Wilkinson G R, Shand D G
Clin Pharmacol Ther. 1975 Oct;18(4):377-90. doi: 10.1002/cpt1975184377.
A physiological approach has been developed recognizing that hepatic blood flow, the activity of the overall elimination process (intrinsic clearance), drug binding in the blood, and the anatomical arrangement of the hepatic circulation are the major biological determinants of hepatic drug clearance. This approach permits quantitative prediction of both the unbound and total drug concentration/time relationships in the blood after intravenous and oral administration, and any changes that may occur as a result of alterations in the above biological parameters. These considerations have led to a classification of drug metabolism based on the hepatic extraction ratio. The proposed classification allows prediction and interpretation of the effects of individual variations in drug-metabolizing activity, route of administration, pharmacokinetic interactions, and disease states on hepatic drug elimination.
已经开发出一种生理学方法,该方法认识到肝血流量、整体消除过程的活性(内在清除率)、血液中的药物结合以及肝循环的解剖结构是肝药物清除率的主要生物学决定因素。这种方法允许定量预测静脉内和口服给药后血液中游离药物和总药物浓度/时间的关系,以及由于上述生物学参数的改变可能发生的任何变化。这些考虑因素导致了基于肝提取率的药物代谢分类。所提出的分类允许预测和解释药物代谢活性、给药途径、药代动力学相互作用和疾病状态的个体差异对肝药物消除的影响。