Drug Groups

approved; investigational

Description

A dopamine D2 antagonist that is used as an antiemetic. [PubChem]

Indication

For the treatment of gastroesophageal reflux disease (GERD). It is also used in treating nausea and vomiting, and to increase gastric emptying.

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.

Toxicity

Oral, mouse LD₅₀: 280 mg/kg. Signs of overdose include drowsiness, disorientation, and extrapyramidal reactions.

Affected Organisms

Biotransformation

Hepatic

Absorption

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

Half Life

5-6 hr

Protein Binding

30%

Elimination

Approximately 85% of the radioactivity of an orally administered dose appears in the urine within 72 hours.

Distribution

* 4.4±0.65 L/kg

Clearance

* 0.67 +/- 0.14 L/hr/kg [infants (0.9-5.4 months) with gastroesophageal reflux (GER)]

References

External Links