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Active ingredients
Metoclopramide
Release form
Pills
Composition
1 tablet contains: Active substance: metoclopramide hydrochloride monohydrate 10.54 mg, incl. metoclopramide hydrochloride 10 mg. Auxiliary substances: potato starch, lactose monohydrate, gelatin, magnesium stearate, silica precipitated.
Pharmacological effect
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 contents into the esophagus by increasing the pressure of the esophageal sphincter 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.
Pharmacokinetics
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.
Indications
Prevention of postoperative nausea and vomiting. Symptomatic treatment of nausea and vomiting, including acute migraine. Prevention of nausea and vomiting caused by radiation therapy and chemotherapy.
Contraindications
Hypersensitivity to metoclopramide and components of the drug, gastrointestinal bleeding, mechanical intestinal obstruction or perforation of the stomach wall and intestines, conditions in which stimulation of gastrointestinal motility is a risk, confirmed or suspected pheochromocytoma due to the risk of developing severe arterial hypertheis, late dyskinesia,which developed after treatment with neuroleptics or metoclopramide in history; epilepsy tumor, lactase deficiency, lactose intolerance, glucose-galactose malabsorption, children under 15 years of age, breastfeeding period.
Precautionary measures
It is used with caution in patients with bronchial asthma, arterial hypertension, impaired liver and / or kidney function, in Parkinson’s disease.
Use during pregnancy and lactation
It is contraindicated for use during pregnancy. When used during lactation (breastfeeding), it should be taken into account that metoclopramide penetrates into breast milk. In experimental studies, no adverse effect of metoclopramide on the fetus has been established.
Dosage and administration
Inside Adults and children over 15 years old with a body weight of more than 60 kg. The recommended dose is 1 tablet (10 mg) up to three times per day. The maximum recommended daily dose is 30 mg or 0.5 mg / kg body weight. Children starting 15 years old with a body weight less than 60 kg The recommended dose is 1/2 tablet (5 mg) 1-3 times a day. The maximum recommended daily dose is 0.5 mg / kg / day. In order to avoid overdosing, it is necessary to observe a minimum interval between doses of 6 hours, even in case of vomiting. The maximum duration of treatment is 5 days. Elderly Patients Elderly patients may require a dose reduction depending on the indicators of renal and liver function and general condition. Renal failure In patients with end-stage renal disease (creatinine clearance less than 15 ml / min), the daily dose should be reduced by 75%. In patients with moderate to severe renal failure (CC 15-60 ml / min), the dose should be reduced by 50%. Hepatic function impairment In severely severe liver failure patients, the dose should be reduced by 50%.
Side effects
The frequency of adverse reactions is classified as follows: very often (≥1 / 10), often (≥1 / 100 - <1/10), infrequently (≥1 / 1000 - <1/100), rarely (≥1 / 10000 - < 1/1000), very rarely (<1/10000), frequency unknown (cannot be estimated based on available data).On the part of the blood and lymphatic system: the frequency is unknown - methemoglobinemia, probably associated with a 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), leukopenia, neutropenia, agranulocytosis. From the side of the heart: rarely bradycardia: the frequency is unknown cardiac arrest, which can be caused by bradycardia, atrioventricular block, sinus node block, lengthening of the QT interval on the electrocardiogram, arrhythmia type "pirouette". On the part of the vessels: often - lowering blood pressure; frequency is unknown - cardiogenic shock, acute increase in blood pressure in patients with pheochromocytoma. From the endocrine system *: infrequently - amenorrhea, hyperirolactinemia: rarely - galactorrhea; frequency unknown - gynecomastia. * Endocrine disorders during prolonged treatment are associated with hyperprolactinemia (amenorrhea, galactorrhea, gynecomastia). On the part of the gastrointestinal tract: often - nausea, diarrhea, constipation. On the part of the kidneys and urinary tract: the frequency is unknown - polyuria, urinary incontinence. Genital and mammary gland organs: unknown frequency, sexual dysfunction, priapism. On the part of the immune system: infrequently - hypersensitivity; frequency is unknown - anaphylactic reactions (including anaphylactic shock), allergic reactions (urticaria, maculopapular rash). On the part of the nervous system: very often - drowsiness; often - asthenia, 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 - dystopia, dyskinesia. disturbance of consciousness: rarely - seizures, especially in patients with epilepsy; frequency unknown - tardive dyskinesia. sometimes persistent, during or after long-term treatment, especially in elderly patients, neuroleptic malignant syndrome. Disturbance of mind: often - depression; infrequently - hallucinations; confusion rarely. The adverse reactions most frequently encountered with high doses of the drug — Extrapyramidal symptoms: acute dystonia and dyskinesia, parkinsonism syndrome, akatizia developed even after the use of a single dose of the drug, especially in children and young patients (see the Special Instructions section).- Drowsiness, decreased level of consciousness, confusion, hallucinations.
Interaction with other drugs
With simultaneous use with anticholinergic agents, mutual weakening of effects is possible. With simultaneous use with neuroleptics (especially the phenothiazine series and butyrophenone derivatives), the risk of extrapyramidal reactions increases. With simultaneous use, the absorption of acetylsalicylic acid, paracetamol, ethanol is enhanced. diazepam absorption and increases its maximum concentration in the blood plasma. When used simultaneously with slow growth oryayuscheysya dosage form may decrease digoxin serum concentrations of digoxin 1/3. With simultaneous use with digoxin in a liquid dosage form or in the form of an instant dissolving dosage form, the interaction is not observed. With simultaneous use with zopiclone, the absorption of zopiclone is accelerated; with cabergoline - may decrease the effectiveness of cabergoline; with ketoprofen - decreases the bioavailability of ketoprofen. Due to antagonism against dopamine receptors, metoclopramide may reduce the anti-Parkinsonian effect of levodopa, while increasing the bioavailability of levodopa due to acceleration of its evacuation from the stomach under the influence of metoclopramide. The results of the interaction are ambiguous. When used simultaneously with mexiletin, absorption of mexiletin is accelerated; mefloquine - increases the absorption rate of mefloquine and its concentration in the blood plasma, while reducing its side effects. When used simultaneously with morphine, morphine absorption is accelerated when taken orally and its sedative effect increases. When applied simultaneously with nitrofurantoin, the absorption of nitrofurantoin decreases. metoclopramide immediately before the administration of propofol or thiopental may require a decrease in their induction doses. In patients receiving metoclopramide, vayutsya and are prolonged effects of suxamethonium hlorida.Pri simultaneous use of tolterodine decreases the effectiveness of metoclopramide; with fluvoxamine - described the case of the development of extrapyramidal disorders; with fluoxetine - there is a risk of extrapyramidal disorders; with cyclosporine - increases the absorption of cyclosporine and increases its concentration in the blood plasma.
special instructions
With extreme caution should be used in children, especially young children, because they have a significantly higher risk of dyskinetic syndrome. Metoclopramide in some cases can be effective with vomiting caused by taking cytotoxic drugs. When used in elderly patients, it must be borne in mind that with prolonged use of metoclopramide in high or medium doses, extrapyramidal disorders, especially parkinsonism and tardive dyskinesia, are the most frequent side effects. background of the use of metoclopramide may be distorted data of laboratory parameters of liver function and determine the concentration of aldosterone and prolactin in the blood plasma. on the ability to drive vehicles and management mehanizmamiV treatment period potentially hazardous should avoid activities that require attention, rapid psychomotor reactions.