Baker M T, Bates J N, Leff S V
Department of Anesthesia, College of Medicine, University of Iowa, Iowa City 52242.
Anesth Analg. 1987 Nov;66(11):1141-7.
The structural similarity of the halothane metabolite, 2-chloro-1,1-difluoroethene (CDE), to haloethenes that are metabolized by and inactivate cytochrome P-450, suggests that CDE may undergo secondary metabolism and degrade these isozymes. This possibility was examined in hepatic microsomes by determining fluoride release and cytochrome P-450 loss due to CDE metabolism in the presence of several anesthetics. CDE alone decreased cytochrome P-450 from phenobarbital-treated rats by as much as 37%, but the addition of isoflurane or halothane to incubations containing CDE increased the loss of cytochrome P-450 nearly twofold. Fluoride release was enhanced approximately 2.5 to 3 times by halothane or isoflurane; however, fluroxene inhibited fluoride release and did not enhance the loss of cytochrome P-450. Extrapolation of these results to the clinical situation suggests that the metabolism of CDE produced during halothane anesthesia and the accompanying cytochrome P-450 loss may contribute to the inhibition of drug metabolism produced by halothane.
氟烷代谢产物2-氯-1,1-二氟乙烯(CDE)与可被细胞色素P-450代谢并使其失活的卤代乙烯结构相似,这表明CDE可能会经历二次代谢并降解这些同工酶。通过在几种麻醉剂存在的情况下,测定因CDE代谢导致的氟离子释放和细胞色素P-450损失,在肝微粒体中对这种可能性进行了研究。单独的CDE可使苯巴比妥处理的大鼠的细胞色素P-450减少多达37%,但在含有CDE的孵育体系中添加异氟烷或氟烷,可使细胞色素P-450的损失增加近两倍。氟烷或异氟烷可使氟离子释放增强约2.5至3倍;然而,氟烯抑制氟离子释放,且不会增加细胞色素P-450的损失。将这些结果外推至临床情况表明,氟烷麻醉期间产生的CDE代谢以及随之而来的细胞色素P-450损失,可能会导致氟烷对药物代谢的抑制作用。