinal bleeding, pyloric stenosis, mechanical intestinal obstruction, perforation of the stomach or intestines, 3-4 days after surgery on the stomach and/or intestines, pheochromocytoma, extrapyramidal disorders, epilepsy, prolactin-dependent tumors, pregnancy, children under 3- x years, lactation period.
Due to the sodium sulfite content, metoclopramide solution should not be prescribed to patients with bronchial asthma with hypersensitivity to sulfite.
Precautionary measures
Use with caution in case of bronchial asthma, arterial hypertension, Parkinson's disease, liver and/or kidney failure, in old age, early childhood (increased risk of dyskinetic syndrome).
Directions for use and doses
The injection solution is administered intravenously or intramuscularly over 1-2 minutes: for adults at a dose of 10 mg 3 to 4 times a day (maximum single dose - 20 mg, maximum daily dose - 60 mg); children over 6 years old - 2.5 - 5 mg 1 - 3 times a day; for children under 6 years of age, the daily dose is 0.5 - 1 mg/kg, the frequency of administration is 1-3 times. The highest daily dose for children is 0.5 mg/kg.
The average duration of treatment is 4-6 weeks, in some cases up to 6 months.
For the prevention and treatment of nausea and vomiting, caused by the use of cytostatics or radiation therapy, the drug is administered:
Intermittent intravenous infusion (over at least 15 minutes) at a dose of up to 2 mg/kg 30 minutes before the use of cytostatics or irradiation, and also after 1.5; 3.5; 5.5 and 8.5 hours after application (maximum daily dose 10 mg/kg);
Long-term intravenous infusion at a dose of 1 (0.5) mg/kg body weight per hour, starting 2 hours before the use of a cytostatic agent and ending at the time of use of the cytostatic agent, then at a dose of 0.5 (0.25) mg/kg body weight bodies per hour for 12 - 24 hours after use of a cytostatic agent (maximum daily dose 10 mg/kg).
Each short (within 15 minutes) intravenous drip infusion is carried out after preliminary dilution of a single dose in 50 ml of infusion solution. The solution can be diluted with isotonic sodium chloride solution or 5% glucose solution. The drug must not be mixed with alkaline infusion solutions.
For decreased kidney function, the drug is prescribed:
With creatinine clearance up to 10 ml/min - 10 mg 1 time per day;
With creatinine clearance from 11 to 60 ml/min - 15 mg/day, divided into 2 injections (10 mg and 5 mg).
Side effect
From the digestive system: at the beginning of treatment, constipation and diarrhea are possible; rarely - dry mouth.
From the side of the central NS: at the beginning of treatment, feelings 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 (usually disappear immediately after stopping metoclopramide). With long-term use, more often in elderly patients, parkinsonism and dyskinesia are possible.
From the hematopoietic system: agranulocytosis is possible at the beginning of treatment.
From the endocrine system: rarely, with long-term use in high doses - galactorrhea, gynecomastia, menstrual irregularities.
Allergic reactions: rarely - skin rash.
special instructions
During treatment with the drug, you should not drink alcohol or alcohol-containing drugs.
Use during pregnancy and breastfeeding
Contraindicated for use during pregnancy.
When used during lactation (breastfeeding), it should be taken into account that metoclopramide passes into breast milk.
Experimental studies have not established any adverse effects of metoclopramide on the fetus.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Interaction with other drugs
The effect may be weakened by cholinesterase inhibitors.
The drug enhances the absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol; reduces the absorption of digoxin and cimetidine.
The drug is not prescribed simultaneously with antipsychotics (the risk of extrapyramidal disorders increases).
Overdose
Symptoms:
Hypersomnia, increased or decreased blood pressure, dysfunction of the cardiovascular system with bradycardia, disorientation and extrapyramidal disorders.
Symptoms disappear after stopping the drug for 24 hours.
Treatment:
In case of severe poisoning, extrapyramidal disorders can be quickly eliminated by slow intravenous administration of biperiden (doses for adults are 2.5 - 5 mg, for children 0.04 mg/kg body weight).
Package
In ampoules of 2 ml, in packaging No. 10, No. 10 x 1.
Storage
In a place protected from light, at a temperature not exceeding 25ºС. Keep out of the reach of children.
Best before date- 3 years.
Manufacturer
Open Joint Stock Company "Borisov Medical Preparations Plant", Republic of Belarus
