Designer Benzodiazepines: Another Class of New Psychoactive Substances
Designer Benzodiazepines: Another Class of New Psychoactive Substances
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DOI：
10.1007/164_2018_154
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发表时间：
2018-01-01
期刊：
影响因子：
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通讯作者：
Auwaerter, Volker
中科院分区：
文献类型：
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作者：
Moosmann, Bjoern;Auwaerter, Volker
苯二氮卓类药物在20世纪60年代作为医疗药物引入。它们取代了毒性更大的巴比妥类药物，巴比妥类药物当时通常用于治疗焦虑或睡眠障碍。然而，苯二氮卓类药物显示出滥用和依赖的高潜力。虽然这些药物具有很大的价值，但对这些药物的依赖是全世界关注的问题，部分原因是处方过度和容易获得。因此，通过互联网商店不受限制地低价出售苯二氮卓类药物的现象令人震惊，并对公众健康构成严重威胁。这些化合物中的大多数（例如，非那西泮和依替唑仑除外）从未在世界任何地方作为医疗药物获得许可，它们在结构上源自医用苯二氮卓类药物。秘密生产者生产新化合物的策略包括根据结构-活性关系对医学上使用的1,4-苯二氮卓类药物进行典型的结构变异，以及合成这些化合物的活性代谢物和三唑类类似物。由于它们显然是为了规避国家麻醉品法律或国际管制而设计的，它们可以被称为“设计苯二氮卓类药物”。这些化合物中的大多数，如双氮安定、氯硝唑仑和硝唑仑，已经在科学文献或专利文献中被描述过。然而，人们对它们的药理特性和使用它们的具体风险知之甚少。本章描述了设计苯二氮卓类药物的现象，并总结了药物动力学和药效学方面的现有数据以及检测它们的分析方法。
Benzodiazepines have been introduced as medical drugs in the 1960s. They replaced the more toxic barbiturates, which were commonly used for treatment of anxiety or sleep disorders at the time. However, benzodiazepines show a high potential of misuse and dependence. Although being of great value as medicines, dependence to these drugs is a concern worldwide, in part due to overprescription and easy availability. Therefore, the phenomenon of benzodiazepines sold via Internet shops without restrictions at low prices is alarming and poses a serious threat to public health. Most of these compounds (with the exception of, e.g., phenazepam and etizolam) have never been licensed as medical drugs in any part of the world and are structurally derived from medically used benzodiazepines. Strategies of clandestine producers to generate new compounds include typical structural variations of medically used 1,4-benzodiazepines based on structure-activity relationships as well as synthesis of active metabolites and triazolo analogs of these compounds. As they were obviously designed to circumvent national narcotics laws or international control, they can be referred to as "designer benzodiazepines." The majority of these compounds, such as diclazepam, clonazolam, and nitrazolam, have been described in scientific or patent literature. However, little is known about their pharmacological properties and specific risks related to their use. This chapter describes the phenomenon of designer benzodiazepines and summarizes the available data on pharmacokinetics and pharmacodynamics as well as analytical approaches for their detection.