Mephedrone is a popular synthetic cathinone, known for its psychostimulant effects. At present, there is no data available on the pharmacokinetics of mephedrone and its metabolites in concurrently collected whole blood and plasma samples after a controlled intranasal administration to healthy volunteers. In this study, six healthy male volunteers nasally insufflated 100 mg of pure mephedrone hydrochloride (Day 1). Whole blood and plasma samples were collected at different timepoints after the administration and were analysed for the presence of mephedrone and its metabolites, dihydro-mephedrone (DHM), nor-mephedrone (NOR), hydroxytolyl-mephedrone (HYDROXY), 4-carboxy-mephedrone (4-CARBOXY) and dihydro-nor-mephedrone (DHNM), by validated liquid chromatography–tandem mass spectrometry methods. All analytes were detected in whole blood and plasma for 6 h post administration, with mephedrone and NOR also being detectable on Day 2 in some participants. 4-CARBOXY, followed by NOR, were the most abundant metabolites in both matrices. Compared to other psychostimulants, mephedrone showed rapid absorption (mean T_max of 52.5 ± 20.7 min in plasma and 55.0 ± 18.2 min in whole blood) and elimination (mean t_1/2 of 1.98 ± 0.30 h in plasma and 2.12 ± 0.33 h in whole blood). In addition, statistical analysis showed that median whole blood to plasma distribution ratios, reported here for the first time, were statistically different from 1 (unity) for mephedrone (median: 1.11), DHM (median: 1.30) and NOR (median: 0.765). It is hoped that the study will aid forensic and clinical toxicologists in detection, identification and interpretation of cases associated with mephedrone use.

中文翻译：

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健康志愿者经鼻内控制给药后全血和血浆中甲氧麻黄酮及其代谢物的药代动力学。

甲氧麻黄酮是一种流行的合成卡西酮，以其精神兴奋作用而闻名。目前，尚无关于对健康志愿者进行受控鼻内给药后同时采集的全血和血浆样品中甲氧麻黄酮及其代谢物的药代动力学数据。在这项研究中，六名健康男性志愿者向鼻腔吹入了 100 毫克纯盐酸甲氧麻黄酮（第 1 天）。在给药后的不同时间点收集全血和血浆样本，并分析甲氧麻黄酮及其代谢物二氢甲氧麻黄酮 (DHM)、去甲甲氧麻黄酮 (NOR)、羟甲苯基甲氧麻黄酮 (HYDROXY)、4-羧基- Mephedrone (4-CARBOXY) 和 dihydro-nor-mephedrone (DHNM)，通过经过验证的液相色谱-串联质谱法。在给药后 6 小时内在全血和血浆中检测到所有分析物，在第 2 天也可检测到一些参与者的甲氧麻黄酮和 NOR。4-羧基，其次是 NOR，是两种基质中最丰富的代谢物。与其他精神兴奋剂相比，甲氧麻黄酮显示出快速吸收（平均 T血浆中_最长52.5 ± 20.7 分钟，全血中 55.0 ± 18.2 分钟）和消除（血浆中 1.98 ± 0.30 小时和全血中 2.12 ± 0.33 小时的平均 t _1/2）。此外，统计分析显示，此处首次报告的全血与血浆分布比率中位数在统计学上不同于甲氧麻黄酮（中位数：1.11）、DHM（中位数：1.30）和 NOR（中位数：0.765）的 1（单位） ）。希望这项研究将有助于法医和临床毒理学家检测、识别和解释与使用甲氧麻黄酮相关的病例。