Levine W G
Annu Rev Pharmacol Toxicol. 1978;18:81-96. doi: 10.1146/annurev.pa.18.040178.000501.
A vast number and variety of xenobiotics appear in the bile. For some this is a final excretory process, for others it is merely one step in the active enterohepatic circulation. For still others it may be a vital step in a toxicologic or carcinogenic process. During the past ten years there has been a steady accumulation of observations in the literature bearing on biliary excretion mechanisms. Phenomena such as molecular weight thresholds and other aspects of species variation as well as response to inducing agents are described in many papers and much speculation is available as to their meaning. The clinical significance of this work is still somewhat dependent upon results obtained from lower animals, although studies occasionally appear on patients who have temporary bile drainage subsequent to surgery. It is important that efforts persist in obtaining data in humans since extrapolation from lower animals in the area of drug disposition is often precarious. The basic physiological and biochemical mechanism governing the biliary fate of drugs and other xenobiotics have yet to be elucidated fully. Perhaps the use of drugs and other pharmacological tools will hasten progress toward this goal.
大量各种各样的外源性物质出现在胆汁中。对一些物质来说,这是最终的排泄过程;对另一些物质而言,这仅仅是活跃的肠肝循环中的一个步骤。对还有一些物质来说,这可能是毒理学或致癌过程中的关键一步。在过去十年里,文献中关于胆汁排泄机制的观察结果一直在稳步积累。许多论文描述了诸如分子量阈值、物种差异的其他方面以及对诱导剂的反应等现象,并且对于它们的意义有很多推测。这项工作的临床意义在一定程度上仍然依赖于从低等动物获得的结果,尽管偶尔会有关于术后有临时胆汁引流的患者的研究出现。持续努力获取人类数据很重要,因为在药物处置领域从低等动物进行推断往往是不可靠的。控制药物和其他外源性物质胆汁命运的基本生理和生化机制尚未完全阐明。也许使用药物和其他药理学工具将加速朝着这个目标取得进展。