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Indication
For the treatment of gastroesophageal reflux disease (GERD)

Pharmacology
Metoclopramide, although chemically related to procainamide, does not possess local anesthetic or antiarrhythmic properties. Metoclopramide is used to enhance GI motility, to treat diabetic gastroparesis, as an antinauseant, and to facilitate intubation of the small bowel during radiologic examination. Metoclopramide may be used to treat chemotherapy-induced emesis and as a radiosensitizing agents in the treatment of non-small cell lung carcinoma and glioblastomas in the future.

Mechanism Of Action
Metoclopramide inhibits gastric smooth muscle relaxation produced by dopamine, therefore increasing cholinergic response of the gastrointestinal smooth muscle. It accelerates intestinal transit and gastric emptying by preventing relaxation of gastric body and increasing the phasic activity of antrum. Simultaneously, this action is accompanied by relaxation of the upper small intestine, resulting in an improved coordination between the body and antrum of the stomach and the upper small intestine. Metoclopramide also decreases reflux into the esophagus by increasing the resting pressure of the lower esophageal sphincter and improves acid clearance from the esophagus by increasing amplitude of esophageal peristaltic contractions. Metoclopramide's dopamine antagonist action raises the threshold of activity in the chemoreceptor trigger zone and decreases the input from afferent visceral nerves. Studies have also shown that high doses of metoclopramide can antagonize 5-hydroxytryptamine (5-HT) receptors in the peripheral nervous system in animals.

Drug Category
Antiemetics; Prokinetic Agents; Dopamine Antagonists; ATC:A03FA01

Brand Names/Synonyms
Apo-Metoclop; CHEMBANK734; Cerucal; Clopra; Clopra-Yellow; Clopromate; DEL; DEL 1267; DEL-1267; Duraclamid; Elieten; Emetid; Emperal; Eucil; Gastrese; Gastro-Timelets; Gastrobid; Gastromax; Gastronerton; Gastrosil; Gastrotablinen; Gastrotem; Imperan; M0763; M117; Maxeran; Maxolon; Meclopran; Metaclopramide; Metaclopromide; Metamide; Methochlopramide; Methoclopramide; Metochlopramide; Metoclol; Metoclopramida [Inn-Spanish]; Metoclopramide; Metoclopramide Hcl; Metoclopramide Hydrochloride; Metoclopramide Intensol; Metoclopramide Omega; Metoclopramidum [Inn-Latin]; Metocobil; Metramid; Moriperan; Mygdalon; Neu-Sensamide; Nu-Metoclopramide; Octamide; Parmid; Paspertin; Peraprin; Plasil; Pms-Metoclopramide; Pramiel; Pramin; Primperan; Reclomide; Reglan; Reliveran; Terperan

Dosage Forms
LIQUID; SYRUP; TABLET

Absorption
Rapidly and well absorbed (oral bioavailability 80±15.5%).

Interactions
DRUG INTERACTIONS The effects of metoclopramide on gastrointestinal motility are antagonized by anticholinergic drugs and narcotic analgesics. Additive sedative effects can occur when metoclopramide is given with alcohol, sedatives, hypnotics, narcotics, or tranquilizers. The finding that metoclopramide releases catecholamines in patients with essential hypertension suggests that it should be used cautiously, if at all, in patients receiving monoamine oxi-dase inhibitors. Absorption of drugs from the stomach may be diminished (e.g., digoxin) by metoclopramide, whereas the rate and/or extent of absorption of drugs from the small bowel may be increased (e.g., acetaminophen, tetracycline, levodopa, ethanol, cyclosporine). Gastroparesis (gastric stasis) may be responsible for poor diabetic control in some patients. Exogenously administered insulin may begin to act before food has left the stomach and lead to hypoglycemia. Because the action of metoclopramide will influence the delivery of food to the intestines and thus the rate of absorption, insulin dosage or timing of dosage may require adjustment.

Chemical IUPAC Name
4-amino-5-chloro-N-(2-diethylaminoethyl)-2-methoxy-benzamide

Chemical Formula
C14H22ClN3O2

Half Life
5-6 hr

Drug Type
Approved Drug

# Accession No
APRD00665

CAS Registry Number
364-62-5