Metoclopramide: Rapid Relief from Nausea and Gastroparesis
Metoclopramide is a dopamine antagonist and prokinetic agent widely utilized in clinical practice for the management of gastrointestinal motility disorders and chemotherapy-induced nausea and vomiting. Its mechanism of action involves antagonism of dopamine D2 receptors in the chemoreceptor trigger zone and enhancement of acetylcholine release in the myenteric plexus, leading to accelerated gastric emptying and improved upper GI tract coordination. This product card provides a comprehensive, evidence-based overview of metoclopramide for healthcare professionals, detailing its pharmacological profile, therapeutic applications, and essential safety information to support informed clinical decision-making.
Features
- Active ingredient: Metoclopramide hydrochloride
- Pharmacologic class: Dopamine D2 receptor antagonist, prokinetic agent
- Available formulations: Oral tablets (5 mg, 10 mg), orally disintegrating tablets, oral solution, injectable solution (5 mg/mL)
- Bioavailability: Approximately 80% orally, with rapid absorption
- Half-life: 5–6 hours in individuals with normal renal function
- Metabolism: Hepatic, primarily via CYP2D6 and glucuronidation
- Excretion: Renal (approximately 85%)
Benefits
- Accelerates gastric emptying and enhances coordination of antroduodenal motility, providing relief from gastroparesis symptoms such as postprandial fullness, nausea, and vomiting.
- Effectively prevents and treats nausea and vomiting associated with chemotherapy, radiotherapy, and postoperative settings through central antiemetic action.
- Reduces symptoms of diabetic gastroparesis, improving quality of life and nutritional intake in affected patients.
- Offers flexible administration routes (oral, IV, IM) allowing for tailored therapy in both outpatient and acute care settings.
- Rapid onset of action, with symptomatic relief often occurring within 30–60 minutes following administration.
Common use
Metoclopramide is indicated for the short-term (4–12 weeks) therapy of adults with symptomatic diabetic gastroparesis. It is also used for the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, and for the prevention of postoperative nausea and vomiting. Off-label uses include management of gastroesophageal reflux disease refractory to conventional therapy, facilitation of small bowel intubation, and as an adjunct in radiologic examinations to accelerate gastric emptying.
Dosage and direction
For diabetic gastroparesis: 10 mg orally 30 minutes before each meal and at bedtime for up to 12 weeks. For chemotherapy-induced nausea/vomiting: 1–2 mg/kg IV 30 minutes before chemotherapy, repeated every 2–3 hours as needed. For postoperative nausea/vomiting: 10–20 mg IM near end of surgery. Maximum daily dose should not exceed 0.5 mg/kg or 30–40 mg in adults. Dosage adjustment is required in patients with renal impairment (CrCl <40 mL/min) and CYP2D6 poor metabolizers.
Precautions
Use with caution in elderly patients due to increased risk of extrapyramidal symptoms and tardive dyskinesia. Monitor for neurological adverse effects, especially with prolonged use (>12 weeks). Assess renal function before initiation and periodically during therapy. Avoid use in patients with history of depression or Parkinson’s disease. May cause drowsiness; caution patients about operating machinery or driving. Use during pregnancy only if clearly needed (FDA Category B). Excreted in breast milk; consider alternative feeding methods during treatment.
Contraindications
Hypersensitivity to metoclopramide or any component of the formulation. Concomitant use with drugs likely to cause extrapyramidal reactions. Pheochromocytoma due to risk of hypertensive crisis. Gastrointestinal obstruction, perforation, or hemorrhage. Epilepsy or history of seizures. Concurrent use with levodopa or dopamine agonists.
Possible side effect
Common: Drowsiness (10–25%), restlessness (10%), fatigue (5–10%), diarrhea (5%). Less common: Extrapyramidal symptoms (akathisia, dystonia, parkinsonism—1–5%), hyperprolactinemia, galactorrhea. Rare but serious: Tardive dyskinesia (risk increases with duration and total cumulative dose), neuroleptic malignant syndrome, seizures, depression. Cardiovascular effects: hypotension, hypertension, supraventricular tachycardia.
Drug interaction
Strong CYP2D6 inhibitors (fluoxetine, paroxetine, quinidine) may increase metoclopramide levels. Additive sedative effects with CNS depressants (alcohol, benzodiazepines, opioids). Antagonizes effects of dopamine agonists (levodopa, bromocriptine). May enhance effects of succinylcholine. Serotonin syndrome risk with serotonergic drugs (SSRIs, SNRIs, tramadol). May reduce absorption of drugs requiring gastric acidity (digoxin, azole antifungals).
Missed dose
If a dose is missed, administer as soon as possible. However, if it is near the time of the next scheduled dose, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed administration. For scheduled pre-meal dosing, if the meal has already been consumed, consider skipping that dose to avoid potential side effects without therapeutic benefit.
Overdose
Symptoms may include drowsiness, confusion, extrapyramidal reactions, seizures, and cardiovascular instability. Management is supportive and symptomatic: gastric lavage if recent ingestion, activated charcoal, and close monitoring. Extrapyramidal symptoms may be treated with diphenhydramine 25–50 mg IV/IM or benztropine 1–2 mg IV/IM. Seizures may require benzodiazepines. There is no specific antidote. Hemodialysis is not effective due to high protein binding and large volume of distribution.
Storage
Store at controlled room temperature (20–25°C/68–77°F). Protect from light and moisture. Keep oral solution in original container; do not freeze. Injectable solution should be inspected for particulate matter and discoloration before use. Discard any unused portion of oral solution after 30 days of opening. Keep all medications out of reach of children and pets.
Disclaimer
This information is intended for healthcare professionals and should not replace clinical judgment. Prescribers should consult full prescribing information and consider individual patient factors before initiating therapy. The use of metoclopramide beyond 12 weeks is not generally recommended due to risk of tardive dyskinesia. Patients should be advised to report any involuntary movements immediately. This document does not contain all possible information about this medication.
Reviews
“Metoclopramide remains a valuable agent in our gastroenterology practice for short-term management of refractory gastroparesis. Its prokinetic effects are predictable, though we maintain vigilance for neurological side effects.” — Gastroenterologist, 15 years experience
“In oncology settings, metoclopramide provides effective antiemetic coverage for moderately emetogenic chemotherapy when combined with dexamethasone. The IV formulation is particularly useful for acute breakthrough nausea.” — Oncology Pharmacist, 10 years experience
“While effective, we reserve metoclopramide for cases where other antiemetics have failed due to the black box warning regarding tardive dyskinesia. Patient education about risk factors and early symptoms is crucial.” — Neurologist, 20 years experience