Metoclopramide plasma levels following oral administration of high doses for prophylaxis of emesis in cytostatic therapy
Vergin, H.; Köhler, M.; Senn, H.J.
Arzneimittel-Forschung 34(11): 1595-1597
1984
ISSN/ISBN: 0004-4172 PMID: 6543137 Document Number: 231928
To investigate the effectiveness of high oral doses of the antiemetic agent 4-amino-5-chloro-N-(2-diethyl-aminoethyl)-2-methoxybenzamide (metoclopramide, MCP, Gastrosil) against nausea and vomiting induced by certain cyostatic drugs, blood was withdrawn repeatedly from 9 patients; MCP plasma levels were then determined. Patients received 3 X 50 mg MCP-hydrochloride tablets in intervals of 4 h. Plasma levels determined from 7 patients were as follows: 173 ng/ml 1 h following the first dose of MCP 235 ng/ml 1 h following the second dose and finally 265 ng/ml following the third dose. Using the oral MCP dosage regimen presented in this study, high and relatively constant MCP plasma concentrations without undesired peak levels could be achieved.