Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic. Metoclopramide is a dopamine receptor antagonist which has been used for treatment of a variety of gastrointestinal symptoms over the last thirty years. In various countries, metoclopramide is the antiemetic drug of choice in pregnant women. Findings provide reassurance regarding the safety of metoclopramide for the fetus when the drug is given to women to relieve nausea and vomiting during pregnancy. Evidence also supports its use for gastroparesis (poor stomach emptying) and gastroesophageal reflux disease. It appears to bind to dopamine D2 receptors where it is a receptor antagonist, and is also a mixed 5-HT3 receptor antagonist/ 5-HT4 receptor agonist.
|Animal models||Male albino Swiss mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||10 mM in DMSO|
Risk of extrapyramidal side effects comparing continuous vs. bolus intravenous metoclopramide administration: a systematic review and meta-analysis of randomised controlled trials.
Cavero-Redondo I, et al. J Clin Nurs. 2015 Dec;24(23-24):3638-46. PMID: 26373874.
Antinociception by metoclopramide, ketamine and their combinations in mice.
Mohammad FK, et al. Pharmacol Rep. 2012;64(2):299-304. PMID: 22661179.
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