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抗菌药物药代动力学中的药物转运体与代谢酶:作用机制、药物相互作用及临床意义

Drug Transporters and Metabolizing Enzymes in Antimicrobial Drug Pharmacokinetics: Mechanisms, Drug-Drug Interactions, and Clinical Implications.

作者信息

Lin Kaili, Wang Ruoqing, Li Tong, Zuo Yawen, Yang Shilei, Dong Deshi, Zhu Yanna

机构信息

Department of Pharmacy, First Affiliated Hospital of Dalian Medical University, Dalian 116011, China.

出版信息

Biomolecules. 2025 Jun 13;15(6):864. doi: 10.3390/biom15060864.

Abstract

Drug transporters and metabolizing enzymes are integral components of drug disposition, governing the absorption, distribution, metabolism, and excretion (ADME) of pharmaceuticals. Their activities critically determine therapeutic efficacy and toxicity profiles, particularly for antimicrobial agents, one of the most widely prescribed drug classes frequently co-administered with other medications. Emerging evidence highlights the clinical significance of the drug-drug interactions (DDIs) mediated by these systems, which may alter antimicrobial pharmacokinetics, compromise treatment outcomes, or precipitate adverse events. With the continuous introduction of novel antimicrobial agents into clinical practice, the role of drug transporters and metabolizing enzymes in the pharmacokinetics of antibiotics and the DDIs between antibiotics and other drugs mediated by these transporters and enzymes are important to determine in order to provide a theoretical basis for the safe and effective use of antimicrobial drugs in clinical use.

摘要

药物转运体和代谢酶是药物处置的重要组成部分,控制着药物的吸收、分布、代谢和排泄(ADME)。它们的活性对于治疗效果和毒性特征起着关键作用,尤其是对于抗菌药物而言,抗菌药物是最广泛处方的药物类别之一,经常与其他药物联合使用。新出现的证据凸显了由这些系统介导的药物-药物相互作用(DDIs)的临床重要性,这些相互作用可能改变抗菌药物的药代动力学、损害治疗效果或引发不良事件。随着新型抗菌药物不断引入临床实践,确定药物转运体和代谢酶在抗生素药代动力学中的作用以及这些转运体和酶介导的抗生素与其他药物之间的药物-药物相互作用,对于为抗菌药物在临床使用中的安全有效应用提供理论依据至关重要。

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