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[大剂量口服甲氧氯普胺预防细胞毒性疗法中呕吐时的血浆水平]

[Metoclopramide plasma levels following oral administration of high doses for prophylaxis of emesis in cytostatic therapy].

作者信息

Vergin H, Köhler M, Senn H J

出版信息

Arzneimittelforschung. 1984;34(11):1595-7.

PMID:6543137
Abstract

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(metoclopramide, MCP, Gastrosil) against nausea and vomiting induced by certain cyostatic drugs, blood was withdrawn repeatedly from 9 patients; MCP plasma levels were then determined.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.

摘要

为研究口服高剂量止吐药4-氨基-5-氯-N-(2-二乙氨基乙基)-2-甲氧基苯甲酰胺(胃复安,MCP,胃硅酮)对某些细胞抑制剂所致恶心和呕吐的疗效,对9例患者反复采血;随后测定MCP血浆水平。患者每隔4小时服用3片50毫克盐酸MCP片剂。7例患者测定的血浆水平如下:首次服用MCP后1小时为173纳克/毫升,第二次服用后1小时为235纳克/毫升,第三次服用后最终为265纳克/毫升。采用本研究中提出的口服MCP给药方案,可实现较高且相对恒定的MCP血浆浓度,而不会出现不期望的峰值水平。

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