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地西泮和溴替唑仑的血药浓度及脑电图效应

Blood levels and electroencephalographic effects of diazepam and bromazepam.

作者信息

Fink M, Weinfeld R E, Schwartz M A, Conney A H

出版信息

Clin Pharmacol Ther. 1976 Aug;20(2):184-91. doi: 10.1002/cpt1976202184.

DOI:10.1002/cpt1976202184
PMID:7375
Abstract

Blood levels and electroencephalographic (EEG) data were collected for 2 hr after single oral doses of bromazepam (9 mg), diazepam (10 mg), and placebo in 13 male adult volunteers. Both drugs caused an increase in beta activity (above 13 Hz) and a decrease in alpha activity (9 to 11 Hz) in the EEG. Blood levels of 100 ng/ml of diazepam or 50 ng/ml of bromazepam were associated with significant changes in EEG beta activity. Temporal changes in the EEG after administration of diazepam or bromazepam paralleled development of plasma levels of these drugs. Although a weakly significant correlation was found between measurable diazepam blood levels and amount of increased EEG beta activity, the relationship between measurable bromazepam blood levels and the degree of EEG changes was not significant. Quantitative EEG is a sensitive continuous response measure, useful in defining cerebral activity, response latency, and relative potency of psychoactive benzodiazepines.

摘要

对13名成年男性志愿者单次口服9毫克溴西泮、10毫克地西泮及安慰剂后,收集2小时的血药浓度和脑电图(EEG)数据。两种药物均导致脑电图中β波活动(高于13赫兹)增加,α波活动(9至11赫兹)减少。地西泮血药浓度达100纳克/毫升或溴西泮血药浓度达50纳克/毫升与脑电图β波活动的显著变化相关。服用地西泮或溴西泮后脑电图的时间变化与这些药物血浆浓度的变化趋势平行。尽管可测的地西泮血药浓度与脑电图β波活动增加量之间存在微弱的显著相关性,但可测的溴西泮血药浓度与脑电图变化程度之间的关系并不显著。定量脑电图是一种敏感的连续反应测量方法,有助于确定大脑活动、反应潜伏期以及精神活性苯二氮䓬类药物的相对效价。

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