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抗焦虑/镇静药物的合理使用。

Rational use of anxiolytic/sedative drugs.

作者信息

Lader M, Petursson H

出版信息

Drugs. 1983 May;25(5):514-28. doi: 10.2165/00003495-198325050-00004.

Abstract

The benzodiazepines are the most effective, safest, and most widely used antianxiety drugs. As a class of drugs, there are few major differences between the various benzodiazepine derivatives. The main distinguishing features are different plasma half-lives and the presence or absence of pharmacologically active metabolites. Plasma half-lives vary considerably, from 2 to 3 hours to more than 100 hours. All benzodiazepines are equally effective in the short term management of anxiety and insomnia, and their classification into 'anxiolytics' and 'hypnotics' is not justified. There are numerous other indications for benzodiazepine use, such as muscle spasm in osteoarthritic conditions, and acute alcohol withdrawal, but the benzodiazepines have no antidepressive or analgesic effects. While there is no good evidence for their long term efficacy in the treatment of anxiety and insomnia, the benzodiazepines are more effective and safer than their main predecessors, the barbiturates. Some of the benzodiazepines, particularly those with long plasma half-lives which are commonly used as hypnotics, have a prolonged duration of action and cause marked 'hang-over' effects. Alcohol enhances the effects of these drugs, and thus can also increase their side effects. Adversely effects such as oversedation, tremor, ataxia and confusion are much more common in elderly patients. Ever since the benzodiazepines were first marketed 20 years ago their use has increased rapidly, and it is now estimated that between 12 and 16% of the adult population in developed countries use tranquillisers at some time each year. However, their overall use has probably diminished somewhat in the last few years. Although their indications are very common, it is possible that some of this extensive usage may be the result of dependence. Until recently, published reports of such dependence were comparatively few. However, withdrawal symptoms have now been demonstrated in a substantial proportion of patients on long term, normal dose benzodiazepine treatment. The abstinence syndrome usually lasts for 8 to 10 days, and is characterised by insomnia, anxiety, loss of appetite and bodyweight, tremor, perspiration, and a host of perceptual disturbances. More serious developments such as epileptic fits and psychosis are probably infrequent during withdrawal from therapeutic doses. The overall incidence of benzodiazepine dependence remains unknown.

摘要

苯二氮䓬类药物是最有效、最安全且使用最广泛的抗焦虑药物。作为一类药物,各种苯二氮䓬衍生物之间几乎没有重大差异。主要的区别特征在于不同的血浆半衰期以及是否存在药理活性代谢物。血浆半衰期差异很大,从2至3小时到超过100小时不等。所有苯二氮䓬类药物在焦虑和失眠的短期治疗中效果相同,将它们分类为“抗焦虑药”和“催眠药”是不合理的。苯二氮䓬类药物还有许多其他适应证,如骨关节炎病症中的肌肉痉挛以及急性酒精戒断,但苯二氮䓬类药物没有抗抑郁或镇痛作用。虽然没有充分证据表明它们在治疗焦虑和失眠方面的长期疗效,但苯二氮䓬类药物比其主要前身巴比妥类药物更有效且更安全。一些苯二氮䓬类药物,特别是那些血浆半衰期长且常用作催眠药的药物,作用持续时间延长,并会引起明显的“宿醉”效应。酒精会增强这些药物的作用,因此也会增加其副作用。诸如过度镇静、震颤、共济失调和意识模糊等不良反应在老年患者中更为常见。自从苯二氮䓬类药物20年前首次上市以来,其使用迅速增加,现在估计发达国家每年有12%至16%的成年人口在某些时候使用镇静剂。然而,在过去几年中其总体使用量可能有所减少。虽然它们的适应证非常常见,但这种广泛使用可能部分是依赖的结果。直到最近,关于这种依赖的已发表报告相对较少。然而,现在已证实在接受长期、正常剂量苯二氮䓬类药物治疗的相当一部分患者中会出现戒断症状。戒断综合征通常持续8至10天,其特征为失眠、焦虑、食欲不振和体重减轻、震颤、出汗以及一系列感知障碍。在从治疗剂量撤药期间,癫痫发作和精神病等更严重的情况可能很少见。苯二氮䓬类药物依赖的总体发生率仍然未知。

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