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苯二氮(艹卓)类药物(BZS)早在70年代初就应用于临床,目前其衍生物的发展已不下十多种,且应用更为广泛。特别近年来,对BZS的基础和临床药理学的研究有了新进展,无疑也为麻醉期间的应用,提供了理论的依据。 1977年提出,在大脑内存在着BZS受体。尽管体内其它器官也可有BZS受体,但其密度远低于大脑皮质与边缘-前脑区域,且外周的BZS受体与药物的结合弱。BZS受体的分布状况和亲和力,与药效密切相关。并认为BZS受体是γ-氨基丁酸(GABA)受体复合物的一部分,从而影响氯离子流入细胞内或向细胞外转移,后者则具有决定性的“换能器”的作用。
Benzodiazepines (benzodiazepines) drugs (BZS) as early as the early 70s applied to clinical, the current development of its derivatives no less than a dozen, and more widely used. In recent years, the research on BZS basic and clinical pharmacology has made new progress, which undoubtedly also provides theoretical basis for the application during anesthesia. In 1977, BZS receptors were present in the brain. Although other organs in the body may also have BZS receptors, their density is much lower than that of the cerebral cortex and marginal-forebrain regions, and peripheral BZS receptors are weakly bound to drugs. BZS receptor distribution and affinity, and closely related to efficacy. The BZS receptor is thought to be part of the GABA receptor complex that affects the influx of chloride ions into or out of cells, the latter having a decisive “transducer” effect.