Bradshaw J J, Ivanetich K M
Anesth Analg. 1984 Sep;63(9):805-13.
Isoflurane is metabolized by both rat and human hepatic microsomal cytochrome P-450 in vitro to fluoride ion and organofluorine metabolites. The forms of rat liver microsomal cytochrome P-450 induced by phenobarbital and pregnenolone-16 alpha-carbonitrile appear to be involved in the metabolism of isoflurane, while the forms induced by beta-naphthoflavone do not. Different pathways are favored for the metabolism of isoflurane by rat and by human liver microsomes: trifluoroacetaldehyde appears to be produced from isoflurane by rat liver microsomal cytochrome P-450, while trifluoroacetate or other nonvolatile fluorinated metabolites were not. The trifluoroacetaldehyde so produced binds tightly to microsomal constituents. Human liver microsomes converted isoflurane extensively to nonvolatile fluorinated products, one of which appears to be trifluoroacetate. The proposed pathways for the metabolism of isoflurane are considered in view of the above results.
异氟烷在体外经大鼠和人肝微粒体细胞色素P - 450代谢为氟离子和有机氟代谢产物。苯巴比妥和孕烯醇酮-16α-腈诱导的大鼠肝微粒体细胞色素P - 450形式似乎参与异氟烷的代谢，而β-萘黄酮诱导的形式则不参与。大鼠和人肝微粒体对异氟烷的代谢倾向于不同途径：大鼠肝微粒体细胞色素P - 450似乎能使异氟烷产生三氟乙醛，而不会产生三氟乙酸盐或其他非挥发性氟化代谢产物。如此产生的三氟乙醛与微粒体成分紧密结合。人肝微粒体将异氟烷大量转化为非挥发性氟化产物，其中一种似乎是三氟乙酸盐。根据上述结果对所提出的异氟烷代谢途径进行了探讨。
