Metoclopramide, tablets 10 mg 56 pcs

Pharmacodynamics

Antiemetic, is a specific blocker of dopamine (D2) and serotonin receptors. It has antiemetic effect, eliminates nausea and hiccups. It reduces esophageal motility, increases the tone of the lower esophageal sphincter, accelerates gastric emptying, and also accelerates the movement of food through the small intestine without causing diarrhea. Normalizes the secretion of bile, reduces spasm of the sphincter of Oddi, eliminates gall bladder dyskinesia. It stimulates the secretion of prolactin.

Pharmacokinetics

Fast absorption from the gastrointestinal tract. Bioavailability is 60-80%. Time of maximum concentration achievement in blood plasma is 1-2 hours. The elimination half-life is 3 to 5 hours, with impaired renal function up to 14 hours. The drug is eliminated mainly by the kidneys within 24 hours in unchanged form and as conjugates. Passes through the placental and blood-brain barrier, passes into the mother’s milk.

Indications

Gastric and 12 duodenal ulcer, Hiccups, Gastritis, Biliary dyskinesia, Reflux esophagitis, Gastroduodenitis, Vomiting, Meteorism, Nausea

• gastric and intestinal atony and hypotension (particularly postoperative);
• dyskinesia of the biliary tract;
• reflux esophagitis, flatulence, exacerbation of gastric and duodenal ulcer (as a part of complex therapy);
• when performing X-ray contrast studies of the gastrointestinal tract (to increase peristalsis).

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Active ingredient

Metoclopramide

Composition

One tablet:
Metoclopramide hydrochloride monohydrate – 0.0105 g
(in terms of anhydrous) – 0.0100 g
Excipients:
lactose monohydrate (milk sugar) – 0.0660 g
potato starch – 0.0200 g
calcium stearate – 0.0010 g
povidone-K30 – 0.0020 g
colloidal silica (aerosil) – 0.0005 g

How to take, the dosage

Inside. Adults: 10 mg 3-4 times daily 30 min before a meal, the tablet should be swallowed in whole with small amount of water. The maximum single dose is 20 mg, the daily dose is 60 mg.

Interaction

When concomitant use of Metoclopramide with some drugs the following effects may occur: Ethanol: increased effect on the central nervous system; Cholinesterase inhibitors: weakening of metoclopramide action; Sleeping pills: increased sedative effect; H2-histamine receptor blockers: increased effectiveness of therapy; Diazepam, tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol: increased absorption; Digoxin, cimetidine: delayed absorption; Neuroleptics: increased risk of extrapyramidal symptoms.

Consult a physician before concomitant use of Metoclopramide with other medicinal agents.

Special Instructions

During the treatment it is not recommended to use ethanol.

If necessary, treatment with central cholinoblockers and other antiparkinsonian drugs is carried out.

In elderly patients taking the drug, development of tardive dyskinesia is possible. The risk of tardive dyskinesia depends on the duration of the course of pharmacotherapy and the total dose of the drug. Irreversible changes usually develop if the drug is prescribed for more than 12 weeks.

It is not recommended to prescribe the drug for more than 12 weeks, except in cases where the benefits of long-term use of the drug exceed the potential risks of adverse reactions. When prescribing the drug in a short course and in low doses the development of tardive dyskinesia is also possible, but these changes usually disappear some time after discontinuation of the drug.

Ability to influence the reaction rate when driving motor transport or operating other mechanisms
During the treatment, caution should be exercised when driving vehicles and engaging in other activities that require high concentration and rapid psychomotor reactions.

Contraindications

Hypersensitivity, gastrointestinal bleeding, gastric pylorus stenosis, mechanical intestinal obstruction, perforation of the stomach or intestinal wall, pheochromocytoma, extrapyramidal disorders, epilepsy, prolactin-dependent tumors, pregnancy, lactation, children under 18 years.

With caution
Bronchial asthma, arterial hypertension, Parkinson’s disease, renal and/or hepatic failure, advanced age.

Side effects

Cardiovascular system: atrioventricular block;

Central nervous system: Extrapyramidal disorders – trismus, facial muscle spasm, spastic torticollis, bulbar speech type, rhythmic tongue protrusion, extraocular muscle spasm (including oculogyric crisis), muscle opisthotonus, hypertonus; parkinsonism (muscle rigidity, hyperkinesis – manifestation of dopamine-blocking action, the risk of development in children increases when the dose of 0.5 mg/kg per day is exceeded), dyskinesia (in chronic renal failure and elderly patients), depression, headache, drowsiness, anxiety, fatigue, confusion, tinnitus;

Endocrine system: rarely (with prolonged therapy in high doses) – galactorrhea, gynecomastia, menstrual disorders;

Digestive system: diarrhea, constipation; rarely – dry mouth;

Hematopoietic system: Leukopenia, neutropenia, sulfhemoglobinemia in adults;

Metabolism: porphyria;

Allergic reactions: Angioneurotic edema, bronchospasm, urticaria;

Other: at the beginning of treatment – agranulocytosis; rarely (when using high doses) – nasal mucosal hyperemia.

In case of the above symptoms, their worsening or other side effects should be seen by a physician.

Overdose

Symptoms: drowsiness, confusion, irritability, restlessness, seizures, extrapyramidal motor disorders, cardiovascular dysfunction with bradycardia and decreased or increased blood pressure. In mild forms of poisoning, symptoms disappear within 24 hours after withdrawal of the drug. Depending on the severity of the symptoms, it is recommended to establish monitoring of the patient’s vital functions. Fatal cases of poisoning in overdose have not been identified.

Treatment: symptomatic. Extrapyramidal disorders are eliminated by slow administration of biperiden in dose for adults 2.5-5 mg (biperiden is administered only under hospital conditions, under medical supervision). Diazepam may be used to sedate the patient. If large doses of metoclopramide are ingested, gastric lavage, activated charcoal and sodium sulfate are used.

Pregnancy use

The drug is contraindicated in the first trimester of pregnancy. In II and III trimesters the drug is used only in cases of extreme necessity when the potential benefit to the mother exceeds the possible risk to the fetus.
If it is necessary to use the drug during lactation, breastfeeding should be stopped for the duration of treatment.

Similarities

Cerucal, Metoclopramide