The antiemetic drug metoclopramide. What are Metoclopramide tablets for? Use during pregnancy and breastfeeding
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The drug metoclopramide
Metoclopramide– medicinal antiemetic drug, used for vomiting of various origins.Other reactions:
- increased frequency of urination or urinary incontinence;
- gynecomastia (one- or two-sided excessive enlargement of the mammary glands in men, similar to women’s);
- menstrual irregularities;
- galactorrhea (discharge of milk or milk-like fluid from the mammary glands);
- porphyria (pigment metabolism disorder);
- bronchospasm;
- hyperemia (redness) of the nasal mucosa.
Treatment with metoclopramide
How to take metoclopramide?Metoclopramide is taken 15-30 minutes before meals, without chewing; Take the tablet with a small amount of water. Metoclopramide in solution for injection can be administered both intravenously and intramuscularly. This solution can also be used as nasal drops.
During treatment with metoclopramide, you should avoid drinking alcoholic beverages, as they increase the risk of complications.
Given the decrease in concentration and slower reactions when taking metoclopramide, you should stop driving a car during the course of treatment, and also avoid working with potentially dangerous equipment.
Metoclopramide dosage
Pills
Adults are prescribed 5-10 mg orally (0.5-1 tablet) 3-4 times a day. The maximum single dose for adults is 20 mg (2 tablets), the maximum daily dose is 60 mg (6 tablets).
The average duration of treatment in adults is 4-6 weeks.
Injection
Adults are prescribed intramuscularly or intravenously:
- for paresis of the stomach and intestines, 10-15 mg up to 4 times a day;
- for the purpose of prevention and treatment of vomiting (nausea) during chemotherapy or radiation therapy - administer an intravenous dose at the rate of 1-2 mg per 1 kg of weight half an hour before a chemotherapy session (or radiation therapy) and then every 2-4 hours (if necessary) ;
- 5-15 minutes before an X-ray examination or before insertion of a probe, 10-20 mg of metoclopramide is administered intravenously to adult patients.
For intranasal administration, a solution of metoclopramide is instilled into each nasal passage, 10-20 mg of the drug several times a day.
The following signs will indicate an overdose of the drug: hypersomnia (severe drowsiness during the day or very long night sleep), confusion and the appearance of extrapyramidal disorders (impaired muscle tone and movements from involuntary twitching to immobility). If these signs occur, you should stop taking metoclopramide. Symptoms will disappear within a day after stopping use.
Metoclopramide for children
In early childhood (up to 2 years), metoclopramide is contraindicated in any dosage form.Children under 6 years of age can only use tablet forms according to strict indications and with caution. Dosage – 0.5-1 mg per 1 kg of child’s body weight per day. The daily dose is divided into 3 doses. Older children are prescribed 5 mg (0.5 tablets) 3 times a day.
When carrying out chemotherapy and radiation therapy, 1-2 mg of metoclopramide per 1 kg of body weight is administered intravenously half an hour before the treatment session, then repeated if necessary after 3-4 hours.
The course of treatment with metoclopramide in children should be as short as possible.
Before an X-ray examination of the gastrointestinal tract or before insertion of a probe, the drug is administered intravenously 5-15 minutes: children under 6 years old - 0.1 mg per 1 kg of body weight, and children over 6 years old - 2.5-5 mg per 1 kg body weight.
Metoclopramide during pregnancy
Metoclopramide is contraindicated in the first trimester of pregnancy. In the second and third trimesters, the use of metoclopramide is allowed only for health reasons, because studies were carried out only on animals, although no adverse effects of the drug on the fetus were detected. Since metoclopramide passes into breast milk, if it is necessary to prescribe it during lactation, you should stop breastfeeding the baby.
Interaction of metoclopramide with other drugs
Metoclopramide enhances the effect of hypnotics and the effect of alcohol on the central nervous system; increases the absorption of Ampicillin, Tetracycline, Levodopa, Paracetamol, Aspirin (acetylsalicylic acid); increases the effectiveness of drugs that reduce the acidity of gastric juice - such as Ranitidine, Famotidine; slows down the absorption of Cimetidine and Digoxin (dosage adjustments of these drugs may be required).The effect of metoclopramide can be weakened by cholinesterase inhibitors (Galantamine, Ezerin or Physostigmine, Prozerin, Pirofos, Armin, Phosphacol). The effect of the drug on gastrointestinal motility can be blocked by drugs containing opioids.
The simultaneous use of metoclopramide and antipsychotics (especially butiformenone derivatives and phenothiazines) is undesirable, because at the same time, the risk of developing extrapyramidal disorders increases (changes in muscle tone and movement disorders from hyperkinesis or twitching to immobility).
Metoclopramide analogues
There are many structural analogues (synonyms) of metoclopramide:Raglan, Metoclopramide hydrochloride, Clometol, Cerucal, Reliverin, Perinorm, Priperil, Bimaral, Primperan, Comportan, Pramin, Viscal, Gastrobids, Plastil, Peraprin, Imperial, Paspertine, Maxolon, Clopan, Metoclol, Nauzifar, Moriperan, Legir, Emetizan, Maxeran , Regastrol, Terperan, Rimetin.
Preparations with a similar effect (but with a different chemical composition):
Domrid, Domstal, Motoricum, Dimetcarb, Dimetpramid.
1. Pharmacological action
A drug that eliminates nausea, the gag reflex and can stimulate the natural fluctuations of the digestive system, which leads to faster movement of food. It blocks serotonin receptors and is able to stimulate the production of prolactin and increase the concentration of aldosterone.2. indications for use
- Nausea of various origins;
- Hiccups of various origins;
- Decreased or complete loss of tone of the digestive system organs, caused by various reasons;
- Reverse movement of food;
- Acceleration of natural vibrations of the organs of the digestive system (preparation for instrumental and x-ray examinations);
- Vomiting of various origins;
- Narrowing of the lumen of the biliary tract;
- Gastric ulcer in the acute stage (as part of a medicinal complex);
- Duodenal ulcer (as part of a drug complex).
3. Method of application
Recommended dosage of Metoclopramide for:- pediatric patients (up to 6 years): 0.5-1 mg of the drug per kg of body weight up to three times a day;
- pediatric patients (over 6 years): 5 mg of the drug up to three times a day;
- adult patients: 5-10 mg of the drug up to three times a day;
- maximum single oral dose (adult patients): 20 mg of the drug;
- maximum daily dose for adult patients: 60 mg of the drug.
- Patients suffering from high blood pressure, renal impairment, liver dysfunction, or Parkinson's disease should take Metoclopramide with caution;
- Long-term use may cause movement disorders associated with the activity of the central nervous system;
- Use may cause distortion of laboratory tests for liver function, aldosterone and prolactin concentrations;
- During treatment, you should refrain from engaging in vigorous activities, including driving vehicles and operating complex machinery.
4. Side effects
- Endocrine system: leakage of milk from the mammary glands, menstruation irregularities;
- Central nervous system: increased fatigue, dizziness, depression, motor restlessness, the appearance of uncontrolled movements, spasms of various muscle groups, drowsiness, headaches, various movement disorders, parkinsonism;
- Hypersensitivity reactions of patients to Metoclopramide: skin rashes;
- Hematopoietic system: increased number of agranulocytes;
- Digestive system: dry mouth, indigestion.
5. Contraindications
- Active bleeding of the digestive system;
- Phenomena of perforation of the digestive system;
- Motor disorders due to damage to the nervous system;
- Presence of prolactin-dependent tumors;
- Any trimester of pregnancy;
- Concomitant use of Metoclopramide with acetylcholine blockers;
- Hypersensitivity of patients to Metoclopramide or its components;
- Intestinal obstruction caused by mechanical reasons;
- Presence of an adrenal tumor;
- Periodic epileptic seizures;
- Individual intolerance to Metoclopramide or its components;
- Breastfeeding during treatment with Metoclopramide;
- Patients with glaucoma.
6. During pregnancy and lactation
Use of Metoclopramide during pregnancy strictly contraindicated.The use of Metoclopramide during breastfeeding is possible only after its cessation.
7. Interaction with other drugs
Concomitant use of Metoclopramide with:- blockers of acetylcholine receptors leads to a mutual decrease in their effectiveness;
- sedatives lead to movement disorders;
- Paracetamol, Acetylsalicylic acid, ethyl alcohol or alcohol leads to increased absorption;
- Cabergoline or Levodopa drugs leads to a decrease in their medicinal effect;
- Ketoprofen leads to a decrease in the bioavailability of the latter;
- Mexiletine accelerates the elimination of Mexiletine from the body;
- Mephchloin leads to accelerated absorption of Mephchloin and an increase in its plasma concentration;
- Morphine leads to an increase in its sedative effect;
- Nitrofurantoin leads to a decrease in the absorption of Nitrofurantoin from the gastrointestinal tract;
- Tolterodine leads to a decrease in the effectiveness of Metoclopramide;
- Fluoxetine leads to movement disorders;
- Cyclosporine leads to an increase in its concentration in the blood plasma and the occurrence of side effects.
8. Overdose
Overdose with Metoclopramide has not been described.The side effects of the drug may increase.
9. Release form
Tablets, 10 mg - 10, 20, 30, 40 or 50 pcs.Solution for injection in ampoules, 10 mg/2 ml - amp. 5, 10 or 20 pcs; 5 mg/ml - 2 ml amp. 10 pieces.
10. Storage conditions
Metoclopramide is stored in a dry, dark place.11. Composition
1 tablet:
- metoclopramide - 10 mg.
1 ml solution:
- metoclopramide hydrochloride - 5 mg.
12. Conditions for dispensing from pharmacies
The drug is dispensed according to the prescription of the attending physician.Found a mistake? Select it and press Ctrl + Enter
* Instructions for medical use of the drug Metoclopramide are published in free translation. THERE ARE CONTRAINDICATIONS. BEFORE USE, YOU MUST CONSULT WITH A SPECIALIST
Compound
One ampoule (2 ml of solution) contains - active substanceva: 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 of the gastrointestinal tract; prokinetics.
ATX code: A03FA01.
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. T½ – 3 – 5 hours, in case of impaired renal function – 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.
In children, the pharmacodynamics of metoclopramide after intravenous administration is very variable and a clear concentration-effect relationship has not been established. Although the pharmacokinetics of metoclopramide have been studied in children for chemotherapy-induced nausea and vomiting, insufficient data are available to conclude whether the pharmacokinetics of metoclopramide are similar in adults and children. The half-life of metoclopramide in neonates (3.5 weeks of age) after the first and tenth dose was significantly longer (23.1 and 10.3 hours, respectively) compared to children of other age groups due to decreased clearance. This may be due to age-related immaturity of liver and kidney function at birth. The mean half-life of metoclopramide in children of other age groups was 4.1–4.5 hours (range: 1.7 to 12.5 hours).
In patients with renal failure, the clearance of metoclopramide decreases in proportion to the decrease in creatinine clearance, while its half-life increases. However, in this group of patients the pharmacokinetics of metoclopramide remain linear. Due to the decreased clearance of metoclopramide in this group of patients, the maintenance dose of metoclopramide should be reduced to avoid its accumulation. In severe renal failure, the clearance of metoclopramide is reduced by 70%, and the half-life is increased to 10 hours (with a creatinine clearance of 10 - 50 ml/min) and 15 hours (with a creatinine clearance of less than 10 ml/min).
In patients with impaired liver function (cirrhosis), accumulation of metoclopramide is possible, associated with a decrease in its clearance by 50%.
There are no data on the pharmacokinetics of the solution after administration to elderly people. There may be changes in pharmacokinetic parameters associated with age-related changes in liver and kidney function.
Indications for use
For adults. For the prevention of postoperative nausea and vomiting.
For the symptomatic treatment of nausea and vomiting, including nausea and vomiting due to acute migraine.
For the prevention of nausea and vomiting induced by 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.
Contraindications
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 a history of neuroleptic or metoclopramide-induced tardive dyskinesia), epilepsy, prolactin-dependent tumors, a history of episodes of methemoglobinemia while taking metoclopramide or with NADP-cytochrome-b5 deficiency, concomitant use of levodopa or dopamine stimulants receptors, pregnancy, children under 1 year of age, lactation period.
Due to the sodium sulfite content, metoclopramide solution should not be prescribed to patients with bronchial asthma with hypersensitivity to sulfite.
Directions for use and doses
The maximum duration of use of the drug is 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.
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.
Side effect
From the digestive system: at the beginning of treatment, constipation and diarrhea are possible; rarely - dry mouth.
From the central nervous system: at the beginning of treatment, a feeling of fatigue, drowsiness, dizziness, headache, depression, akathisia is possible, not often - dystonia, disturbances of consciousness, rarely - convulsions (especially in patients with epilepsy), frequency unknown - tardive dyskinesia, which can be constant, during or after long-term treatment (especially in elderly patients), neuroleptic malignant syndrome. With long-term use, more often in elderly patients, parkinsonism and dyskinesia are possible.
Mental disorders: rarely – hallucinations.
From the hematopoietic and lymphatic systems: at the beginning of treatment, agranulocytosis is possible, the frequency is unknown - methemoglobinemia, which may be associated with a deficiency of NADP-cytochrome b5 reductase, especially in newborns; sulfhemoglobinemia caused by sulfur-containing substances in the composition of the drug (mainly with the concomitant use of high doses of drugs containing sulfur).
From the heart: rarely - bradycardia, frequency unknown - cardiac arrest (occurs soon after injection, and may be a consequence of bradycardia); atrioventricular block, sinus node block (especially with intravenous administration); prolongation of the QT interval; arrhythmia by type torsade de points.
From the side of blood vessels: often - hypotension, especially with intravenous administration, frequency unknown - shock, fainting after injection, acute arterial hypertension in patients with pheochromocytoma.
From the endocrine system: rarely, with long-term use in high doses - hyperprolactinemia and associated amenorrhea, galactorrhea, gynecomastia, menstrual irregularities.
Common disorders: often - asthenia.
From the immune system: rarely - hypersensitivity reactions, frequency unknown - anaphylactic reactions (including anaphylactic shock, especially with intravenous administration).
Allergic reactions: rarely – skin rash.
The following reactions occur most often if high doses of metoclopramide are used: extrapyramidal symptoms: acute dystonia and dyskinesia, parkinsonism syndrome, akathisia (even after administration of a single dose of the drug, especially in children and young people); drowsiness, disturbances of consciousness, hallucinations.
Precautionary measures
During treatment with the drug, you should not drink alcohol or alcohol-containing drugs.
It should be used with caution in case of bronchial asthma, arterial hypertension, liver and/or kidney failure, in old age, early childhood (increased risk of dyskinetic syndrome).
Neurological disorders. Extrapyramidal disorders occur more often in children or when the drug is prescribed in high doses. As a rule, they occur at the beginning of therapy, even with a single dose of the drug. These disorders are completely reversible and, if they occur, the administration of metoclopramide must be stopped immediately. In severe cases, the administration of benzodiazepines (in children) or anticholinergic antiparkinsonian drugs (in adults) may be necessary to reduce extrapyramidal disturbances.
To reduce the risk of overdose, the time interval between injections should not be less than 6 hours.
Long-term treatment with metoclopramide may lead to the development of irreversible tardive dyskinesia. In order to prevent this complication, the duration of treatment should not exceed 3 months. When the first symptoms of tardive dyskinesia appear, the administration of metoclopramide should be stopped immediately. When administered in combination with neuroleptics (extremely rarely as monotherapy), metoclopramide can provoke the development of neuroleptic malignant syndrome. In this case, metoclopramide should also be stopped immediately and treatment should be started.
Metoclopramide may increase the manifestations of parkinsonism.
Methemoglobinemia. Although there have been no reports of metoclopramide causing episodes of methemoglobinemia, if it develops (especially in individuals with NADP-cytochrome-b5 deficiency), its use should be discontinued and methylene blue administered.
Cardiovascular pathology. There are isolated cases of cardiovascular failure, severe bradycardia (up to cardiac arrest), and prolongation of the QT interval after intravenous administration of metoclopramide. This should be taken into account when administering metoclopramide intravenously, especially in patients with risk factors (those with QT prolongation, uncompensated electrolyte imbalance, bradycardia and taking concomitant drugs that affect repolarization). To reduce the risk of cardiovascular complications, the dose of metoclopramide should be administered over at least 3 minutes.
The drug contains sodium sulfite as excipients, which in rare cases can provoke severe allergic reactions and bronchospasm.
The solution contains a small amount (less than 1 mmol per dose) of sodium ions, which should be taken into account when administering it to young children.
Features of use in pediatric and geriatric practice
Metoclopramide is contraindicated in children under 1 year of age. Since in children the pharmacodynamics of metoclopramide after oral and intravenous administration is variable and a clear concentration-effect relationship has not been established.
Adolescents and young adults (15–19 years of age), as well as older adults, have an increased risk of extrapyramidal reactions when treated with metoclopramide.
Treatment with metoclopramide for more than 5 days should be avoided unless the therapeutic benefit is considered to outweigh the risk of tardive dyskinesia.
Use during pregnancy and breastfeeding
Contraindicated for use during pregnancy. There is evidence that the use of metoclopramide during pregnancy does not cause congenital disorders or fetotoxic changes. However, its use can only be justified as a last resort, since the development of extrapyramidal syndrome in a child after birth is possible. You should refrain from using metoclopramide in the last weeks of pregnancy, and conduct neonatal monitoring if it is prescribed during pregnancy.
When used during lactation (breastfeeding), it should be taken into account that metoclopramide passes into breast milk. Despite the fact that the level of metoclopramide in milk is low, its effect on the child in this case cannot be excluded. Consideration should be given to stopping breastfeeding if metoclopramide is necessary.
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 due to the risk of developing drowsiness, dizziness, dystonia and dyskinesia, as well as impaired visual reactions.
Interaction with other drugs
Contraindicated combinations. The drug is not prescribed simultaneously with levodopa drugs or dopamine receptor stimulants (antagonism with metoclopramide).
Combinations to avoid. Alcohol enhances the sedative effect of metoclopramide.
Combinations to consider when prescribing metoclopramida. Due to the prokinetic effects of metoclopramide, the absorption of some drugs may be altered.
Anticholinergics and morphine enhance the inhibitory effect of metoclopramide on gastrointestinal motility.
CNS depressants (morphine and its derivatives, tranquilizers, sedatives, antihistamines, antidepressants, barbiturates and clonidine) mutually enhance the effect when used with metoclopramide.
Neuroleptics increase the risk of extrapyramidal disorders. Taking metoclopramide together with antidepressants from the group of serotonin reuptake blockers increases the risk of serotonin syndrome.
Metoclopramide reduces the bioavailability of digoxin, and monitoring of plasma digoxin concentrations is required.
The drug enhances the absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol, cyclosporine (maximum concentration by 46%, effect by 22%, which requires monitoring the concentration of cyclosporine); reduces the absorption of cimetidine.
When administered during the use of mivacuronium and suxamethonium, it can increase the duration of muscle relaxation (due to blockade of cholinesterase). The effect of metoclopramide may be reduced by cholinesterase inhibitors.
Strong CYP2D6 inhibitors (fluoxetine and paroxetine) may increase the effects of metoclopramide (although the clinical significance of this is not yet clear).
Metoclopramide solution is pharmaceutically (physically and chemically) compatible (up to 48 hours) with solutions of cimetidine, mannitol, potassium acetate and potassium phosphate; physically compatible (up to 48 hours) with solutions of ascorbic acid, benztropine mesylate, cytarabine, dexamethasone sodium phosphate, diphenhydramine, doxorubicin, sodium heparin, hydrocortisone sodium phosphate, lidocaine hydrochloride, solutions of multivitamins (if stored in the refrigerator), solutions of B vitamins ascorbic acid.
Metoclopramide solutions are physically compatible for up to 24 hours (do not use if precipitation occurs) with clindamycin phosphate, cyclophosphamide, insulin. Conditionally compatible (use within one hour of mixing or can be infused directly into the same venous line) with ampicillin sodium, cisplatin, erythromycin lactobionate, methotrexate sodium, benzylpenicillin potassium, tetracycline hydrochloride. Incompatible (do not combine) with cephalothin sodium, chloramphenicol sodium, sodium bicarbonate.
Metoclopramide is a white crystalline substance that is almost insoluble in water and odorless. This drug is absorbed quite quickly from the digestive tract after taking the drug orally.
Types of medication, commercial names of analogues, release forms
Metoclopramide can be purchased in the form of tablets or solution, from which intramuscular or intravenous injections are subsequently prepared.Metoclopramide can be bought in pharmacies under other names - Metamol, Ceruglan, Cerucal, Apo-Metoclop, Perinorm, Raglan.
Manufacturers of metoclopramide
| Company manufacturer | Commercial name of the drug | A country | Release form | Dosage |
| NIOPIK SSC | Metoclopramide | Russia | Pills | You should take the tablets immediately before meals. For adults It is prescribed to take 5 – 10 mg once. 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 medication per day. For children over six years old a single dose is 5 mg. Children under six years old prescribed 0.5 - 1 milligram ( no more than 3 times a day). |
| Borisov Pharmaceutical Plant | Metoclopramide | Republic of Belarus | ||
| Update | Metoclopramide | Russia | ||
| North Star | Metoclopramide | Russia | ||
| Chemical and pharmaceutical plant AKRIKHIN | Metoclopramide-ACRI | Russia | ||
| PharmFirma Sotex | Metoclopramide | Russia | Solution for the preparation of intramuscular or intravenous injections. | Injections are usually prescribed for severe nausea and vomiting. Single dosage for adults is 10 milligrams, which should be administered three times a day. Children aged 6 years and older 5 milligrams are administered. Children under six years old Prescribe 0.5 - 1 milligram. The frequency of administration is 1 – 3 times a day. |
| Armavir Biofactory | Metoclopramide | Russia | ||
| Novosibkhimpharm | Metoclopramide | Russia | ||
| Moscow endocrine plant | Metoclopramide | Russia | ||
| Eskom | Metoclopramide-ESKOM |
The mechanism of therapeutic action of the drug
Metoclopramide has antiemetic, antihiccup 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 vomiting center. 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 gastric contractions, relaxing the pyloric sphincter ( orbicularis muscle separating the stomach from the duodenum), increasing gastric emptying and relaxing the duodenum. At the same time, the muscle contractions of the gallbladder are normalized, due to which the outflow of bile is normalized ( eliminates biliary dyskinesia). It is also worth noting that large doses of this antiemetic medication directly affect serotonin receptors, which also has an antiemetic effect ( the gag reflex is suppressed).Metoclopramide is prescribed as an antiemetic in the following cases:
- adverse reactions of certain medications that may cause vomiting ( cytostatics, some antibiotics, morphine, as well as anti-tuberculosis drugs);
- diet violation;
- vomiting during pregnancy;
- radiotherapy in the treatment of malignant tumors;
- vomiting due to traumatic brain injury;
- vomiting due to kidney disease and liver disease;
- uremia ( accumulation of urea in the blood against the background of chronic renal failure).
Metoclopramide can also be used in the treatment of migraine ( part of complex therapy). Metoclopramide also prevents food from stagnating in the stomach and thereby stimulates the absorption of anti-migraine drugs.
Metoclopramide is well absorbed through the mucous membrane of the digestive system and penetrates relatively quickly into the circulatory system. Metoclopramide quite easily crosses the placental barrier and the blood-brain barrier ( can penetrate nerve cells), and may also pass into breast milk. The onset of action of metoclopramide when administered intravenously 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 removal of this medication from the body.
While taking metoclopramide, you should avoid drinking alcohol due to the possibility of various side effects and complications. Also, under the influence of this medication, concentration may decrease, which may affect work that requires quick reactions ( driving a car, as well as working with potentially dangerous production equipment).
For what pathologies is it prescribed?
Metoclopramide can effectively relieve nausea and vomiting of various origins. It can also be prescribed in the treatment of migraines for better absorption of anti-migraine medications.Use of metoclopramide
| Indications for use | Mechanism of action | Dosage |
| Hiccups | 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 part 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 ( pills), and intramuscularly or intravenously ( injections). Tablets are taken a few minutes before meals, 5 to 10 milligrams three times a day. You should take no more than 20 mg at a time, and no more than 60 mg per day. Intravenously for adults administer 10 mg up to three times a day. For children aged six years and older You need to take 5 milligrams one time. Children under six years of age , prescribe 0.5 - 1 milligram. The drug should be used in childhood from one to three times a day. |
| Nausea | ||
| Vomit | ||
| Digestive disorder | ||
| Gastroesophageal reflux
(reflux of food from the stomach into the esophagus) |
||
| Atony and hypotension of the stomach and duodenum
(retention of food in the stomach and duodenum, due to a decrease in muscle tone) |
||
| Flatulence
(bloating due to gas accumulation 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) | Normalizes muscle contractions of the gallbladder, due to which the normal outflow of bile is restored. Eliminates biliary dyskinesia. |
|
| As preparation for diagnostic methods for examining the gastrointestinal tract | The same as for biliary dyskinesia. | Intravenously in an 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 medications in the wall of the mucous membrane of the upper floors of the digestive tract. | The dosage is selected by the doctor. |
How to use the medicine?
Metoclopramide can be prescribed both in the form of intramuscular and intravenous injections, and in the form of regular tablets. Metoclopramide tablets are taken just a few minutes before meals.
Adults should take a single dose of 5–10 mg three times a day. The maximum single dosage is 20 mg, and the maximum daily dosage should not exceed 60 mg.
Children under six are prescribed metoclopramide in a single dosage of 0.5 - 1 milligram, and children over six years of age 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 given one to three times a day.
Children who are already six years old are administered 5 milligrams of the drug, and children under six years old are administered 0.5 - 1 milligram 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 of 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 when taking metoclopramide:
- disorders of the digestive system;
- disorders of the nervous system;
- disorders of the hematopoietic system;
- drug allergies;
- disorders of the endocrine system.
Digestive disorders
Adverse reactions from the digestive system occur most often during long-term use of metoclopramide. Taking this antiemetic medication with other drugs that have hepatotoxicity ( negatively affects liver tissue) may 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.The following disorders of the digestive system are distinguished:
- xerostomia;
Jaundice is a pathological condition characterized by yellow discoloration of the skin and mucous membranes. Jaundice occurs due to a malfunction of the liver, as a result of which the level of bilirubin in the blood and tissues increases significantly ( bile pigment). It is bilirubin that colors the skin and mucous membranes yellow. Jaundice can occur, as a rule, while taking another drug that is toxic to liver tissue ( hepatotoxic effect).
Nervous system disorders
Even a single dose of metoclopramide can cause serious side effects on the nervous system. These reactions are observed most often in children and adolescents, as well as in the elderly. Nervous system disorders occur due to the direct effect of the medication on the nerve cells of the brain.Metoclopramide may cause the following problems:
- fatigue;
- dizziness;
- drowsiness;
- akathisia;
- spasm of the facial muscles;
- hyperkinesis;
- spastic torticollis;
- parkinsonism;
- dyskinesia.
Facial muscle spasm(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 orbicularis oculi muscle. Subsequently, the contractions progress and affect almost the entire half of the face. These clonic or tonic contractions ( in the form of involuntary twitching or significant muscle contractions) may significantly interfere with vision with the eye on the affected side. Also, a spasm of the facial muscles can begin with contractions of the cheek muscles, and then spread upward.
Hyperkinesis are pathological contractions of different muscle groups that occur involuntarily. Hyperkinesis occurs due to damage to nerve cells of different brain structures ( thalamus, subthalamic nuclei, extrapyramidal system, etc.). The intensity and frequency can be reduced by volitional influence, a change in posture, or painful stimulation. It should be noted that during sleep these involuntary contractions completely disappear.
Spasmodic torticollis is a disease in which the normal position of the head is disrupted due to tension in the neck muscles. Painful sensations are less pronounced in the first half of the day and gradually intensify in the evening. Often a stressful situation or physical activity increases 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 maintaining balance when walking ( postural instability), as well as muscle resistance during passive movements. Drug-induced parkinsonism occurs especially often in older people.
Dyskinesia, or tardive dyskinesia, are manifested by involuntary movements of the limbs, which occur against the background of long-term use of medications that can block dopamine receptors. Dyskinesia can manifest itself in the form of tremor, tic ( involuntary elementary and stereotypical movements), akathisia or other manifestations that are often combined. A feature of dyskinesia is the persistence of these symptoms after discontinuation of the drug ( from several months to several years).
Disorders of the hematopoietic system
In rare cases, taking metoclopramide may be accompanied by the occurrence of agranulocytosis. With this pathology in the blood there is a decrease in the number of subtypes 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 causes the human body to become 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 are perceived as a foreign substance ( antigen). Subsequently, the body produces antibodies to them ( special protein molecules), and upon secondary penetration of this drug, the immune system attacks any cell that is associated with the antigen. It is worth noting that agranulocytosis most often occurs only in the first few days after the start of treatment.Drug allergy
In rare cases, taking metoclopramide may cause a skin rash. As a rule, red spots or small blisters appear on various parts of the body, which can cause an unpleasant burning sensation to varying degrees. Urticaria may also occur in some cases. This allergic reaction is characterized by the appearance of fairly large blisters on the skin, which visually resemble blisters from a nettle burn. These blisters have a slightly pinkish tint and rise slightly above the surface of the skin. A rash with urticaria can be either solitary and appear only on one part of the body, or be generalized, covering the torso and limbs.Disorders of the endocrine system
Long-term use of high doses of metoclopramide can negatively affect the endocrine system, causing serious disruption. This is due to the fact that by penetrating the brain the drug can affect the functioning of the higher centers of the endocrine system ( hypothalamus and pituitary gland).Metoclopramide in rare cases can lead to the following adverse reactions:
- galactorrhea;
- menstrual irregularities;
- gynecomastia.
Menstrual irregularities characterized by any 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 - 30 days. As a rule, these disorders are manifested by irregular menstrual cycles, heavy menstruation with blood clots ( menorrhagia) or, conversely, very scanty and spotting vaginal discharge that lasts less than 3 days ( oligomenorrhea). Also, menstrual irregularities are often accompanied by moderate or severe pain in the lower abdomen ( algomenorrhea).
Gynecomastia is a pathological condition in men in which enlargement of the mammary glands occurs due to the proliferation 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). This pathology is characterized by a feeling of heaviness in the chest, fullness and itching. When palpating the mammary gland, a relatively mobile formation with clear boundaries can be detected.
Approximate cost of the medicine
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 slightly different.Average cost of metoclopramide
| City | Average cost of a medicinal substance | |
| Pills | 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 |
Metoclopramide is a medicine used by adults to treat vomiting from a variety of causes. Not everyone knows whether this drug can be given to children, in what situations it is allowed and in what dosage.
Release form
The drug is presented in pharmacies in two forms:
- Tablets, of which there are from 10 to 100 pieces in one pack. They are white or yellowish-white in color and may have some marbling.
- Ampoules for intramuscular or intravenous administration, packaged in 5-20 pieces. Inside the ampoule there is a slightly colored or colorless transparent liquid.
Compound
The effect of the medicine is due to a substance that has the same name as the drug - metoclopramide. It is presented in the form of hydrochloride and is contained in 1 tablet and 1 ampoule in a dosage of 10 mg (in 1 ml of injectable medicine - in an amount of 5 mg).
Among the auxiliary components of tablets from different manufacturers you can see lactose, povidone, talc, Ca stearate and other substances. The ampoules contain sodium chloride, sterile water, sodium sulfite and other compounds.
Operating principle
Metoclopramide affects serotonin and dopamine receptors in the brain, and also reduces the sensitivity of the nerves that conduct impulses from the digestive tract to the vomiting center. This is manifested by suppression of the gag reflex.
In addition, the medicine has the ability, through its influence on the parasympathetic nervous system and hypothalamus, to enhance gastrointestinal motility, due to which it helps get rid of hiccups and nausea.
After taking the drug, the stomach empties faster, but gastric juice is released in normal quantities. Although food moves through the intestines more quickly as a result of the influence of the medication, the use of Metoclopramide does not provoke diarrhea.
The drug also normalizes bile secretion, helping with gallbladder dyskinesia. The drug has the ability to stimulate the healing of ulcerative lesions of the gastrointestinal tract.
The effect of Metoclopramide begins to manifest itself quite quickly - 1-3 minutes after injection into a vein, approximately 10 minutes after an intramuscular injection. The tablets begin to act in 30-60 minutes. The duration of the antiemetic effect of this drug reaches 12 hours.
Indications
The main reason to prescribe Metoclopramide to a child is vomiting.
The reasons for its occurrence are:
- taking medications - for example, antibacterial or cytostatic;
- liver pathology;
- traumatic brain injury;
- eating disorders;
- renal failure;
- radiation therapy.
In addition, the medicine is used:
- with reflux esophagitis;
- with flatulence;
- for peptic ulcers of the stomach and intestines;
- with biliary dyskinesia;
- with postoperative decrease in gastrointestinal motility;
- with Tourette's syndrome;
- for migraines;
- in preparation for probing or x-ray examination of the gastrointestinal tract.
At what age is it allowed to take it?
Children in the first two years of life are not prescribed any form of Metoclopramide. Tablet medicine can be given from the age of 2, but only when indicated and under the supervision of a doctor. Injections are used in the treatment of children 6 years of age and older.
Contraindications
The medicine should not be given to children:
- with hypersensitivity to any of the ingredients of the selected form of Metoclopramide;
- with epilepsy;
- with bleeding in the gastrointestinal tract;
- with glaucoma;
- with intestinal obstruction;
- with pheochromocytoma;
- with renal failure;
- with high blood pressure;
- with extrapyramidal disorders;
- after operations on the gastrointestinal tract;
- with bronchial asthma;
- with pyloric stenosis;
- with a prolactin-dependent tumor;
- with perforation of the wall of the digestive tract;
- with liver failure.
The drug is not prescribed for vomiting caused by motion sickness, since it does not help eliminate vestibular disorders.
Side effects
In some young patients, the use of Metoclopramide may cause drowsiness, fatigue, dry mouth, dizziness, restlessness, changes in blood pressure or heart rate, allergic rash, changes in stool and other negative effects. If they occur, you should immediately show the child to the doctor.
Instructions for use and dosage
The following must be taken into account:
- Metoclopramide tablets are taken 15-30 minutes before meals. The drug is not chewed, but swallowed and washed down with water.
- Injections are given both intramuscularly and into a vein. The method of administration is determined individually.
- The dosage for children 2-6 years old is calculated by weight - it is multiplied by 0.5-1 mg. The daily dose obtained by this calculation is divided into three doses. At this age, medication is given only in tablets.
- For a child over 6 years old, any of the forms of Metoclopramild is prescribed in a single dose of 5 mg (half a tablet or 1 ml of solution) - one to three times a day.
Overdose
Too much of an injection or tablet drug affects the nervous system and can cause confusion, drowsiness, seizures and other symptoms. In case of overdose, you should immediately consult a doctor with your child.
Interaction with other drugs
Treatment with Metoclopramide affects the intake of many medications (sleeping pills, tetracyclines, famotidine, digoxin, antipsychotics, paracetamol, etc.), which the doctor must take into account when prescribing such a medication.
Terms of sale
To purchase any form of Metoclopramide, you must show a prescription from a pediatrician, gastroenterologist or other specialist. The price of the drug is influenced by both the manufacturer and the form of the drug. On average, 50 tablets cost about 30 rubles, and 10 ampoules cost about 50-60 rubles.
