section name header

Pronunciation ⬇

met-oh-KLOE-pra-mide

Classifications ⬆ ⬇

Therapeutic Classification: antiemetics

Indications ⬆ ⬇

BEERS REMS


Unlabeled Use:
  • Hiccups.

Action ⬆ ⬇

  • Blocks dopamine receptors in chemoreceptor trigger zone of the CNS.
  • Stimulates motility of the upper GI tract and accelerates gastric emptying.
Therapeutic effects:
  • Decreased nausea and vomiting.
  • Decreased symptoms of gastric stasis.
  • Easier passage of nasogastric tube into small bowel.

Pharmacokinetics ⬆ ⬇

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.

Time/Action Profile ⬆ ⬇

(effects on peristalsis)

ROUTEONSETPEAKDURATION
PO30–60 minunknown1–2 hr
IM10–15 minunknown1–2 hr
Intranasalunknownunknownunknown
IV1–3 minimmediate1–2 hr



Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

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

Interactions ⬆ ⬇

Drug-drug:

Route/Dosage ⬆ ⬇

Prevention of Chemotherapy-Induced Nausea and Vomiting

Facilitation of Small Bowel Intubation

Diabetic Gastroparesis

Renal Impairment

Hepatic Impairment

Gastroesophageal Reflux

Renal Impairment

Hepatic Impairment

Prevention of Postoperative Nausea and Vomiting

Hiccups

Availability ⬆ ⬇

(Generic available)

Assessment ⬆ ⬇

Lab Test Considerations:

Implementation ⬆ ⬇

IV Administration:

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆

Gimoti, Reglan