A-Z Drug Facts > Metoclopramide

Metoclopramide

Pronouncation: (MET-oh-kloe-PRA-mide)
Class: Antidopaminergic, GI stimulant

Trade Names:
Maxolon
- Tablets 10 mg (as monohydrochloride monohydrate)

Trade Names:
Octamide
- Tablets 10 mg (as monohydrochloride monohydrate)

Trade Names:
Octamide PFS
- Injection 5 mg/mL (as monohydrochloride monohydrate)

Trade Names:
Reglan
- Tablets 5 mg (as monohydrochloride monohydrate)
- Tablets 10 mg (as monohydrochloride monohydrate)
- Syrup 5 mg/5 mL (as monohydrochloride monohydrate)
- Injection 5 mg/5 mL (as monohydrochloride monohydrate)

APO-Metoclop (Canada)
Maxeran (Canada)
Metoclopramide Omega (Canada)
Nu-Metoclopramide (Canada)

Pharmacology

Stimulates upper GI tract motility, resulting in accelerated gastric emptying and intestinal transit and increased resting tone of lower esophageal sphincter. Exerts antiemetic properties through antagonism of central and peripheral dopamine receptors.

Pharmacokinetics

Absorption

Absolute oral bioavailability is approximately 80%; T _max is 1 to 2 h.

Distribution

Approximately 30% is protein bound; Vd is approximately 3.5 L/kg.

Elimination

Approximately 85% of dose appears in urine within 72 h (50% of the 85% is present as free n conjugated metoclopramide). The t _½ is 5 to 6 h.

Onset

Onsets are 1 to 3 h (IV), 10 to 15 min (IM), and 30 to 60 min (oral).

Duration

Duration is 1 to 2 h.

Special Populations

Renal Function Impairment

The reduction in Cl suggests that adjustment downward of maintenance dosage should be done to avoid drug accumulation.

Indications and Usage

PO

Relief of symptoms associated with acute and recurrent diabetic gastroparesis; short-term therapy of symptomatic, documented gastroesophageal reflux disease in adults who fail to respond to conventional therapy.

Parenteral

Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy; prophylaxis of postoperative nausea and vomiting when nasogastric suction is undesirable; facilitation of small bowel intubation when tube does not pass pylorus with conventional maneuvers.

Unlabeled Uses

Treatment of hiccoughs, migraines, postoperative gastric bezoars, improvement in lactation, radiation-induced emesis.

Contraindications

Patients in whom increase in GI motility could be harmful (eg, in presence of GI hemorrhage, mechanical obstruction, perforation); pheochromocytoma; epilepsy; patients receiving drugs likely to cause extrapyramidal reactions.

Dosage and Administration

Nausea and Vomiting Caused by Highly Emetogenic Chemotherapy
Adults

IV 2 mg/kg by infusion for 2 doses; give the first dose 30 min before chemotherapy, the second dose 2 h later. If vomiting persists, 3 additional doses of 2 mg/kg may be given every 3 h. If vomiting is controlled, 3 additional doses of 1 mg/kg may be given every 3 h. PO 2 mg/kg 1 h before chemotherapy, followed by 3 more doses at 2-h intervals. If vomiting persists, 2 additional doses may be given every 3 h (total daily dose of 12 mg/kg).

Nausea and Vomiting with Less Emetogenic Chemotherapy
Adults

IV 1 mg/kg by infusion 30 min before chemotherapy, repeated every 2 h for 3 doses.

Prevention of Delayed Nausea and Vomiting Caused by Chemotherapy
Adults

PO 0.5 mg/kg 4 times daily for 4 days beginning 16 to 24 h after chemotherapy given, in combination with dexamethasone. May be given IV in patients unable to take PO.

Adjustment in Renal Insufficiency

Reduce initial dose 50% in patients with CrCl less than 40 mL/min. Titrate subsequent doses based on patient response.

Drug Interactions

Acetaminophen, cyclosporine, ethanol, levodopa, tetracycline

Metoclopramide may increase oral bioavailability or absorption of these drugs.

Anticholinergic, opioid analgesics, levodopa

May decrease effect of metoclopramide on gastric emptying.

Cefprozil, cimetidine, digoxin

Metoclopramide may decrease oral absorption of these drugs.

CNS depressants (eg, alcohol, anesthetics, barbiturates, opiates)

May potentiate CNS depressant effects of metoclopramide.

Succinylcholine and possibly mivacurium

By inhibiting plasma cholinesterase metoclopramide may prolong neuromuscular blocking effects such as respiratory depression and paralysis.

Incompatibility

Cephalothin, chloramphenicol, sodium bicarbonate.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Dizziness; drowsiness; depression; hallucinations; extrapyramidal symptoms that respond rapidly to treatment with anticholinergic agents (eg, diphenhydramine IV); exacerbation of Parkinson disease; tardive dyskinesia; akathisia.

Dermatologic

Transient flushing of face or upper body with high IV doses.

Endocrine

Hyperprolactinemia; galactorrhea; gynecomastia (in men).

GI

Diarrhea.

Genitourinary

Urinary frequency; incontinence; amenorrhea.

Hypersensitivity

Injectable solutions may contain sodium metabisulfite, a sulfite. Sensitive individuals may experience allergic reactions (eg, anaphylaxis, bronchospasm, angioedema).

Precautions

Pregnancy

Category B .

Lactation

Excreted in breast milk.

Children

Some efficacy has been demonstrated. However, methemoglobinemia has occurred in newborns.

Carcinogenesis

Because the drug elevates serum prolactin concentration, use caution if administration of metoclopramide is considered in patient with previously detected breast cancer.

Anastomosis or closure of gut

Drug could theoretically put increased pressure on suture lines after gut anastomosis or closure.

Depression

Depression has occurred with or without history of depression. Symptoms have ranged from mild to severe and have included suicidal ideation and suicide.

Extrapyramidal symptoms

Manifest primarily as acute dystonic reactions, occurring usually during first 24 to 48 h and more frequently in children and young adults or at higher doses.

Hypertension

Use with caution.

Parkinson-like symptoms

Occur more commonly within first 6 mo of treatment but also can occur after longer periods. Symptoms generally subside within 2 to 3 mo after drug discontinuation. Give drug cautiously, if at all, to patients with preexisting Parkinson disease.

Tardive dyskinesia

Tardive dyskinesia may develop, especially in the elderly. Risk of development and likelihood of irreversibility increases with treatment duration and total cumulative dose.

Overdosage

Symptoms

Drowsiness, disorientation, extrapyramidal reactions, muscle hypertonia, irritability, agitation.

Patient Information

• Instruct patient to take medication 30 min before meals.
• Instruct patient to report the following symptoms to the health care provider: involuntary movement of eyes, face, or limbs.
• Caution patient to avoid intake of alcoholic beverages.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.

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