咪达唑仑和其他苯二氮卓类。

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Olkkola KT, Ahonen J

咪达唑仑和其他苯二氮卓类。

Handb Exp杂志。2008;(182):335 - 60。doi: 10.1007 / 978 - 3 - 540 - 74806 - 9 - _16。

PubMed ID

18175099 (在PubMed

]

文摘

苯二氮卓类的行为是由于神经的增强作用介导的抑制γ-氨基丁酸(GABA)。几乎所有的苯二氮卓类结果从他们的行动ionotropic GABA (A)受体在中枢神经系统。苯二氮卓类不激活GABA (A)直接但他们需要GABA受体。的主要影响苯二氮卓类镇静,催眠,减少焦虑,顺行性遗忘,集中介导肌肉放松和anti-convulsant活动。除了他们的行动对中枢神经系统、苯二氮卓类通气镇静剂的效果存在剂量依赖的相关性,它们也造成适度降低动脉血压和心率的增加导致全身血管阻力降低。四苯二氮卓类,广泛应用于临床麻醉,受体激动剂咪达唑仑、安定、氯羟去甲安定和拮抗剂flumazenil。咪达唑仑、安定和flumazenil代谢的细胞色素P450 (CYP)由葡糖苷酸酶和接合而直接经历葡糖苷酸结合氯羟去甲安定。CYP3A4是重要的生物转化的咪达唑仑和安定。CYP2C19安定的生物转化是很重要的。肝脏和肾脏功能障碍只有轻微影响的药物氯羟去甲安定但他们慢下来的消除其他苯二氮平类药物用于临床麻醉。 The duration of action of all benzodiazepines is strongly dependent on the duration of their administration. Based on clinical studies and computer simulations, midazolam has the shortest recovery profile followed by lorazepam and diazepam. Being metabolized by CYP enzymes, midazolam and diazepam have many clinically significant interactions with inhibitors and inducers of CYP3A4 and 2C19. In addition to pharmacokinetic interactions, benzodiazepines have synergistic interactions with other hypnotics and opioids. Midazolam, diazepam and lorazepam are widely used for sedation and to some extent also for induction and maintenance of anaesthesia. Flumazenil is very useful in reversing benzodiazepine-induced sedation as well as to diagnose or treat benzodiazepine overdose.

DrugBank数据引用了这篇文章

药物

Flumazenil

药物酶

药物	酶	类	生物	药理作用	行动
氯羟去甲安定	细胞色素P450 3 a4	蛋白质	人类	没有	底物	细节