| Item |
Information |
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Drug Groups
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approved; investigational |
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Description
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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 |
| • |
Humans and other mammals |
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| 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 |
| • |
JUSTIN-BESANCON L, LAVILLE C: [ANTIEMETIC ACTION OF METOCLOPRAMIDE WITH RESPECT TO APOMORPHINE AND HYDERGINE.] C R Seances Soc Biol Fil. 1964;158:723-7.
[Pubmed]
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| • |
Tonini M, Candura SM, Messori E, Rizzi CA: Therapeutic potential of drugs with mixed 5-HT4 agonist/5-HT3 antagonist action in the control of emesis. Pharmacol Res. 1995 May;31(5):257-60.
[Pubmed]
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| External Links |
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