苯二氮䓬类

title: 名称.
content: 苯二氮䓬类,又称苯二氮䓬类药物,是一类中枢神经抑制剂,以其核心化学结构命名,苯代表苯环,䓬代表䓬环,二氮代表嵌套在䓬环上的两个氮原子。因“䓬”字为化学专用的罕见字,且读音与汉字“卓”相同,所以误用“卓”字来替代“䓬”字的情况很普遍,也有音译为“苯二氮平”的情况。
title: 作用机理.
content: 此类药物作用于体内抑制性神经递质:γ-氨基丁酸(GABA)的一种受体"GABA受体复合物"(复合物包含GABA受体,苯二氮平类药物受体和一个与GABA受体偶联的氯离子通道),而药物与受体的这种作用诱导GABA受体偶联的氯离子通道加强开放,这样会增加氯离子流入胞内的数量,产生超极化而抑制突触后电位,减少中枢某些重要神经元放电,引起中枢抑制。由苯二氮平类药物的作用机理可知,这类药物的效应是和脑内GABA水平密切相关的,如果脑内GABA水平较高,则此类药物的效应会更加明显。
title: 不良反应.
content: 催眠剂量的此类药物可引起眩晕、困倦、乏力、精细运动不协调等不良反应大剂量应用会造成共济失调、运动能力障碍、皮疹、白血球减少及暂时性记忆缺失,久服会引起耐受和依赖。  依赖
title: 发展历史.
content: 此类药物是近40年来发展起来的,最早的苯二氮平类药物是1960年用于临床的氯氮䓬,此后人们通过消除与生理活性无关的基团,和对分子结构中活性较高的部分进行拼环等改造,开发出了副作用更小,在体内更稳定的苯二氮平类新药,其中的地西泮又名安定,是目前临床应用较多的。

Summary: 苯二氮䓬类药物(、䓬/zhuó/),又译苯二氮平,是一种精神药物,其核心化学结构是一个苯环和一个䓬环。第一种此类药物是氯氮䓬(利眠宁),由Leo Sternbach在1955年偶然发现,后来由罗氏制药生产销售,罗氏制药于1963年开始上市销售地西泮(安定)。 在1977年,苯二氮䓬类药物已是全球最高处方量的药物。

Benzodiazepine: Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. The first such drug, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955, and made available in 1960 by Hoffmann–La Roche, which, since 1963, has also marketed the benzodiazepine diazepam (Valium). In 1977 benzodiazepines were globally the most prescribed medications. They are in the family of drugs commonly known as minor tranquilizers. Benzodiazepines enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA receptor, resulting in sedative, hypnotic (sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties. High doses of many shorter-acting benzodiazepines may also cause anterograde amnesia and dissociation. These properties make benzodiazepines useful in treating anxiety, insomnia, agitation, seizures, muscle spasms, alcohol withdrawal and as a premedication for medical or dental procedures. Benzodiazepines are categorized as either short, intermediary, or long-acting. Short- and intermediate-acting benzodiazepines are preferred for the treatment of insomnia; longer-acting benzodiazepines are recommended for the treatment of anxiety. Benzodiazepines are generally viewed as safe and effective for short-term use, although cognitive impairment and paradoxical effects such as aggression or behavioral disinhibition occasionally occur. A minority of people can have paradoxical reactions such as worsened agitation or panic. Benzodiazepines are also associated with increased risk of suicide. Long-term use is controversial because of concerns about decreasing effectiveness, physical dependence, withdrawal, and an increased risk of dementia and cancer. In the long-term, stopping benzodiazepines often leads to improved physical and mental health. The elderly are at an increased risk of both short- and long-term adverse effects, and as a result, all benzodiazepines are listed in the Beers List of inappropriate medications for older adults. There is controversy concerning the safety of benzodiazepines in pregnancy. While they are not major teratogens, uncertainty remains as to whether they cause cleft palate in a small number of babies and whether neurobehavioural effects occur as a result of prenatal exposure; they are known to cause withdrawal symptoms in the newborn.