SW Metoclopramide

Tablet: Round, white, convex, plain tablet with single score on one side only.
Each tablet contains 10 mg Metoclopramide HCl equivalent to anhydrous Metoclopramide HCl.
Syrup: A clear, yellow syrup with banana flavour.
Each 5 mL contains 5 mg Metoclopramide HCl equivalent to anhydrous Metoclopramide HCl.

Pharmacology: Metoclopramide increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and duodenal bulb, and increases peristalsis of the duodenum and jejunum, resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder. Like the phenothiazines and related drugs, which are also dopamine antagonists, metoclopramide produces sedation and may produce extrapyramidal reactions, although comparatively rare. Metoclopramide inhibits the central and peripheral effects of apomorphine, induces release of prolactin, and causes a transient increase in circulating aldosterone levels, which may be associated with transient fluid retention. The onset of pharmacological action of metoclopramide is 30 to 60 minutes following an oral dose; pharmacological effects persist for 1 to 2 hours. Approximately 85% of the radioactivity of an orally administered radioactive dose appears in the urine within 72 hours. Of the 85% eliminated in the urine, about half is present as free or conjugated metoclopramide.

Adult population: Metoclopramide is indicated in adults for: Prevention of delayed chemotherapy induced nausea and vomiting (CINV).
Prevention of radiotherapy induced nausea and vomiting (RINV).
Symptomatic treatment of nausea and vomiting, including acute migraine induced nausea and vomiting.
Paediatric population: Metoclopramide is indicated in children (aged 1-18 years) for: Prevention of delayed chemotherapy induced nausea and vomiting (CINV) as a second line option.

Adults: The recommended single dose is 10 mg, repeated up to three times daily.
The maximum recommended daily dose is 30 mg or 0.5 mg/kg body weight.
The maximum recommended treatment duration is 5 days.
Prevention of delayed chemotherapy induced nausea and vomiting (CINV) (paediatric patients aged 1-18 years): The recommended dose is 0.1 to 0.15 mg/kg body weight, repeated up to three times daily by oral route. The maximum dose in 24 hours is 0.5 mg/kg body weight.
Dosing table: (See table.)

Click on icon to see table/diagram/image

The maximum treatment duration is 5 days for prevention of delayed chemotherapy induced nausea and vomiting (CINV).
Tablet is not suitable for use in children weighing less than 30 kg. Other pharmaceutical forms may be more appropriate for administration to this population.
Frequency of administration: A minimum interval of 6 hours between two administrations is to be respected, even if vomiting or rejection of the dose occurs.
Special population: Elderly: In elderly patients, a dose reduction should be considered, based on renal and hepatic function and overall frailty.
Renal impairment: In patients with end stage renal disease (Creatinine clearance ≤15 ml/min), the daily dose should be reduced by 75%.
In patients with moderate to severe renal impairment (Creatinine clearance 15-60 ml/min), the dose should be reduced by 50%.
Hepatic impairment: In patients with severe hepatic impairment, the dose should be reduced by 50%.

Symptoms and Treatment for overdosage and antidote(s): Symptoms of overdosage may include drowsiness, disorientation, and extrapyramidal reactions. Anticholinergic or antiparkinson drugs or antihistamines with anticholinergic properties may be helpful in controlling the extrapyramidal reactions. Symptoms are self-timing and usually disappear within 24 hours.

Hypersensitivity to the active substance or to any of the excipients listed.
Gastrointestinal hemorrhage, mechanical obstruction, or gastrointestinal perforation for which the stimulation of gastrointestinal motility constitutes a risk.
Confirmed or suspected pheochromocytoma, due to the risk of severe hypertension episodes.
History of neuroleptic or metoclopramide-induced tardive dyskinesia.
Epilepsy (increased crises frequency and intensity).
Parkinson's disease.
Combination with levodopa or dopaminergic agonists.
Known history of methaemoglobinaemia with metoclopramide or of NADH cytochrome-b5 deficiency.
Use in children less than 1 year of age.

Neurological disorders: Extrapyramidal disorders may occur, particularly in children and young adults, and/or when high doses are used. These reactions generally occur at the beginning of treatment, and can occur after single dose. If extrapyramidal symptoms occur, metoclopramide should be discontinued immediately. These effects are generally completely reversible after treatment discontinuation; however, symptomatic treatment may be required (benzodiazepines in children, and/or anticholinergic antiparkinsonian medicinal products in adults).
An interval of at least six hours should be respected between each dose, even if vomiting or rejection of the dose occurs, in order to avoid overdose. Long-term treatment with metoclopramide may cause potentially irreversible tardive dyskinesia, particularly in elderly subjects. Treatment should not exceed 3 months because of the risk of tardive dyskinesia. Treatment must be discontinued if clinical signs of tardive dyskinesia occur.
Neuroleptic malignant syndrome has been described with metoclopramide in combination with neuroleptics and with metoclopramide monotherapy. Metoclopramide must be immediately discontinued if symptoms of neuroleptic malignant syndrome develop, and appropriate treatment should be initiated.
Particular caution should be exercised in patients with underlying neurological disorders, and in patients receiving other centrally-acting drugs. Symptoms of Parkinson's disease may also be exacerbated by metoclopramide.
Methemoglobinemia: Methemoglobinemia, which could be related to NADH-cytochrome-b5 reductase deficiency, has been reported. If this occurs, treatment must be immediately and permanently discontinued, and appropriate measures initiated (such as treatment with methylene blue).
Cardiac disorders: Serious cardiovascular undesirable effects, including cases of severe bradycardia, circulatory collapse, cardiac arrest, and QT prolongation, have been reported during administration of metoclopramide by injection, particularly via the intravenous route.
Particular caution should be exercised when administering metoclopramide, particularly via the intravenous route, in elderly subjects, patients with cardiac conduction disorders (including QT prolongation), patients with electrolyte imbalance, bradycardia, and patients taking other drugs known to prolong QT interval. The intravenous injection must be given as slow bolus (of at least 3 minutes duration) in order to reduce the risk of undesirable effects (e.g. hypotension, akathisia).
Kidney or liver failure: In patients with kidney failure or severe liver failure, a dose reduction is recommended.
Avoid doses exceeding 0.5 mg/kg/day.
Extrapyramidal effects, especially dystonic reaction of metoclopramide, are more likely to occur in children shortly after initiation of therapy, and usually with doses higher than 0.5 mg per kg of body weight per day.
Effects on ability to drive and use machines: Not known.

As there are no adequate and well-controlled studies in pregnant women, this drug should be used during pregnancy only if clearly needed.
Metoclopramide is excreted in human milk. Caution should be exercised when metoclopramide is administered to a nursing mother.

The most frequent adverse reactions of metoclopramide are restlessness, drowsiness, fatigue and lassitude that occur in approximately 10% of patients. Less frequently, insomia, headache, dizziness, nausea, bowel disturbance or extrapyramidal symptoms may occur. Rarely depression and persistent dyskinesia have been reported.
A single instance of supraventricular tachycardia following intramuscular administration has been reported.

The effect of metoclopramide on gastrointestinal motility is antagonised by anticholinergic drugs and narcotic analgesics. Additive sedative effect can occur when metoclopramide is given with alcohol, sedatives, hypnotics, narcotics or tranquilizers.
The finding that metoclopramide releases catecholamines in patients with essential hypertension suggests that it should be used cautiously, if at all, in patients receiving monoamine oxidase inhibitors. Absorption of drugs from the stomach may be diminished (e.g. digoxin) by metoclopramide, whereas the rate and/or extent of absorption of drugs from the small bowel may be increased (e.g. acetaminophen, tetracycline, levodopa, ethanol, cyclosporine).

Incompatibilities: It is not compatible with cephalothin sodium, chloramphenicol sodium, and sodium bicarbonate.

Store at or below 30°C. Protect from light.
Shelf-life: Tablet: 5 years.
Syrup: 3 years.

Antiemetics

A03FA01 - metoclopramide ; Belongs to the class of propulsives. Used in the treatment of functional gastrointestinal disorders.

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