Metoclopramide

Prokinetic, Antiemetic, Dopamine D2 antagonist

Metoclopramide

Reglan, Gimoti (intranasal), Metozolv ODT

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Summary

Classes

Prokinetic, Antiemetic, Dopamine D2 antagonist

Common uses

Gastroparesis0, GERD (refractory; short-term)0, Postoperative nausea and vomiting0, Chemotherapy-induced nausea and vomiting (less first-line since 5-HT3 antagonists)0, Migraine rescue (with NSAID or triptan)0

Pharmacy

Starting dose

10 mg PO/IV/IM QID, not to exceed 12 weeks (tardive dyskinesia risk); intranasal Gimoti 15 mg BID

Preparations

5, 10 mg tablets; 5 mg/5 mL solution; 5 mg/mL IV; 15 mg/spray intranasal

US FDA Max

40 mg/d

Pharmacology

Routes

Oral, IV, IM, intranasal

Onset

IV/IM 1-3 minutes; PO 30-60 minutes

Duration

4-6 hours

Half-life

5-6 hours^[1]

Bioavailability

~80% (oral; reduced by significant first-pass)^[1]

Pregnancy

Widely used for hyperemesis gravidarum; reassuring data.^{[citation needed]}

Legal status

Rx-only in US. Carries a Boxed Warning for tardive dyskinesia (irreversible movement disorder), driving the 12-week chronic-use limit^[1]

Purported mechanism

Metoclopramide antagonizes D2 dopamine receptors in the area postrema (antiemetic effect) and sensitizes gut tissue to acetylcholine, increasing lower esophageal sphincter tone, gastric antral contractions, and small bowel motility (the prokinetic effect); 5-HT4 agonism is a secondary mechanism contributing to prokinesis.0 D2 antagonism is also the source of the extrapyramidal adverse effects: acute dystonia (especially in young women), akathisia, parkinsonism, and the boxed-warning tardive dyskinesia (cumulative-dose and chronic-use dependent). Domperidone has the same prokinetic effect with less CNS penetration but is not FDA-approved in the US^[1].

References

↑ ^1.0 ^1.1 ^1.2 ^1.3 FDA Prescribing Information, Reglan (metoclopramide), ANI, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/017854s064,017862s080lbl.pdf

[reglan-label-1] 1.0 ^1.1 ^1.2 ^1.3 FDA Prescribing Information, Reglan (metoclopramide), ANI, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/017854s064,017862s080lbl.pdf

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