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首页> 外文期刊>Journal of mass spectrometry: JMS >Detection and identification of the designer benzodiazepine flubromazepam and preliminary data on its metabolism and pharmacokinetics
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Detection and identification of the designer benzodiazepine flubromazepam and preliminary data on its metabolism and pharmacokinetics

机译：设计师二苯并二氮杂氟溴西epa的检测和鉴定及其代谢和药代动力学的初步数据

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摘要

The appearance of pyrazolam in Internet shops selling 'research chemicals' in 2012 marked the beginning of designer benzodiazepines being sold as recreational drugs or 'self medication'. With recent changes in national narcotics laws in many countries, where two uncontrolled benzodiazepines (phenazepam and etizolam), which were marketed by pharmaceutical companies in some countries, were scheduled, clandestine laboratories seem to turn to poorly characterized research drug candidates as legal substitutes. Following the appearance of pyrazolam, it comes with no surprise that recently, flubromazepam (7-bromo-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one), a second designer benzodiazepine, was offered on the market. In this article, this new compound was characterized using nuclear magnetic resonance, gas chromatography- mass spectrometry (GC-MS), liquid chromatography-mass spectrometry (LC-MS/MS) and liquid chromatography quadrupole time-of-flight MS (LC-Q-ToF-MS). Additionally, a study was carried out, in which one of the authors consumed 4mg of flubromazepam to gain preliminary data on the pharmacokinetic properties and the metabolism of this compound. For this purpose, serum as well as urine samples were collected for up to 31 days post-ingestion and analyzed applying LC-MS/MS and LC-Q-ToF-MS techniques. On the basis of this study, flubromazepam appears to have an extremely long elimination half-life of more than 100 h. One monohydroxylated compound and the debrominated compound could be identified as the predominant metabolites, the first allowing a detection of a consumption for up to 28 days post-ingestion when analyzing urine samples in our case. Additionally, various immunochemical assays were evaluated, showing that the crossreactivity of the used assay seems not to be sufficient for safe detection of the applied dose in urine samples, bearing the risk that it could be misused in drug-withdrawal settings or in other circumstances requiring regular drug testing. Furthermore, it may be used in drug-facilitated crimes without being detected.
机译：吡唑仑在2012年在销售“研究化学品”的互联网商店中的出现标志着设计师苯二氮卓类药物以休闲药物或“自用药”形式出售的开始。随着许多国家的国家麻醉法的最新变化，一些国家的制药公司在市场上计划了两种不受管制的苯二氮卓类药物（苯那西m和依替唑仑），秘密实验室似乎转向了特性不佳的研究药物候选物作为合法替代品。吡唑仑唑出现后，毫不奇怪，最近，氟溴西epa（7-溴-5-（2-氟苯基）-1,3-二氢-2H-1,4-苯并二氮杂-2-一）是第二位设计师苯二氮卓在市场上有售。本文使用核磁共振，气相色谱-质谱（GC-MS），液相色谱-质谱（LC-MS / MS）和液相色谱四极杆飞行时间质谱（LC-MS）对这种新化合物进行了表征Q-ToF-MS）。此外，进行了一项研究，其中一位作者食用了4mg氟溴西epa，以获得该化合物的药代动力学特性和代谢的初步数据。为此，在摄入后长达31天的时间内收集血清和尿液样本，并使用LC-MS / MS和LC-Q-ToF-MS技术进行分析。根据这项研究，氟溴西epa似乎具有超过100小时的极长消除半衰期。一种单羟基化的化合物和脱溴的化合物可以被确定为主要的代谢产物，在我们的案例中分析尿样时，第一种可以检测到摄入后长达28天的消耗量。此外，还评估了各种免疫化学测定法，表明所用测定法的交叉反应性似乎不足以安全检测尿液样品中的所施加剂量，并带有可能在戒断环境中或在其他情况下可能被误用的风险定期进行药物测试。此外，它可能被用于毒品犯罪而不被发现。

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