The mechanisms of action of metoclopramide involve 5-HT4 receptor agonism, vagal and central 5-HTj antagonism, possible sensitization of muscarinic receptors on smooth muscle, and dopamine receptor antagonism. Metoclopramide, one of the oldest true prokinetic agents, stimulates coordinated contractions that enhance transit. Its effects are confined largely to the upper digestive tract, where it increases lower esophageal sphincter tone and stimulates antral and small intestinal contractions. Metoclopramide has no clinically significant effects on large-bowel motility.
Therapeutic Use and Pharmacokinetics Metoclopramide is indicated in symptomatic patients with gastroparesis, in whom it may modestly improve gastric emptying. Metoclopramide injection is used as an adjunctive measure in medical or diagnostic procedures such as intestinal intubation or contrast radiography of the GI tract. Although it has been used in patients with postoperative ileus, its ability to improve transit in disorders of small-bowel motility is limited. In general, its greatest utility lies in its ability to ameliorate the nausea and vomiting that often accompany GI dysmotility syndromes.
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