Nishikawa T, Kamijo Y, Kondo R, Sugie H, Kurihara K, Okuda T, Matsumoto N, Okada Y, Ohtani H
Department of Clinical Pathology, Kitasato University School of Medicine, Kanagawa, Japan.
J Anal Toxicol. 2000 Nov-Dec;24(8):691-5. doi: 10.1093/jat/24.8.691.
Bromoisovalerylurea (bromisovalum) is a sedative-hypnotic given orally as a racemic mixture of optical isomers (i.e., (+)- and (-)-enantiomer) and frequently taken in overdose in order to commit suicide. Sera from 16 overdosed subjects were analyzed for each enantiomer by high-performance liquid chromatography on chiral stationary phases. The (+)-enantiomer concentration was lower than the (-)-enantiomer concentration in all specimens, that is, the ratio of the (+)-enantiomer to the total concentration ranged from about 50% to 0%. The ratio of the (+)-enantiomer was continuously decreasing in each subject. The data indicate that the drug in gastrointestinal tract was absorbed into blood nonstereoselectively and that the drug in blood was eliminated stereoselectively. The enantioselective determination of this drug will give useful information on absorption and elimination.
溴异戊酰脲(溴米索伐)是一种口服的镇静催眠药,以光学异构体(即(+)-和(-)-对映体)的外消旋混合物形式给药,常因过量服用而用于自杀。通过在手性固定相上进行高效液相色谱分析,对16名过量服药受试者的血清中每种对映体进行了检测。在所有样本中,(+)-对映体浓度均低于(-)-对映体浓度,即(+)-对映体与总浓度的比值范围约为50%至0%。在每个受试者中,(+)-对映体的比例持续下降。数据表明,胃肠道中的药物以非立体选择性方式吸收入血,而血液中的药物以立体选择性方式消除。该药物的对映体选择性测定将为吸收和消除提供有用信息。