Metoclopramide Tablets is an antiemetic drug used for vomiting of various origins. The drug also eliminates nausea and hiccups, regulates the function of the gastrointestinal tract: it enhances its motility (physical activity). Gastric emptying is accelerated, while the secretory function of the stomach (secretion of gastric juice) does not change. Food promotion through the small intestine is accelerated, but diarrhea does not occur. Normalization of bile is normalized, dyskinesia of the gallbladder is eliminated. Metoclopramide contributes to the healing of ulcers in the duodenum and stomach. The drug has a stimulating effect on the production of prolactin (anterior pituitary hormone hormone with a diverse effect on the body).
Active ingredient: metoclopramide hydrochloride - 10 mg. Excipients: lactose - 50.0 mg, potato starch - 37.9 mg, povidone - 1.9 mg, magnesium stearate - 0.2 mg.
Antiemetic, helps reduce nausea, hiccups; stimulates gastrointestinal peristalsis. An antiemetic effect due to blockade of dopamine D2 receptors and an increase in the threshold of chemoreceptors of the trigger zone, is a blocker of serotonin receptors. Metoclopramide is believed to inhibit the relaxation of the smooth muscles of the stomach caused by dopamine, thus enhancing the cholinergic reactions of the smooth muscles of the gastrointestinal tract. It contributes to the acceleration of gastric emptying by preventing the relaxation of the body of the stomach and increasing the activity of the antrum and the upper small intestine. It reduces the reflux of the contents into the esophagus by increasing the pressure of the sphincter of the esophagus at rest and increases the clearance of acid from the esophagus due to an increase in the amplitude of its peristaltic contractions. Metoclopramide stimulates the secretion of prolactin and causes a transient increase in the level of circulating aldosterone, which may be accompanied by short-term fluid retention.
After ingestion is rapidly absorbed from the gastrointestinal tract. Plasma protein binding is about 30%. Biotransforming in the liver.It is excreted mainly by the kidneys both in unchanged form and in the form of metabolites. T1 / 2 is from 4 to 6 h.
Adults: prevention of delayed nausea and vomiting caused by chemotherapy. Prevention of nausea and vomiting caused by radiation therapy. Symptomatic treatment of nausea and vomiting, including acute migraine. Metoclopramide can be used in combination with oral analgesics to improve the absorption of analgesics in acute migraine. Adolescents 15-18 years of age: prevention of delayed nausea and vomiting caused by chemotherapy - as a second-line therapy.
Bleeding from the gastrointestinal tract, mechanical intestinal obstruction, perforation of the stomach or intestines, pheochromocytoma, extrapyramidal disorders, epilepsy, prolactino-dependent tumors, glaucoma, pregnancy, lactation, simultaneous use of anticholinergic drugs, increased sensitivity to metoclopramide.
Before use, consult with your doctor.
Use during pregnancy and lactation
Metoclopramide is contraindicated in the third trimester of pregnancy due to the risk of extrapyramidal disorders in newborns. When using metoclopramide in pregnant women should be monitored for newborns. Metoclopramide is excreted in breast milk. The use of metoclopramide during lactation is not recommended, if necessary, use of the drug should stop breastfeeding.
Dosage and administration
Inside for 30 minutes before a meal, washed down with a small amount of water. Adults: The recommended single dose is 10 mg up to 3 times per day. The maximum daily dose is 30 mg. Adolescents 15-18 years: 10 mg up to 3 times per day. The maximum daily dose is 30 mg. Tablets are not prescribed to adolescents weighing less than 61 kg. The maximum duration of treatment is 5 days. The 6-hour interval between taking the drug should be observed, even in the event of vomiting or if the dose has not been absorbed. Specific patient groups Elderly patients: Consider reducing the dose, taking into account the function of the kidneys and liver, as well as the general condition of the patient. Impaired renal function: in patients with end-stage renal disease (creatinine clearance ≤ 15 ml / min), the daily dose should be reduced by 75%. In patients with moderate or severe renal impairment (creatinine clearance 15-60 ml / min), the dose should be reduced by half.Abnormal liver function: in patients with severely impaired liver function, the dose should be reduced by half.
The frequency of adverse reactions is given in accordance with the classification: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000 , <1/1000), very rarely (<1/10000), the frequency is unknown (the frequency cannot be estimated based on the available data). Blood and lymphatic system disorders: frequency unknown - methemoglobinemia, probably due to deficiency of the enzyme NADH-dependent cytochrome b5 reductase (especially in newborns), sulfhemoglobinemia (most often with simultaneous use of high doses of sulfur-containing drugs). Cardiac disorders: infrequently - bradycardia, frequency unknown - cardiac arrest, which may be caused by bradycardia, atrioventricular block, sinus node block, prolongation of QT interval on the electrocardiogram, “pirouette” type arrhythmia. Vascular disorders: often - lowering of blood pressure, frequency unknown - cardiogenic shock, acute increase in blood pressure in patients with pheochromocytoma. Disorders of the endocrine system: rarely - amenorrhea, hyperprolactinemia, rarely - galactorrhea, the frequency is unknown - gynecomastia. * Endocrine disorders during prolonged treatment are associated with hyperprolactinemia (amenorrhea, galactorrhea, gynecomastia). Disorders of the gastrointestinal tract: often - diarrhea, rarely - dry mouth. Immune system disorders: infrequently - hypersensitivity reactions, frequency unknown - anaphylactic reactions (including anaphylactic shock). Nervous system disorders: very often - drowsiness, often - extrapyramidal disorders (especially in children and young patients and / or when the recommended doses of the drug are exceeded, even after a single injection), parkinsonism, akathisia, infrequently - dystonia, dyskinesia, impaired consciousness, rarely - convulsions, especially in patients with epilepsy, the frequency is unknown - tardive dyskinesia, sometimes persistent, during or after long-term treatment, especially in elderly patients, is a malignant neuroleptic syndrome. Mental disorders: often - depression, rarely - hallucinations, rarely - confusion. General disorders and disorders at the injection site: often asthenia.Adverse reactions that are most common when using high doses of the drug: extrapyramidal symptoms (acute dystonia and dyskinesia, Parkinson's syndrome, akathisia developed even after using a single dose of the drug, especially in children and young patients), drowsiness, decreased level of consciousness, confusion, hallucinations .
Symptoms: extrapyramidal disorders, drowsiness, decreased consciousness, confusion, hallucinations, cardiac arrest and respiration. Treatment: In the case of extrapyramidal symptoms caused by overdose or for other reasons, the treatment is purely symptomatic (benzodiazepines in children and / or anticholinergic antiparkinsonian drugs in adults). Requires symptomatic treatment and constant monitoring of cardiac and respiratory function, depending on the clinical condition of the patient.
Interaction with other drugs
Contraindicated combinations: the simultaneous use of metoclopramide with levodopa or dopamine receptor antagonists is contraindicated in connection with the existing mutual antagonism. Combinations to be avoided: alcohol increases the sedative effect of metoclopramide. Combinations that should be taken into account: in connection with the prokinetic effect of metoclopramid. may be violated. M-holinoblokatory and morphine derivatives have mutual antagonism with metoclopramide in relation to the effects on the motility of the gastrointestinal tract. Medications that inhibit the central nervous system (morphine derivatives, tranquilizers, H1-histamine receptor blockers, antidepressants with a sedative effect, barbiturates, clonidine, and other drugs of these groups) may increase the sedative effect under the influence of metoclopramide. Metoclopramide enhances the effects of neuroleptics on extrapyramidal symptoms. The use of metoclopramide with serotonergic drugs, for example, with selective serotonin reuptake inhibitors, increases the risk of developing serotonin syndrome (serotonin intoxication). Metoclopramide reduces digoxin bioavailability. The concentration of digoxin in the blood plasma should be monitored.Metoclopramide increases the bioavailability of cyclosporine (Cmax by 46% and exposure by 22%). It is necessary to regularly monitor the concentration of cyclosporine in the blood plasma. The clinical implications of this interaction have not been established. With the simultaneous appointment of metoclopramide with suxametonium, the duration of neuro-muscular blockade may increase (due to inhibition of plasma cholinesterase). Exposure of metoclopramide increases with simultaneous use with potent inhibitors of the CYP2D6 isoenzyme, for example, fluoxetine and paroxetine. Although the clinical significance of this interaction has not been established, it is necessary to monitor the occurrence of adverse reactions in patients. Metoclopramide increases the absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, slows down the absorption of cimetidine. Simultaneous use with drugs that have a central stimulating effect (for example, monoamine oxidase inhibitors and sympathomimetics) may change their effect, which may require adjustments dosages.
Contraindications Hypersensitivity to metoclopramide or other components of the drug, gastrointestinal bleeding, mechanical intestinal obstruction, perforation of the stomach wall or intestine, a condition in which stimulation of gastrointestinal motility is a risk confirmed or suspected pheochromocytoma due to the risk of developing severe arterial hypertension , epilepsy (an increase in the frequency and severity of seizures), Parkinson's disease, tardive dyskinesia that developed after treatment neurolepticism lactase, children up to 15 years. With care - old age, renal / hepatic failure, bronchial asthma, impaired cardiac conduction (including prolongation of the QT interval), impaired water and electrolyte balance, bradycardia,simultaneous use of other drugs that prolong the QT interval, arterial hypertension, concomitant neurological diseases, simultaneous use of drugs affecting the central nervous system, depression (history), pregnancy (I, II trimester). Not effective in vomiting of vestibular genesis. Not prescribed after operations on the gastrointestinal tract (like pyloroplasty or intestinal anastomosis), since vigorous muscle contractions prevent healing. The use of metoclopramide may lead to distortions in these laboratory parameters of liver function and determine the concentration of aldosterone and prolactin in plasma. With the appointment of metoclopramide, often in high doses, extrapyramidal disorders may develop, especially in children and young patients, even after the administration of a single dose. Caution must be exercised when used in patients with concomitant neurological diseases and in patients taking drugs affecting the central nervous system. Symptoms of Parkinson's disease may also be noted when using the drug. Cases of methemoglobinemia have been reported, which could be caused by a deficiency of the enzyme NADH-dependent cytochrome b5 reductase. In this case, the drug should be promptly terminated and appropriate measures taken. Cases of severe cardiovascular side effects have been reported, including vascular insufficiency, marked bradycardia, cardiac arrest and prolongation of the QT interval after administration of metoclopramide. Special care should be taken when prescribing intravenously to patients with “weak sinus” syndrome or other impairments of cardiac muscle conduction (including lengthening of the QT interval), elderly patients, patients with electrolyte imbalance, bradycardia, as well as when taking drugs that lengthen the QT interval. Most side effects occur within 36 hours of starting treatment and disappear within 24 hours after withdrawal. The course of treatment should be as short as possible. During the period of drug treatment is not recommended alcohol. Effect on ability to concentrate: when taking the drug, you should avoid potentially dangerous activities that require increased attention, quick mental and motor responses (driving, etc.) due to the possible development of such side effects as dizziness, drowsiness, dyskinesia, dystonia.