Williams K M
Clin Pharmacol Ther. 1984 Dec;36(6):817-23. doi: 10.1038/clpt.1984.262.
The kinetics of misonidazole enantiomers were followed in nine healthy subjects after a single oral dose of racemic misonidazole (1.0 gm/m2). Mean clearance of (+)-misonidazole was 14% greater than that for (-)-misonidazole and mean volume of distribution was slightly greater (3%) for the (+)-enantiomer. After treatment of four of the subjects with cimetidine, there was a small increase in (-)-misonidazole distribution volume, but there was no significant change in other kinetic parameters for either enantiomer. Phenytoin (three subjects) and phenobarbital (two subjects) increased the clearance of both enantiomers (the increase was greater for (+)-misonidazole). The use of (+)-misonidazole together with induction of metabolism may reduce the neurotoxicity associated with racemic misonidazole.
在9名健康受试者单次口服消旋米索硝唑（1.0克/平方米）后，对米索硝唑对映体的动力学进行了跟踪研究。（+）-米索硝唑的平均清除率比（-）-米索硝唑高14%，（+）-对映体的平均分布容积略大（3%）。在4名受试者用西咪替丁治疗后，（-）-米索硝唑的分布容积略有增加，但两种对映体的其他动力学参数均无显著变化。苯妥英（3名受试者）和苯巴比妥（2名受试者）增加了两种对映体的清除率（对（+）-米索硝唑的增加更大）。同时使用（+）-米索硝唑和诱导代谢可能会降低与消旋米索硝唑相关的神经毒性。
