Dosing and uses of Reglan, Metozolv ODT (metoclopramide)
Adult dosage forms and strengths
injectable solution
- 5mg/mL
syrup
- 5mg/5mL
- 10mg/10mL
tablet
- 5mg
- 10mg
Dispersible tablets
- 5mg
- 10mg
Chemotherapy-Induced Nausea & Vomiting
2 mg/kg IV (infused over at least 15 minutes) 30 minutes before chemotherapy, then repeated 2 more times q2hr (after initial dose)
Vomiting suppressed: Decrease to 1 mg/kg IV q3hr for 3 doses
Vomiting not suppressed: Continue same dose q3hr for 3 doses
Diabetic Gastroparesis
10 mg IV/IM/PO q6hr 30 minutes before meals and at bedtime; use injectable dosing only if severe symptoms are present
Small Bowel Intubation/Radiologic Examination of Upper GI Tract
10 mg IV over 1-2 minutes
Gastroesophageal Reflux Disease
10-15 mg PO q6hr 30 minutes before meals and at bedtime; not to exceed 80 mg/day
Postoperative Nausea & Vomiting (Off-label)
10-20 mg IM administered near end of procedure; may be repeated postoperatively q4-6hr PRn
Dosing Modifications
Renal impairment: CrCl <40 mL/min, decrease dose by 50%; CrCl <10 mL/min, decrease dose by 75%
Pediatric dosage forms and strengths
injectable solution
- 5mg/mL
syrup
- 5mg/5mL
- 10mg/10mL
tablets
- 5mg
- 10mg
Dispersible tablets
- 5mg
- 10mg
Small Bowel Intubation/Radiologic Examination of Upper GI Tract
<6 years old: 0.1 mg/kg IV over 1-2 minutes
6-14 years old: 2.5-5 mg IV over 1-2 minutes
≥14 years old: 10 mg IV over 1-2 minutes
Gastroesophageal Reflux Disease (Off-label)
Neonate: 0.15 mg/kg IV q6hr
Infant: 0.1 mg/kg IV/IM/PO q6-8hr 30 minutes before meals and at bedtime
Not to exceed 0.3-0.75 mg/kg/day
Diabetic Gastroparesis (Off-label)
<6 years old: 0.1 mg/kg PO q8hr; not to exceed 0.1 mg/kg
≥6 years old: 0.5 mg/kg/day PO divided q8hr
Postoperative Nausea & Vomiting (Off-label)
0.1-2 mg/kg IV q6-8hr PRn
Chemotherapy-Induced Nausea & Vomiting (Off-label)
1-2 mg/kg IV (infused over at least 15 minutes) 30 minutes before chemotherapy; repeat q2-4hr; pretreatment with diphenhydramine decreases risk of extrapyramidal adverse effects
Reglan, Metozolv ODT (metoclopramide) adverse (side) effects
>10%
Extrapyramidal symptoms (dystonic reactions in 25% of young adults 18-30 years old)
1-10%
Fatigue (2-10%)
Restlessness (10%)
Sedation (10%)
Headache (4-5%)
Dizziness (1-4%)
Somnolence (2-3%)
Frequency not defined
Diarrhea
Nausea
Galactorrhea
Gynecomastia
Impotence
Menstrual disorders
Neuroleptic malignant syndrome
Hematologic abnormalities
Warnings
Black box warnings
May cause tardive dyskinesia (often irreversible)
Risk of developing tardive dyskinesia increases with treatment duration and total cumulative dose
Discontinue with signs or symptoms of tardive dyskinesia
No known treatment exists for tardive dyskinesia
Symptoms may lessen or resolve after metoclopramide treatment is stopped
Do not administer for longer than 12 weeks, except in rare cases where therapeutic benefit is thought to outweigh risk of tardive dyskinesia
Contraindications
Hypersensitivity to metoclopramide or procainamide
GI hemorrhage, mechanical obstruction, perforation, history of seizures, pheochromocytoma
Other drugs causing extrapyramidal symptoms (eg, phenothiazines, butyrophenones)
Cautions
Mental depression reported; use with caution in patients with history of mental illness
Use with caution or avoid in parkinson disease patients; may have increased risk of extrapyramidal symptoms
Use with caution after GI anastomosis or closure; promotility agents reported to increase pressure in suture lines
Use caution in patients with hypertension, CHF, renal impairment, cirrhosis
Use caution in patients who are at risk of fluid overload
Can cause tardive dyskinesia (see Black box warnings), especially in elderly; discontinue if signs or symptoms of tardive dyskinesia develop (metoclopramide itself may completely or partially suppress these manifestations); tardive dyskinesia may persist even after drug is discontinued
Diphenhydramine 50 mg IM can be given for extrapyramidal symptoms
Pseudoparkisonism (eg, tremor, rigidity) may occur within 6 months of therapy; reversible within 2-3 months of discontinuing therapy
Metoclopramide IV administration associated with catecholamine release; use caution in patients with hypertension
Hypertensive crisis reported in patients with undiagnosed pheochromocytoma; discontinue therapy immediately with any sudden increase in blood pressure during therapy
May cause QT prolongation and torsades de pointes in some patients with heart failure patients that also have renal impairment; data on healthy males have failed to show similar effects; implicatiosn unclear; use caution in cardiovascular disease
Pregnancy and lactation
Pregnancy category: B; No association was observed between exposure to metoclopramide during pregnancy and an increased risk of birth defects, spontaneous abortion, or stillbirth, according to results of a large, register-based study [JAMA 2013 310(15)]; other studies have also shown no association with first trimester use and major congenital malformations [N Engl J Med 2009 360(24)]
Lactation: Drug crosses into breast milk; use caution; concern may be warranted according to American Academy of Pediatrics
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Reglan, Metozolv ODT (metoclopramide)
Mechanism of action
Blocks dopamine receptors (at high dose) and serotonin receptors in chemoreceptor trigger zone of CNS; and sensitizes tissues to acetylcholine; increases upper GI motility but not secretions; increases lower esophageal sphincter tone
Absorption
Bioavailability: IM, 74-96%; PO, 65-95%
Onset: 1-3 min (IV, ); 10-15 min (IM); 30-60 min (PO)
Duration: 1-2 hr regardless of route
Peak serum time: IV, 15 min; PO, 60-120 min
Distribution
Protein bound: 30-40%
Vd: 3.5 L/kg
Metabolism
Metabolized by liver
Metabolites: Metoclopramide glucuronides, metoclopramide sulfates, aminoacetic acid (inactive)
Elimination
Half-life (IV/IM): 5-6hr (adults); 4 hr (children)
Dialyzable: Not significant; dose adjustment after dialysis unnecessary
Total body clearance: 0.53-0.55 L/hr/kg (prolonged in neonates as compared with adults)
Excretion: Primarily urine (85%)
Administration
IV Incompatibilities
Solution: D5W (at high drug concentration)
Additive: Dexamethasone sodium phosphate with lorazepam and diphenhydramine, erythromycin lactobionate, floxacillin, fluorouracil, furosemide
Syringe: Ampicillin, calcium gluconate, chloramphenicol sodium succinate, furosemide, methotrexate, penicillin G potassium, sodium bicarbonate
Y-site: Allopurinol, amphotericin B cholesteryl sulfate, amsacrine, cefepime, doxorubicin liposomal, furosemide, propofoL
IV Compatibilities
Additive: Cimetidine, clindamycin, meperidine, meropenem, morphine sulphate, potassium chloride, verapamiL
Syringe (partial list): Butorphanol, chlorpromazine, cisplatin, cyclophosphamide, cytarabine, dexamethasone, dimenhydrinate, diphenhydramine, doxorubicin, fentanyl, fentanyl with midazolam, fluorouracil, heparin, hydromorphone, hydroxyzine, insulin, lidocaine, magnesium sulfate, meperidine, midazolam, morphine, ondansetron, pentazocine, prochlorperazine, promethazine, ranitidine, vitamins B and C
Y-site (partial list): Aztreonam, bivalirudin, ciprofloxacin, cisplatin, cytarabine, diltiazem, docetaxel, doxorubicin, famotidine, fentanyl, fluconazole, fluorouracil, heparin, hydromorphone, linezolid, meperidine, morphine sulfate, ondansetron, quinupristin-dalfopristin, zidovudine
IV Administration
NS is preferred diluent because drug is most stable in this solution
Dose ≤10 mg: IV push over 1-2 minutes
Dose >10 mg: Dilute in 50 mL D5W or NS, and infuse over at least 15 minutes
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