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新型设计苯二氮䓬类药物:临床进展与不良反应综述

Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse Effects.

作者信息

Edinoff Amber N, Nix Catherine A, Odisho Amira S, Babin Caroline P, Derouen Alyssa G, Lutfallah Salim C, Cornett Elyse M, Murnane Kevin S, Kaye Adam M, Kaye Alan D

机构信息

Department of Psychiatry, Massachusetts General Hospital, Harvard School of Medicine, Boston, MA 02114, USA.

Department of Psychiatry and Behavioral Medicine, Louisiana State University Health Shreveport, Shreveport, LA 71103, USA.

出版信息

Neurol Int. 2022 Aug 22;14(3):648-663. doi: 10.3390/neurolint14030053.

Abstract

As tranquilizers, benzodiazepines have a wide range of clinical uses. Recently, there has been a significant rise in the number of novel psychoactive substances, including designer benzodiazepines. Flubromazolam(8-bromo-6-(2-fluorophenyl)-1-methyl-4-[1,2,4]triazolo[4,3-a][1,4]benzodiazeZpine) is a triazolo-analogue of flubromazepam. The most common effects noted by recreational users include heavy hypnosis and sedation, long-lasting amnesia, and rapid development of tolerance. Other effects included anxiolysis, muscle-relaxing effects, euphoria, loss of control, and severe withdrawals. Clonazolam, or 6-(2-chlorophenyl)-1-methyl-8-nitro-4H-[1,2,4]triazolo[4,3-α]-[1,4]-benzodiazepine, is a triazolo-analog of clonazepam. It is reported to be over twice as potent as alprazolam. Deschloroetizolam (2-Ethyl-9-methyl-4-phenyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) is part of the thienodiazepine drug class, which, like benzodiazepines, stimulates GABA-A receptors. Meclonazepam ((3S)-5-(2-chlorophenyl)-3-methyl-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one) is a designer benzodiazepine with additional anti-parasitic effects. Although it has proven to be an efficacious therapy for schistosomiasis, its sedative side effects have prevented it from being marketed as a therapeutic agent. The use of DBZs has been a subject of multiple recent clinical studies, likely related to increasing presence and availability on the internet drug market and lack of regulation. Many studies have aimed to identify the prevalence of DBZs and their effects on those using them. This review discussed these designer benzodiazepines and the dangers and adverse effects that the clinician should know.

摘要

作为镇静剂,苯二氮䓬类药物有广泛的临床用途。最近,包括设计型苯二氮䓬类药物在内的新型精神活性物质的数量显著增加。氟溴唑仑(8-溴-6-(2-氟苯基)-1-甲基-4-[1,2,4]三唑并[4,3-a][1,4]苯并二氮杂䓬)是氟溴西泮的三唑类似物。娱乐性使用者指出的最常见效果包括深度催眠和镇静、持久失忆以及耐受性的快速形成。其他效果包括抗焦虑、肌肉松弛作用、欣快感、失控感和严重的戒断反应。氯硝唑仑,即6-(2-氯苯基)-1-甲基-8-硝基-4H-[1,2,4]三唑并[4,3-α]-[1,4]-苯并二氮杂䓬,是氯硝西泮的三唑类似物。据报道其效力是阿普唑仑的两倍多。去氯乙替唑仑(2-乙基-9-甲基-4-苯基-6H-噻吩并[3,2-f][1,2,4]三唑并[4,3-a][1,4]二氮杂䓬)属于噻吩二氮䓬类药物,与苯二氮䓬类药物一样,刺激GABA-A受体。美克洛仑((3S)-5-(2-氯苯基)-3-甲基-7-硝基-1,3-二氢-1,4-苯并二氮杂䓬-2-酮)是一种具有额外抗寄生虫作用的设计型苯二氮䓬类药物。尽管它已被证明是治疗血吸虫病的有效疗法,但其镇静副作用使其无法作为治疗药物上市。设计型苯二氮䓬类药物的使用一直是近期多项临床研究的主题,这可能与它们在互联网毒品市场上的存在和可得性增加以及缺乏监管有关。许多研究旨在确定设计型苯二氮䓬类药物的流行情况及其对使用者的影响。本综述讨论了这些设计型苯二氮䓬类药物以及临床医生应了解的危险和不良反应。

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