• PO: Gastroesophageal reflux
• PO, IV, Intranasal: Acute and recurrent diabetic gastroparesis.
• IV: Used for the following conditions:
  • Prevention of nausea and vomiting associated with emetogenic chemotherapy,
  • Prevention of postoperative nausea and vomiting when nasogastric suctioning is undesirable,
  • Facilitation of small bowel intubation in radiographic procedures.

Unlabeled Uses:

• Treatment of hiccups.

Contraindicated in:

• Hypersensitivity
• Possible GI obstruction, perforation, or hemorrhage
• Seizure disorders
• Hypertension
• Pheochromocytoma
• History of tardive dyskinesia
• Parkinson's disease
• Concurrent use of MAO inhibitors
• Moderate or severe renal or hepatic impairment (intranasal only)
• CYP2D6 poor metabolizers (↑ risk for tardive dyskinesia) (intranasal only)
• Concurrent use of strong CYP2D6 inhibitors (intranasal only).

Use Cautiously in:

• History of depression
• Diabetes (may alter response to insulin)
• Cirrhosis or HF (↑ risk of fluid retention)
• Renal impairment (↓ dose in CCr <50 mL/min) (oral and IV/IM only)
• Chronic use >12 wk (↑ risk for tardive dyskinesia)
• Moderate or severe hepatic impairment
• CYP2D6 poor metabolizers (↑ risk for tardive dyskinesia) (oral and IV/IM only)
• OB: May cause extrapyramidal symptoms or methemoglobinemia in neonate when used during pregnancy
• Lactation: May lead to diarrhea, extrapyramidal symptoms, or methemoglobinemia in infant when used during breastfeeding
• Pedi: Prolonged clearance in neonates can result in high serum concentrations and ↑ the risk for methemoglobinemia. Side effects are more common in children, especially extrapyramidal reactions. Avoid use of tablets and intranasal because of ↑ risk of tardive dyskinesia and methemoglobinemia (in neonates)
• Geri: Appears on Beers list. ↑ risk of extrapyramidal effects, including tardive dyskinesia, in older adults. Avoid use in older adults, except for gastroparesis (duration for this indication should generally not exceed 12 wk). Intranasal therapy not recommended as initial therapy in older adults (can be transitioned to intranasal therapy once stabilized on oral therapy.

CV: bradycardia, hypertension, hypotension, supraventricular tachycardia.

Endo: gynecomastia, hyperprolactinemia.

GI: constipation, diarrhea, dry mouth, nausea.

Hemat: agranulocytosis, leukopenia, methemoglobinemia, neutropenia.

Neuro: drowsiness, dysgeusia (intranasal), extrapyramidal reactions, restlessness, anxiety, bradykinesia, cog-wheel rigidity, depression, irritability, NEUROLEPTIC MALIGNANT SYNDROME, tardive dyskinesia, tremor.

Drug-Drug:

• MAO inhibitors may cause release of catecholamines which may ↑ BP; avoid concurrent use.
• Additive CNS depression with other CNS depressants, including alcohol, antidepressants, antihistamines, opioid analgesics, and sedative/hypnotics.
• May ↑ absorption and risk of toxicity from cyclosporine.
• May affect the GI absorption of other orally administered drugs as a result of effect on GI motility.
• May exaggerate hypotension during general anesthesia.
• ↑ risk of tardive dyskinesia, extrapyramidal reactions, or neuroleptic malignant syndrome with antipsychotic agents; avoid concurrent use.
• Strong CYP2D6 inhibitors, including bupropion, fluoxetine, paroxetine, or quinidine may ↑ levels and risk of extrapyramidal reactions; avoid concurrent use with intranasal metoclopramide; ↓ PO or IV/IM metoclopramide dose.
• Opioids and anticholinergics may antagonize the GI effects of metoclopramide.
• May ↑ neuromuscular blockade from succinylcholine.
• May ↓ effectiveness of levodopa.
• May ↑ tacrolimus serum levels.

(Generic available)

• Tablets: 5 mg; 10 mg;
• Orally disintegrating tablets: 5 mg; 10 mg;
• Oral solution (apricot-peach flavor): 5 mg/5 mL;
• Nasal spray: 15 mg/metered spray in 9.8–mL bottle (delivers 112 metered sprays);
• Solution for injection: 5 mg/mL;

Prevention of Chemotherapy-Induced Nausea and Vomiting

• IV (Adults and Children): 1–2 mg/kg 30 min before chemotherapy. Additional doses of 1–2 mg/kg may be given every 2–4 hr, pretreatment with diphenhydramine will ↓ the risk of extrapyramidal reactions to this dose.

Facilitation of Small Bowel Intubation

• IV (Adults and Children >14 yr): 10 mg over 1–2 min.
• IV (Children 6–14 yr): 2.5–5 mg (dose should not exceed 0.5 mg/kg) over 1–2 min.
• IV (Children <6 yr): 0.1 mg/kg over 1–2 min.

Diabetic Gastroparesis

• PO, IV, IM (Adults): 10 mg 30 min before meals and at bedtime for 2–8 wk (not to exceed 40 mg/day). CYP2D6 poor metabolizers: 5 mg 30 min before meals and at bedtime for 2–8 wk (not to exceed 20 mg/day). Concurrent use of strong CYP2D6 inhibitor: 5 mg 30 min before meals and at bedtime for 2–8 wk (not to exceed 20 mg/day).
• Intranasal (Adults): One spray (15 mg) in one nostril 30 min before each meal and at bedtime (not to exceed 60 mg/day) for 2–8 wk (not to exceed 12 wk).
• PO, IV, IM (Geriatric Patients): 5 mg 30 min before meals and at bedtime for 2–8 wk; may titrate up to 10 mg 30 min before each meal and at bedtime based on response and tolerability (not to exceed 40 mg/day).
• Intranasal (Geriatric Patients): Patients receiving alternative metoclopramide product at stable dose of 10 mg four times daily: One spray (15 mg) in one nostril 30 min before each meal and at bedtime (not to exceed 60 mg/day) for 2–8 wk (not to exceed 12 wk).

Gastroesophageal Reflux

• PO (Adults): 10–15 mg 30 min before each meal and at bedtime (not to exceed 60 mg/day). CYP2D6 poor metabolizers: 5 mg 30 min before each meal and at bedtime or 10 mg 3 times daily (not to exceed 30 mg/day). Concurrent use of strong CYP2D6 inhibitor: 5 mg 30 min before each meal and at bedtime or 10 mg 3 times daily (not to exceed 30 mg/day).
• PO (Geriatric Patients): 5 mg 30 min before each meal and at bedtime; may titrate up to 10–15 mg 30 min before each meal and at bedtime based on response and tolerability (not to exceed 60 mg/day).

Prevention of Postoperative Nausea and Vomiting

• IM, IV (Adults): 10 mg at the end of surgical procedure, repeat in 6–8 hr if needed.

Treatment of Hiccups

• PO, IM (Adults): 10–20 mg 4 times daily PO; may be preceded by a single 10-mg dose IM.

Gimoti, Reglan

• Blocks dopamine receptors in chemoreceptor trigger zone of the CNS.
• Stimulates motility of the upper GI tract and accelerates gastric emptying.

• Decreased nausea and vomiting.
• Decreased symptoms of gastric stasis.
• Easier passage of nasogastric tube into small bowel.

Therapeutic Classification: antiemetics

Absorption: Well absorbed from the GI tract, from rectal mucosa, and from IM sites. 47% absorbed following intranasal administration. IV administration results in complete bioavailability.

Distribution: Widely distributed into body tissues and fluids. Crosses blood-brain barrier.

Metabolism/Excretion: Partially metabolized by the liver via the CYP2D6 isoenzyme; the CYP2D6 isoenzyme exhibits genetic polymorphism ( 7% of population may be poor metabolizers and may have significantly ↑ metoclopramide concentrations and an ↑ risk of adverse effects). 25% eliminated unchanged in the urine.

Half-life: 2.5–6 hr.

Metonia

(effects on peristalsis)

• Instruct patient to take metoclopramide as directed. Explain how to administer intranasal doses. Take oral missed doses as soon as remembered if not almost time for next dose. If an intranasal dose is missed, omit and take the next dose at regularly scheduled time; do not double doses. Advise patient to read the Medication Guide before starting therapy and with each Rx refill in case of changes.
• Pedi: Unintentional overdose has been reported in infants and children with the use of metoclopramide oral solution. Teach parents how to accurately read labels and administer medication.
• May cause drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
• Advise patient to avoid concurrent use of alcohol and other CNS depressants while taking this medication.
• Inform patient of risk of extrapyramidal symptoms, tardive dyskinesia, and neuroleptic malignant syndrome. Advise patient to notify health care professional immediately if involuntary or repetitive movements of eyes, face, or limbs occur.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Monitor neonates for extrapyramidal signs and methemoglobinemia.

met-oh-KLOE-pra-mide