Metoclopramide Injection 10mg/2mL | Antiemetic Prokinetic

Product Description

1. Composition

Each 2 mL ampoule contains 10 mg metoclopramide hydrochloride.

2. Clinical Pharmacology

Metoclopramide hydrochloride is a substituted benzamide with prokinetic and antiemetic properties. It stimulates motility of the upper gastrointestinal tract without altering gastric, biliary or pancreatic secretion, and enhances gastric peristalsis to accelerate gastric emptying. It also increases duodenal peristalsis, thereby shortening intestinal transit time.

The resting tone of the gastro-oesophageal sphincter is increased, and the pyloric sphincter is relaxed. Metoclopramide exerts parasympathomimetic activity and acts as a dopamine antagonist with a direct effect on the chemoreceptor trigger zone. It may also have 5-HT₃serotonin receptor antagonist properties.

3. Pharmacokinetics

Metoclopramide is widely distributed throughout the body, with an apparent volume of distribution of approximately 3.5 L/kg. It readily crosses the blood-brain barrier and the placental barrier; foetal plasma concentrations reach approximately 60–70% of maternal plasma levels.

Concentrations in breast milk may exceed maternal plasma concentrations, particularly in the early puerperium, and decline gradually in the late puerperium.

Elimination is biphasic, with a terminal elimination half-life of 4 to 6 hours. Half-life may be prolonged in patients with renal impairment, resulting in elevated plasma concentrations. Approximately 85% of a dose is excreted in urine within 72 hours: 20–30% as unchanged metoclopramide, and the remainder as sulphate/glucuronide conjugates and metabolites. Around 5% of a dose is eliminated in faeces via bile.

4. Indications

• Disorders of reduced gastrointestinal motility: gastroparesis, functional ileus, gastro-oesophageal reflux disease and dyspepsia
• Nausea and vomiting associated with gastrointestinal disorders, migraine, postoperative state and cancer chemotherapy
• Adjunct to stimulate gastric emptying during radiographic examinations and to facilitate small bowel intubation
• Management of aspiration syndromes

Note: Metoclopramide is not effective for the prevention or treatment of motion sickness.

5. Dosage and Administration

This product may be administered by intramuscular injection or slow intravenous injection.

General dosing principles

• The maximum total daily dose should not exceed 0.5 mg/kg body weight.
• Dosage reduction is recommended in patients with renal impairment, and may be considered in hepatic impairment.
• Adults: 10 mg metoclopramide hydrochloride, 3 times daily.

Paediatric use (restricted indications only)

Use in patients under 20 years of age is restricted to severe intractable vomiting of known cause, chemotherapy/radiotherapy-induced vomiting, gastrointestinal intubation and premedication. Dosing by age and weight:

Age group	Dose	Body weight range
Under 1 year	1 mg twice daily	Up to 10 kg
3 – 5 years	1 mg, 2–3 times daily	10 – 14 kg
5 – 9 years	2.5 mg 3 times daily	20 – 29 kg
9 – 14 years	5 mg 3 times daily	30 kg and over
15 – 19 years	5 mg 3 times daily	30 – 59 kg
15 – 19 years	10 mg 3 times daily	60 kg and over

When body weight falls below the range for a given age group, dosing should be based on body weight rather than age, and a lower dose should be selected.

6. Contraindications

• Conditions where increased gastrointestinal motility may be harmful: gastrointestinal haemorrhage, stricture, perforation, and immediate postoperative status
• Phaeochromocytoma (risk of hypertensive crisis)
• Epilepsy (may increase seizure frequency and severity)
• Hypersensitivity to metoclopramide hydrochloride or any excipient

7. Warnings and Precautions

• Children, young adults and elderly patients are at increased risk of extrapyramidal reactions; use with caution and monitor closely.
• Patients on prolonged therapy should undergo regular clinical review.
• Use with caution in renal impairment, hepatic impairment and conditions predisposing to fluid retention.
• Use with caution in patients with a history of depression.
• Metoclopramide may cause drowsiness and impaired reaction speed. Patients affected should not drive or operate machinery.

8. Adverse Reactions

• Extrapyramidal symptoms: Acute dystonic reactions are the most characteristic adverse effect, with higher incidence in young patients (especially females). Risk is reduced by keeping the daily dose below 500 µg/kg. Parkinsonism and tardive dyskinesia may occur rarely, typically with long-term use in elderly patients.
• Nervous system: Restlessness, drowsiness, dizziness, headache; rarely neuroleptic malignant syndrome, seizures.
• Gastrointestinal: Diarrhoea, bowel disturbances.
• Cardiovascular: Hypotension, hypertension; rare reports of cardiac conduction disorders, particularly with concomitant cardioactive medications.
• Endocrine: Transient elevation of plasma aldosterone; galactorrhoea and related menstrual disorders may occur due to increased prolactin levels.
• Other: Isolated reports of blood dyscrasias, hypersensitivity reactions, urinary incontinence.

9. Drug Interactions

• Extrapyramidal risk: Concomitant use with phenothiazines and other drugs that cause extrapyramidal reactions increases the risk of acute dystonia.
• CNS-active drugs: Increased toxicity may occur with lithium, antidepressants, antiepileptics and sympathomimetics; monitor closely.
• Antagonism of prokinetic effect: Antimuscarinics and opioid analgesics counteract the gastrointestinal prokinetic effects of metoclopramide.
• Altered drug absorption: Metoclopramide may reduce gastric absorption of drugs such as digoxin, and increase intestinal absorption of drugs such as aspirin and paracetamol.
• Neuromuscular blockade: Metoclopramide inhibits serum cholinesterase and may prolong suxamethonium-induced neuromuscular blockade.
• Prolactin interaction: Metoclopramide raises serum prolactin levels and may reduce the efficacy of hypoprolactinaemic agents such as bromocriptine.
• MAOIs: Concomitant use with monoamine oxidase inhibitors is not recommended.

10. Overdosage and Treatment

Overdosage may cause severe extrapyramidal symptoms and other serious adverse reactions. Management is symptomatic and supportive. Extrapyramidal symptoms may be treated with anticholinergic or antihistamine agents under medical supervision.

11. Storage Instructions

Store in a cool, dry place below(25°C / 77°F) . Protect from light. Keep this medicine out of the reach of children.

12. Pack Information

Available in packs containing 10 ampoules of 2 mL per box.