Investigation on toxicological usefulness of synovial fluids, as an alternative matrix: postmortem distribution/redistribution of triazolam and its predominant metabolite α-hydroxytriazolam in human body fluids

Investigation on toxicological usefulness of synovial fluids, as an alternative matrix: postmortem distribution/redistribution of triazolam and its predominant metabolite α-hydroxytriazolam in human body fluids
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滑液作为替代基质的毒理学用途的研究:三唑仑及其主要代谢物 α-羟基三唑仑在人体体液中的死后分布/再分布

DOI:
10.1007/s11419-021-00604-8
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发表时间:
2021
影响因子:
2.2
通讯作者:
Hasegawa Koutaro
Hasegawa Koutaro
中科院分区:
医学4区
文献类型:
--
作者:
Wurita Amin;Suzuki Masako;Miyoshi Naotomo;Minakata Kayoko;Yamagishi Itaru;Nozawa Hideki;Hasegawa Koutaro

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苯二氮卓类药物是世界各地常用的处方药[1]。由于这些化合物通常与人脑突触膜上的γ-氨基丁酸(GABA)受体具有药理学亲和力,因此苯二氮卓类药物可对中枢神经系统产生抑制作用。此外,它们还具有放松人体肌肉的作用。因此,根据其消除半衰期和效力的差异,各种苯并二氮杂卓类药物一直被用作具有抗癫痫、抗惊厥、镇静和催眠作用的药物。特别是在法医学领域,苯二氮卓类药物也是在许多涉及意外[2]、自杀[3]、杀人[4]和药物便利犯罪(DCF)案件[5,6]的案件中最常遇到的药物之一。(8-氯-6-(邻氯苯基)-1-甲基-4 H-s-三唑并[4,3a][1,4]苯并二氮杂)已被用作治疗失眠的最有效的短效药物之一和麻醉前医疗护理中的镇静剂。其主要代谢物1-羟基三唑仑(α-羟基三唑仑)的活性估计也与母体三唑仑相同,可达到三唑仑活性的约50 - 100%[7];相反,另一种代谢物4-羟基三唑仑的活性降低[7]。与其他苯二氮卓类药物一样,
Benzodiazepine class drugs are commonly prescribed throughout the world [1]. Because these compounds generally have pharmacological affinities to γ-aminobutyric acid (GABA) receptors at synaptic membrane in human brain, benzodiazepines can exert suppressive effects to central nervous system. In addition, they also have muscle-relaxing effects in human body. Thus, various benzodiazepines have been being used for anti-epileptic, anti-convulsant, sedative and hypnotic effects as medicines, according to their differences in elimination half-life and potencies. Especially in forensic area, benzodiazepines have also been one of the most encountered drugs in many cases involved in unexpected [2], suicidal [3], homicidal [4] and drug facilitated crime (DCF) cases [5, 6].Among various types of benzodiazepines, triazolam (8-chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo [4, 3a][1, 4] benzodiazepine) have been used as one of the most potent short acting drugs for treatment of insomnia and as sedatives in pre-anesthetic medical cares. Its major metabolite 1-hydroxytriazolam (α-hydroxytriazolam) is also estimated to be as active as parent triazolam, which can reach about 50 to 100% of activity of triazolam [7]; in contrast, another metabolite 4-hydroxytriazolam has a reduced activity [7]. Like other benzodiazepines, numerous
DOI: --
发表时间: 2005
期刊:
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膝关节滑液中药物的检测[J].
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