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Pronunciation |
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(met
oh kloe PRA
mide) |
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U.S. Brand
Names |
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Maxolon®; Octamide® PFS;
Reglan® |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Apo®-Metoclop;
Maxeran® |
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Pharmacological Index |
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Gastrointestinal Agent, Prokinetic |
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Use |
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Symptomatic treatment of diabetic gastric stasis, gastroesophageal reflux;
prevention of nausea associated with chemotherapy or postsurgery and facilitates
intubation of the small intestine |
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Pregnancy Risk
Factor |
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B |
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Pregnancy/Breast-Feeding
Implications |
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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
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Contraindications |
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Hypersensitivity to metoclopramide or any component; GI obstruction,
perforation or hemorrhage, pheochromocytoma, history of seizure
disorder |
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Warnings/Precautions |
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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 |
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Adverse
Reactions |
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>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 |
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Overdosage/Toxicology |
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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. |
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Drug
Interactions |
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CYP1A2 and 2D6 enzyme substrate
Increased toxicity: Opiate analgesics may increase CNS depression
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Stability |
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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 |
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Mechanism of
Action |
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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 |
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Pharmacodynamics/Kinetics |
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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
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Usual Dosage |
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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
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Dietary
Considerations |
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Alcohol: Additive CNS effect, avoid use |
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Monitoring
Parameters |
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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 |
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Test
Interactions |
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aminotransferase [ALT
(SGPT)/AST (SGOT)] (S),
amylase
(S) |
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Mental Health: Effects
on Mental Status |
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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 |
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Mental Health:
Effects on Psychiatric
Treatment |
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Anticholinergics may antagonize metoclopramide's effects; concurrent use with
psychotropic may produce additive sedation |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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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. |
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Nursing
Implications |
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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 |
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Dosage Forms |
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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 |
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References |
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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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