Robertson M D, Drummer O H
Victorian Institute of Forensic Pathology, Monash University, South Melbourne.
J Forensic Sci. 1995 May;40(3):382-6.
Studies were undertaken to determine the possible role of enteric bacteria in the postmortem bioconversion of the nitrobenzodiazepines flunitrazepam, clonazepam, and nitrazepam. Flunitrazepam, clonazepam, and nitrazepam were completely metabolized in blood in the presence of eight species of enteric bacteria to their respective 7-amino-metabolites. The rates of metabolism, at 37 degrees C, ranged from 0.1 ng/mL/min for Streptococcus faecalis to 8.8 ng/mL/min for Clostridium perfringens. The rate of conversion was reduced to 87% by a combination of 0.7% (w/v) sodium fluoride and potassium oxalate, and almost completely inhibited (96%) by 1% (w/v) sodium fluoride. pH had variable effects on the rate of metabolic bioconversion of nitrobenzodiazepines, while increasing temperatures were found to generally increase the rate of nitrobenzodiazepine bioconversion. These data support the proposal that bacteria may mediate postmortem bioconversion of the nitrobenzodiazepines.
开展了多项研究以确定肠道细菌在硝基苯二氮䓬类药物氟硝西泮、氯硝西泮和硝西泮死后生物转化中可能发挥的作用。在八种肠道细菌存在的情况下，氟硝西泮、氯硝西泮和硝西泮在血液中完全代谢为各自的7-氨基代谢物。在37摄氏度时，代谢速率范围从粪链球菌的0.1纳克/毫升/分钟到产气荚膜梭菌的8.8纳克/毫升/分钟。0.7%（w/v）的氟化钠和草酸钾组合可使转化率降至87%，而1%（w/v）的氟化钠几乎可完全抑制（96%）转化率。pH值对硝基苯二氮䓬类药物的代谢生物转化率有不同影响，而发现温度升高通常会增加硝基苯二氮䓬类药物的生物转化率。这些数据支持了细菌可能介导硝基苯二氮䓬类药物死后生物转化的观点。
