Leopold G
Arzneimittelforschung. 1977 Feb;27(2A):241-9.
Metabolism or decay of a drug prior to, during or shortly after its enteral absorption necessarily reduces the amount of unchanged drug reaching the systemic circulation. This influences the pharmacokinetic properties of a drug and is called first-pass effect. Every drug metabolized in the liver theoretically undergoes a first-pass metabolism after enteral application. Whether it results in a pharmacokinetically obvious first-pass effect depends on extent and rate of this metabolic step. The pharmacokinetic relevance of a first-pass effect does not automatically mean also its therapeutic relevance. For the assessment of the therapeutic relevance of a first-pass effect, extent and slope of its dose-effect curve in man and the therapeutic index of a drug must be taken into accounts.
药物在肠内吸收之前、期间或之后不久发生的代谢或降解必然会减少进入体循环的未变化药物量。这会影响药物的药代动力学性质,被称为首过效应。理论上,每种在肝脏中代谢的药物经肠内给药后都会经历首过代谢。其是否会导致药代动力学上明显的首过效应取决于该代谢步骤的程度和速率。首过效应的药代动力学相关性并不自动意味着其治疗相关性。为了评估首过效应的治疗相关性,必须考虑其在人体中的剂量-效应曲线的程度和斜率以及药物的治疗指数。