Look Up > Drugs > Metoclopramide
Metoclopramide
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Pharmacological Index
Use
Pregnancy Risk Factor
Pregnancy/Breast-Feeding Implications
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(met oh kloe PRA mide)

U.S. Brand Names
Maxolon®; Octamide® PFS; Reglan®

Generic Available

Yes


Canadian Brand Names
Apo®-Metoclop; Maxeran®

Pharmacological Index

Gastrointestinal Agent, Prokinetic


Use

Symptomatic treatment of diabetic gastric stasis, gastroesophageal reflux; prevention of nausea associated with chemotherapy or postsurgery and facilitates intubation of the small intestine


Pregnancy Risk Factor

B


Pregnancy/Breast-Feeding Implications

Clinical effects on the fetus: Crosses the placenta. Available evidence suggests safe use during pregnancy and breast-feeding.

Breast-feeding/lactation: Crosses into breast milk

Clinical effects on the infant: Increased milk production; 2 reports of mild intestinal discomfort; American Academy of Pediatrics states MAY BE OF CONCERN


Contraindications

Hypersensitivity to metoclopramide or any component; GI obstruction, perforation or hemorrhage, pheochromocytoma, history of seizure disorder


Warnings/Precautions

Use with caution in patients with Parkinson's disease and in patients with a history of mental illness; dosage and/or frequency of administration should be modified in response to degree of renal impairment; extrapyramidal reactions, depression; may exacerbate seizures in seizure patients; to prevent extrapyramidal reactions, patients may be pretreated with diphenhydramine; elderly are more likely to develop dystonic reactions than younger adults; use lowest recommended doses initially


Adverse Reactions

>10%:

Central nervous system: Restlessness, drowsiness

Gastrointestinal: Diarrhea

Neuromuscular & skeletal: Weakness

1% to 10%:

Central nervous system: Insomnia, depression

Dermatologic: Rash

Endocrine & metabolic: Breast tenderness, prolactin stimulation

Gastrointestinal: Nausea, xerostomia

<1%: Tachycardia, hypertension or hypotension, extrapyramidal reactions*, tardive dyskinesia, fatigue, anxiety, agitation, constipation, methemoglobinemia

*Note: A recent study suggests the incidence of extrapyramidal reactions due to metoclopramide may be as high as 34% and the incidence appears more often in the elderly


Overdosage/Toxicology

Symptoms of overdose include drowsiness, ataxia, extrapyramidal reactions, seizures, methemoglobinemia (in infants); disorientation, muscle hypertonia, irritability, and agitation are common

Metoclopramide often causes extrapyramidal symptoms (eg, dystonic reactions) requiring management with diphenhydramine 1-2 mg/kg (adults) up to a maximum of 50 mg I.M. or I.V. slow push followed by a maintenance dose for 48-72 hours. When these reactions are unresponsive to diphenhydramine, benztropine mesylate I.V. 1-2 mg (adults) may be effective. These agents are generally effective within 2-5 minutes.


Drug Interactions

CYP1A2 and 2D6 enzyme substrate

Increased toxicity: Opiate analgesics may increase CNS depression


Stability

Injection is a clear, colorless solution and should be stored at controlled room temperature and protected from freezing; injection is photosensitive and should be protected from light during storage; dilutions do not require light protection if used within 24 hours

Standard diluent: 10-150 mg/50 mL D5W or NS

Minimum volume: 50 mL D5W or NS; send 10 mg unmixed to nursing unit

Compatible with diphenhydramine


Mechanism of Action

Blocks dopamine receptors in chemoreceptor trigger zone of the CNS; enhances the response to acetylcholine of tissue in upper GI tract causing enhanced motility and accelerated gastric emptying without stimulating gastric, biliary, or pancreatic secretions


Pharmacodynamics/Kinetics

Onset of effect: Oral: Within 0.5-1 hour; I.V.: Within 1-3 minutes

Duration of therapeutic effect: 1-2 hours, regardless of route administered

Distribution: Crosses the placenta; appears in breast milk

Protein binding: 30%

Half-life, normal renal function: 4-7 hours (may be dose-dependent)

Elimination: Primarily as unchanged drug in urine and feces


Usual Dosage

Children:

Gastroesophageal reflux: Oral: 0.1-0.2 mg/kg/dose up to 4 times/day; efficacy of continuing metoclopramide beyond 12 weeks in reflux has not been determined; total daily dose should not exceed 0.5 mg/kg/day

Gastrointestinal hypomotility (gastroparesis): Oral, I.M., I.V.: 0.1 mg/kg/dose up to 4 times/day, not to exceed 0.5 mg/kg/day

Antiemetic (chemotherapy-induced emesis): I.V.: 1-2 mg/kg 30 minutes before chemotherapy and every 2-4 hours

Facilitate intubation: I.V.:

<6 years: 0.1 mg/kg

6-14 years: 2.5-5 mg

Adults:

Gastroesophageal reflux: Oral: 10-15 mg/dose up to 4 times/day 30 minutes before meals or food and at bedtime; single doses of 20 mg are occasionally needed for provoking situations; efficacy of continuing metoclopramide beyond 12 weeks in reflux has not been determined

Gastrointestinal hypomotility (gastroparesis):

Oral: 10 mg 30 minutes before each meal and at bedtime for 2-8 weeks

I.V. (for severe symptoms): 10 mg over 1-2 minutes; 10 days of I.V. therapy may be necessary for best response

Antiemetic (chemotherapy-induced emesis): I.V.: 1-2 mg/kg 30 minutes before chemotherapy and every 2-4 hours to every 4-6 hours (and usually given with diphenhydramine 25-50 mg I.V./oral)

Postoperative nausea and vomiting: I.M.: 10 mg near end of surgery; 20 mg doses may be used

Facilitate intubation: I.V.: 10 mg

Elderly:

Gastroesophageal reflux: Oral: 5 mg 4 times/day (30 minutes before meals and at bedtime); increase dose to 10 mg 4 times/day if no response at lower dose

Gastrointestinal hypomotility:

Oral: Initial: 5 mg 30 minutes before meals and at bedtime for 2-8 weeks; increase if necessary to 10 mg doses

I.V.: Initiate at 5 mg over 1-2 minutes; increase to 10 mg if necessary

Postoperative nausea and vomiting: I.M.: 5 mg near end of surgery; may repeat dose if necessary

Dosing adjustment in renal impairment:

Clcr 10-40 mL/minute: Administer at 50% of normal dose

Clcr <10 mL/minute: Administer at 25% of normal dose

Hemodialysis: Not dialyzable (0% to 5%); supplemental dose is not necessary


Dietary Considerations

Alcohol: Additive CNS effect, avoid use


Monitoring Parameters

Periodic renal function test; monitor for dystonic reactions; monitor for signs of hypoglycemia in patients using insulin and those being treated for gastroparesis; monitor for agitation and irritable confusion


Test Interactions

aminotransferase [ALT (SGPT)/AST (SGOT)] (S), amylase (S)


Mental Health: Effects on Mental Status

Drowsiness and restlessness are common; may cause insomnia or depression; drug is a D2 blocker; may cause extrapyramidal symptoms especially when used in high dosages or in the elderly


Mental Health: Effects on Psychiatric Treatment

Anticholinergics may antagonize metoclopramide's effects; concurrent use with psychotropic may produce additive sedation


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Take this drug as prescribed, 30 minutes prior to eating. Do not increase dosage. Do not use alcohol or other CNS depressant or sleeping aids without consulting prescriber. May cause dizziness, drowsiness, or blurred vision; use caution when driving or engaging in tasks that require alertness until response to drug is known. May cause restlessness, anxiety, depression, or insomnia (will reverse when medication is discontinued). Report any CNS changes, involuntary movements, unresolved diarrhea. If diabetic, monitor serum glucose regularly. Breast-feeding precautions: Breast-feeding is not recommended.


Nursing Implications

Parenteral doses of up to 10 mg should be administered I.V. push over 1-2 minutes; rapid boluses cause transient anxiety and restlessness followed by drowsiness; higher doses to be administered IVPB; dilute to 0.2 mg/mL (maximum concentration: 5 mg/mL) and infuse over 15-30 minutes (maximum rate of infusion: 5 mg/minute); rapid I.V. administration is associated with a transient but intense feeling of anxiety and restlessness, followed by drowsiness

Monitor periodic renal function test


Dosage Forms

Injection: 5 mg/mL (2 mL, 10 mL, 30 mL, 50 mL, 100 mL)

Solution, oral, concentrated: 10 mg/mL (10 mL, 30 mL)

Syrup, sugar free: 5 mg/5 mL (10 mL, 480 mL)

Tablet: 5 mg, 10 mg


References

DiPalma JR, "Metoclopramide: A Dopamine Receptor Antagonist," Am Fam Physician, 1990, 41(3):919-24.

Francom M, "Compounding Nausea Aid," Am Pharm, 1991, NS31(7):7.

Hughes RL, "Hypotension and Dysrhythmia Following Intravenous Metoclopramide," Anaesthesia, 1984, 39(7):720.

Kearns GL and Fiser DH, "Metoclopramide-Induced Methemoglobinemia," Pediatrics, 1988, 82(3):364-6.

Le Couteur DG and Kay T, "Delayed Neuroleptic Malignant Syndrome Following Cessation of Prolonged Therapy With Metoclopramide," Aust N Z J Med, 1995, 25(3):261.

Low LC and Goel KM, "Metoclopramide Poisoning in Children," Arch Dis Child, 1980, 55(3):310-2.

Malkoff MD, Ponzillo JJ, Myles GL, et al, "Sinus Arrest After Administration of Intravenous Metoclopramide," Ann Pharmacother, 1995, 29(4):381-3.

Patterson JF, "Neuroleptic Malignant Syndrome Associated With Metoclopramide," South Med J, 1988, 81(5):674-5.

Scharman EJ, Lembersky R, and Krenzelok EP, "Efficiency of Whole Bowel Irrigation With and Without Metoclopramide Pretreatment," Am J Emerg Med, 1994, 12(3):302-5.

Van Veldhuizen PJ and Wyatt A, "Metoclopramide-Induced Sulfhemoglobinemia," Am J Gastroenterol, 1995, 90(6):1010-1.


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