Metoclopramide
Metoclopramide: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. Drug interactions
- 12. Analogs
- 13. Terms and conditions of storage
- 14. Terms of dispensing from pharmacies
- 15. Reviews
- 16. Price in pharmacies
Latin name: Metoclopramide
ATX code: A03FA01
Active ingredient: metoclopramide (metoclopramide)
Producer: FGUP Moscow Endocrine Plant, Ellara LLC, Novosibkhimfarm OJSC, SOTEX PharmFirma CJSC, Promomed Rus LLC, PFC Update (Russia), PROMED EXPORTS (India), Borisov Medicines Plant (Belarus), POLFARMA Pharmaceutical Plant JSC (Poland)
Description and photo update: 2019-18-09
Prices in pharmacies: from 25 rubles.
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Metoclopramide is an antiemetic drug.
Release form and composition
Metoclopramide is available in the following dosage forms:
- Tablets: flat-cylindrical, round, with a bevel, almost white or white, marbling is allowed (50 pieces in blisters, 1 package in a cardboard box; 10 pieces in blisters or blisters, 1-5, 10 packages or blisters in a cardboard box; 14 pcs. in blisters, 4 packages in a cardboard box; 50 pcs. in polymer or dark glass jars, 1 jar in a cardboard box);
- Solution for intravenous and intramuscular administration (in 2 ml ampoules, 5 or 10 ampoules in a carton box, or 5 or 10 ampoules in plastic or cell contour packs (pallets), 1 or 2 packs in a carton box).
The composition of 1 tablet of Metoclopramide includes:
- Active ingredient: metoclopramide hydrochloride - 10 mg (in the form of metoclopramide hydrochloride monohydrate in terms of dry matter);
- Auxiliary components: lactose monohydrate - 60 mg, potato starch "Extra" - 28.47 mg, povidone - 0.53 mg, calcium stearate - 1 mg.
The composition of 1 ml of Metoclopramide injection solution contains the active substance: Metoclopramide hydrochloride - 5 mg.
Pharmacological properties
Pharmacodynamics
Metoclopramide is a specific blocker of dopamine (D 2) and serotonin (5-HT 3) receptors. It suppresses the activity of chemoreceptors localized in the trigger zone of the brainstem, and reduces the sensitivity of the visceral nerves responsible for the transmission of impulses from the duodenum and pylorus to the vomiting center.
Metoclopramide acts on the hypothalamus and parasympathetic nervous system, which leads to innervation of the gastrointestinal tract and allows you to regulate and coordinate the motor activity and tone of the upper gastrointestinal tract (including the tone of the lower esophageal sphincter). Strengthens the tone of the stomach and intestines, activates intestinal peristalsis, accelerates gastric emptying, prevents esophageal and pyloric reflux, reduces the severity of hyperacid stasis. The drug normalizes the secretion of bile and eliminates the spasm of the sphincter of Oddi, as well as dyskinesia of the gallbladder, without affecting the tone of the latter.
For metoclopramide, ganglion-blocking, m-anticholinergic, antiserotonin and antihistamine effects are uncommon. Also, the substance does not change the respiratory function, the functioning of the liver and kidneys, does not affect the tone of the blood vessels of the brain, hematopoiesis, blood pressure, secretion of the stomach and pancreas.
Metoclopramide stimulates the synthesis of prolactin and increases the sensitivity of tissues to acetylcholine (the effect is not determined by vagal innervation, but is eliminated with the help of anticholinergics). It also activates the production of aldosterone, while slowing down the excretion of sodium and potassium ions from the body.
Pharmacokinetics
Metoclopramide begins to act on the gastrointestinal tract approximately 10-15 minutes after intramuscular administration and 1-3 minutes after intravenous administration, which is reflected in the accelerated evacuation of stomach contents and antiemetic effect. The substance is metabolized in the liver and excreted mainly in the urine within 24-72 hours (approximately 85% of the dose), 30% of metoclopramide ingested is excreted unchanged. It easily crosses the blood-brain and placental barriers, and is also determined in breast milk.
When taken orally, metoclopramide is rapidly absorbed from the gastrointestinal tract, and its bioavailability is 80 ± 15%. The degree of binding to plasma proteins (in particular albumin) varies from 13 to 22%. The maximum concentration of metoclopramide in the blood is directly proportional to the dose taken and is usually reached after 1–2 hours. The half-life of the drug in tablet form is 2.5–6 hours (with reduced renal function - up to 14 hours).
In patients with severe renal dysfunction, the clearance of metoclopramide is reduced by 70%. An increase in the half-life of it from blood plasma is also observed (approximately 15 hours with CC less than 10 ml / min and 10 hours with CC 10-50 ml / min). In patients with cirrhosis of the liver, the accumulation of metoclopramide is possible, due to a decrease in plasma clearance by 50%.
Indications for use
- Nausea, vomiting, hiccups of various etiology (in some cases, metoclopramide may be effective in treating vomiting caused by taking cytostatics or radiation therapy);
- Functional pyloric stenosis;
- Flatulence;
- Hypotension and atony of the stomach and intestines, including postoperative;
- Reflux esophagitis;
- Hypomotor dyskinesia of the biliary tract;
- Peptic ulcer of the stomach and duodenum (with exacerbation, along with other drugs).
Also, the drug is prescribed when conducting X-ray contrast studies of the gastrointestinal tract (to enhance peristalsis) and as a means of facilitating duodenal intubation (in order to accelerate gastric emptying and the movement of food through the small intestine).
Contraindications
Absolute:
- Glaucoma;
- Pyloric stenosis;
- Bleeding from the gastrointestinal tract;
- Perforation of the walls of the stomach or intestines;
- Prolactin-dependent tumors;
- Parkinson's disease;
- Mechanical intestinal obstruction;
- Pheochromocytoma;
- Extrapyramidal disorders;
- Epilepsy;
- Vomiting associated with treatment or overdose of antipsychotics, as well as in patients with breast cancer;
- Bronchial asthma against a background of hypersensitivity to sulfites (injection solution);
- Lactase deficiency, glucose-galactose deficiency, lactose intolerance (tablets);
- I trimester of pregnancy and lactation;
- Age up to 2 years (any dosage forms of metoclopramide); up to 6 years old (injection solution); up to 14 years old (tablets);
- Hypersensitivity to drug components.
According to the instructions, Metoclopramide in any dosage form should not be used after operations on the gastrointestinal tract (intestinal anastomosis, pyloroplasty), since vigorous muscle contractions prevent healing.
Relative (Metoclopramide should be used with caution in the presence of the following diseases / conditions):
- Bronchial asthma;
- Arterial hypertension;
- Hepatic and / or renal failure;
- Children and elderly (over 65) age;
- II-III trimesters of pregnancy.
Instructions for the use of Metoclopramide: method and dosage
Injection solution
Metoclopramide is administered intravenously or intramuscularly.
The drug is prescribed depending on age:
- Adults: 1-3 times a day, 10-20 mg (maximum 60 mg per day);
- Children from 6 years old: 1-3 times a day, 5 mg.
30 minutes before taking cytostatics or radiation therapy for the treatment and prevention of nausea and vomiting, metoclopramide is administered intravenously at a dose of 2 mg / kg of body weight. If necessary, the solution may be re-administered after 2-3 hours.
5-15 minutes before the X-ray examination, 10-20 mg of metoclopramide is administered intravenously.
In case of clinically severe hepatic and / or renal failure, the dose must be reduced by 2 times, the subsequent dose is determined by the patient's individual response to therapy.
Pills
Metoclopramide tablets are taken orally, 30 minutes before meals, with a small amount of water.
A single dose for adults is 10 mg, the maximum daily dose is 30 mg or 0.5 mg per 1 kg of body weight.
Metoclopramide for children from 14 years old is prescribed at 0.1-0.15 mg per 1 kg of body weight, maximum per day - 0.5 mg per 1 kg of body weight.
The maximum duration of therapy is 5 days.
With renal failure, dose adjustment is necessary:
- Terminal stage (with creatinine clearance less than 15 ml per minute): 25% of the daily dose;
- Moderate and severe stage (with creatinine clearance 15-60 ml per minute): 50% of the daily dose.
In severe liver failure, the dose should be reduced by 50%.
Side effects
- Cardiovascular system: atrioventricular block;
- Central nervous system: extrapyramidal disorders - trismus, spasm of the facial muscles, spastic torticollis, bulbar type of speech, rhythmic protrusion of the tongue, spasm of extraocular muscles (including oculogyric crisis), muscular opisthotonus, hypertonicity; parkinsonism (muscle rigidity, hyperkinesis - a manifestation of dopamine-blocking action, the risk of development in children increases when the dose is exceeded 0.5 mg / kg per day), dyskinesis (in chronic renal failure and in elderly patients), depression, headache, drowsiness, anxiety, fatigue, confusion, tinnitus;
- Endocrine system: rarely (with prolonged therapy in high doses) - galactorrhea, gynecomastia, menstrual irregularities;
- Digestive system: diarrhea, constipation; rarely - dry mouth;
- Hematopoietic system: leukopenia, neutropenia, sulfhemoglobinemia in adults;
- Metabolism: porphyria;
- Allergic reactions: angioedema, bronchospasm, urticaria;
- Others: at the beginning of treatment - agranulocytosis; rarely (when using high doses) - hyperemia of the nasal mucosa.
In the event of the appearance of the above symptoms, their aggravation or the development of other side effects, you should consult a doctor.
Overdose
The main symptoms of an overdose of metoclopramide are considered extrapyramidal disorders, respiratory and cardiac arrest, drowsiness, hallucinations, blurred consciousness, fainting and semi-fainting.
If the patient is diagnosed with extrapyramidal symptoms, provoked by an overdose, or another reason, the appointment of symptomatic therapy is recommended (anticholinergic antiparkinsonian drugs in adults and / or benzodiazepines in children).
Depending on the clinical condition of the patient, symptomatic treatment and regular monitoring of respiratory and cardiac functions are required.
special instructions
With vomiting of vestibular genesis, Metoclopramide is not effective.
When using metoclopramide, the data of laboratory indicators 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 using 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 while using Metoclopramide.
During the treatment period, care should be taken when working with potentially dangerous mechanisms that require increased concentration of attention and rapid psychomotor reactions, as well as when driving.
Application during pregnancy and lactation
The use of metoclopramide is contraindicated in the third trimester of pregnancy, since it can lead to the development of extrapyramidal disorders in newborns. When prescribing the drug to pregnant women, it is necessary to carry out constant monitoring of the newborn.
Metoclopramide is determined in breast milk, so the lactation period is a contraindication to prescribing the drug. Breastfeeding should be discontinued before starting treatment.
Pediatric use
With extreme caution, prescribe metoclopramide to children, especially young children, since in this case the risk of developing dyskinetic syndrome significantly increases.
Drug interactions
With the simultaneous use of metoclopramide with certain drugs, the following effects may occur:
- Ethanol: increased action on the central nervous system;
- Cholinesterase inhibitors: weakening the action of metoclopramide;
- Sleeping pills: enhancing the sedative effect;
- Blockers of H 2 -histamine receptors: increasing the effectiveness of therapy;
- Diazepam, tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol: increased absorption;
- Digoxin, cimetidine: absorption delay;
- Antipsychotics: an increased risk of developing extrapyramidal symptoms.
Before the simultaneous use of other medicines, you should consult your doctor.
Analogs
Analogues of Metoclopramide are: Metamol, Vero-Metoclopramide, Perinorm, Cerucal, Metoclopramide-Vial, Metoclopramide-Eskom, Reglan.
Terms and conditions of storage
Store in a dark, dry place out of reach of children at temperatures up to 25 ° C.
Shelf life:
- Tablets - 2 years;
- Injection solution - 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Metoclopramide
On the Internet, there are often positive reviews about metoclopramide. Patients consider it to be a fairly effective remedy, and doctors are actively using it as part of antiemetic therapy. Patients undergoing treatment with cytostatics, as well as those who are faced with radiation therapy, report that metoclopramide is successful in treating nausea and vomiting.
Price for Metoclopramide in pharmacies
The approximate price of Metoclopramide tablets is 29-35 rubles (the package includes 50 pcs.). You can buy a solution for intravenous and intramuscular administration for about 50-85 rubles (the package includes 10 ampoules).
Metoclopramide: prices in online pharmacies
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Drug name Price Pharmacy |
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Metoclopramide 10 mg tablets 56 pcs. RUB 25 Buy |
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Metoclopramide 5 mg / ml solution for intravenous and intramuscular administration 2 ml 10 pcs. RUB 54 Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
