University Paris Descartes, Department of Pharmaceutical Sciences, Faculty of Pharmacy, 4, avenue de l'Observatoire, FR-75006 Paris.
Chem Biodivers. 2009 Nov;6(11):1933-42. doi: 10.1002/cbdv.200900171.
During the past decades, pharmacokinetics has been defined as the study of drug absorption, distribution, metabolism, and excretion (ADME), when the drug is introduced into a biological system, such as the human body. Pharmacokinetics is now challenged by the growing importance of transporters, a relatively new and potentially major factor in drug ADME. The recent intrusion of drug transporters means that there is no single mechanism by which drugs permeate through membranes. The presence of transporters in membranes modulates the traditional theory of 'diffusional pharmacokinetics' towards 'vectorial pharmacokinetics' in which ADME processes are governed more deterministically. Drug transporters are also clinically important. They can modulate the pharmacological activity of drugs by affecting their intracellular concentrations and causing toxicity in specific organs due to intracellular drug accumulation. Finally, they are key players in drug-drug interactions, where they are as important as the drug metabolizing enzymes.
在过去几十年中，药物动力学被定义为研究药物在被引入生物系统（如人体）时的吸收、分布、代谢和排泄（ADME）过程。药物动力学现在面临着转运体的重要性日益增加的挑战，转运体是药物 ADME 中一个相对较新且具有潜在重大意义的因素。最近转运体药物的出现意味着药物透过细胞膜没有单一的机制。转运体在膜中的存在将传统的“扩散药物动力学”理论朝着“向量药物动力学”方向转变，ADME 过程更具决定性。药物转运体在临床上也很重要。它们可以通过影响细胞内浓度来调节药物的药理活性，并由于细胞内药物积累而导致特定器官的毒性。最后，它们是药物相互作用的关键因素，与药物代谢酶同样重要。
