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帕金森病持续口服治疗期间溴隐亭的药代动力学

Pharmacokinetics of bromocriptine during continuous oral treatment of Parkinson's disease.

作者信息

Friis M L, Grøn U, Larsen N E, Pakkenberg H, Hvidberg E F

出版信息

Eur J Clin Pharmacol. 1979 May 21;15(4):275-80. doi: 10.1007/BF00618517.

Abstract

The plasma kinetics of bromocriptine (BCT), a long-acting dopamine agonist, was studied in twelve patients with Parkinson's disease, using a newly developed gas chromatographic method of analysis. Each patient received BCT for at least three weeks in a constant but different dose regimen. Concomitant treatment with 1-DOPA was not allowed. During a 6-day hospitalization period, a blood sample was taken immediately before the afternoon dose at 14.00 h (Cmin) to determine the steady-state level. On the 6th day blood samples were collected every hour during two 8 h dose intervals. The results showed a significant correlation between the mean values of the AUC and the Cmin. First order elimination kinetics appeared to be followed by BCT, at least for the plasma concentrations commonly found. Considerable inter-individual variation was demonstrated both for the dose/plasma concentration ratio and for calculated plasma clearances. No serious side-effects were observed during the investigation.

摘要

采用新开发的气相色谱分析法,对12例帕金森病患者的长效多巴胺激动剂溴隐亭(BCT)的血浆动力学进行了研究。每位患者以恒定但不同的剂量方案接受BCT治疗至少3周。不允许同时使用左旋多巴治疗。在为期6天的住院期间,于下午14:00服用剂量前即刻采集血样(Cmin)以确定稳态水平。在第6天,在两个8小时的给药间隔内每小时采集血样。结果显示,AUC平均值与Cmin之间存在显著相关性。至少在常见的血浆浓度范围内,BCT似乎遵循一级消除动力学。剂量/血浆浓度比和计算所得的血浆清除率均显示出相当大的个体间差异。研究期间未观察到严重的副作用。

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