药物之间的蛋白结合置换历来被认为是重要的药物相互作用。但近年随着药物动力学研究的进展,发现许多以往认为由药物蛋白结合置换引起的不良反应,实际上系置换药影响被置换药的消除所致。因而对药物结合置换作用本身的临床重要性产生了怀疑。本文就药物蛋白结合的置换对血浆中未结合药物的浓度的影响进行了理论分析,并回顾了机理已阐明的这类相互作用。文章的结论是:尽管药物间的蛋白结合置换作用十分常 Protein-binding substitutions between drugs have historically been regarded as important drug interactions. However, with the progress of pharmacokinetic studies in recent years, many of the adverse reactions that have been previously thought to be caused by the substitution of drug proteins are actually caused by the elimination of replacement drugs. Thus doubting the clinical importance of the drug-binding replacement itself. This paper presents a theoretical analysis of the effect of drug-protein conjugation on the concentration of unbound drug in plasma and reviews mechanisms that have elucidated such interactions. The conclusion of the article is: Although the protein-binding displacement of drugs is very common