Busby M, Lesko L J
Drug Metab Dispos. 1987 Mar-Apr;15(2):204-6.
The effects of chloramphenicol, a potent enzyme inhibitor, on the pharmacokinetics of theophylline were investigated in Sprague-Dawley rats. Chloramphenicol treatment, 75 mg/day intravenously for 3 days, significantly (p less than 0.05) decreased the plasma clearance of theophylline by 31% with no apparent effects on the volume of distribution (0.97 liter/kg). The elimination half-life in chloramphenicol treated rats (N = 6) was 4.8 hr, significantly (p less than 0.05) longer than the corresponding half-life, 3.4 hr, in control rats (N = 6). It appears that chloramphenicol has a marked inhibitory effect on the activity of the cytochrome P-450-dependent mixed function oxidase liver microsome system responsible for the oxidation and demethylation of theophylline.
在斯普拉格-道利大鼠中研究了强效酶抑制剂氯霉素对茶碱药代动力学的影响。静脉注射氯霉素，剂量为75毫克/天，持续3天，显著（p小于0.05）使茶碱的血浆清除率降低了31%，而对分布容积（0.97升/千克）无明显影响。氯霉素处理组大鼠（N = 6）的消除半衰期为4.8小时，显著（p小于0.05）长于对照组大鼠（N = 6）相应的半衰期3.4小时。看来氯霉素对负责茶碱氧化和去甲基化的细胞色素P-450依赖性混合功能氧化酶肝微粒体系统的活性有显著抑制作用。
