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咪达唑仑对八名中国男性脑电图影响的药代动力学-药效学建模

Pharmacokinetic-pharmacodynamic modeling of electroencephalographic effects of midazolam in eight Chinese men.

作者信息

Lu J F, Chen G, Xiang B R, An D K

机构信息

Department of Clinical Pharmacy of Jinling Hospital, Nanjing, China.

出版信息

Zhongguo Yao Li Xue Bao. 1994 Sep;15(5):399-403.

PMID:7717060
Abstract

The effects of midazolam (Mid) on the electroencephalogram (EEG) were related to Mid concentrations in serum in 8 Chinese healthy male volunteers for the assessment of concentration-effect relationship. The total number of waves per second within the frequency range of 12-30 Hz (TNW12-30) in the central-occipital (C1-O1) lead EEG obtained by aperiodic analysis was used as EEG effect of the drug. The PK-PD parameters were calculated by PK-PD software using the sigmoid Emax model. They were: T1(2)keo = 1.3 +/- 0.9 min-1, EC50 = 254 +/- 54 micrograms.L-1, N = 2.9 +/- 0.6. E0 and Emax were calculated from the observed values, being 3.4 +/- 1.3 and 11.4 +/- 2.2 TNW12-30, respectively. Our results showed that the concentration-EEG effect relationship of Mid could be characterized in individual Chinese man using TNW12-30 as a measure of pharmacological response.

摘要

为评估浓度-效应关系,在8名中国健康男性志愿者中研究了咪达唑仑(Mid)对脑电图(EEG)的影响及其与血清中咪达唑仑浓度的关系。通过非周期分析获得的中央-枕叶(C1-O1)导联脑电图在12 - 30 Hz频率范围内每秒的总波数(TNW12-30)被用作该药物的脑电图效应。使用S形Emax模型通过PK-PD软件计算PK-PD参数。结果如下:T1(2)keo = 1.3 +/- 0.9 min-1,EC50 = 254 +/- 54微克·升-1,N = 2.9 +/- 0.6。E0和Emax根据观察值计算得出,分别为3.4 +/- 1.3和11.4 +/- 2.2 TNW12-30。我们的结果表明,以TNW12-30作为药理反应的指标,可以在中国男性个体中表征咪达唑仑的浓度-脑电图效应关系。

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