测定血清肌酐浓度并随后计算估计肾小球滤过率 (eGFR) 是临床医学的基石。停止药物治疗等关键临床决策是基于根据血清肌酐测量值计算出的 eGFR。然而，肌酐不仅在肾脏中过滤，而且还积极分泌到尿液中。近端肾小管细胞中表达的肌酐转运蛋白（例如 OCT2、OCT3、MATE1、MATE2-K 和 OAT2）负责肾主动分泌肌酐。多种药物（例如口服抗肿瘤药物）抑制这些转运蛋白，从而导致肾功能假性恶化，血清肌酐浓度增加，eGFR 降低，而其他 eGFR 测定方法（例如通过半胱氨酸蛋白酶抑制剂 C）显示肾功能正常。由于美国处方信息 (PI) 和欧洲产品特性摘要 (SmPC) 是医生最相关的信息来源，因此我们调查了美国 PI/德国 SmPC 中药物的信息质量，有明确的证据表明肾功能出现假性恶化。鉴定出 514 种可能与肌酐转运蛋白相互作用的药物。其中 149 种药物已被描述会导致血清肌酐浓度升高。现有数据证实其中30种药物存在假性肾功能恶化，而其余119种药物现有数据不足。 30 种药物的 PI/SmPC 中只有 23.5% (12/51) 包含关于这种已证实的肾功能假性恶化的明确声明，并为临床管理提供了明确的建议。总而言之，PI 或 SmPC 中提供的有关肾功能假性恶化的信息不足，会给患者带来不必要的风险。© 2024 作者。临床药理学

Determination of serum creatinine concentrations and subsequent calculation of estimated glomerular filtration rates (eGFR) is a cornerstone of clinical medicine. Crucial clinical decisions such as drug treatment discontinuations are based on eGFR calculated from serum creatinine measurements. However, creatinine is not only filtered in the kidneys, but also actively secreted into urine. Creatinine transporters such as OCT2, OCT3, MATE1, MATE2-K, and OAT2 expressed in proximal tubular cells are responsible for active renal secretion of creatinine. Multiple drugs (e.g., oral antitumor drugs) inhibit these transporters thereby causing a pseudo-worsening of kidney function with an increase in serum creatinine concentrations and a decrease in eGFR while other methods for eGFR determination (e.g., by cystatin C) reveal normal kidney function. Since US Prescribing Information (PI) and European Summaries of Product Characteristics (SmPCs) are the most relevant source of information for physicians, we investigated the quality of information in US PI/German SmPCs of drugs with clear evidence for pseudo-worsening of kidney function. 514 drugs putatively interacting with creatinine transporters were identified. For 149 of those drugs, an increase in serum creatinine concentrations has been described. Available data confirmed the existence of pseudo-worsening of kidney function for 30 of those drugs, for the remaining 119 drugs existing data are insufficient. Only 23.5% (12/51) of the 30 drugs' PI/SmPCs contained unambiguous statements on this proven pseudo-worsening of kidney function and gave clear recommendations for clinical management. Taken together, inadequate information provided in PI or SmPCs on the pseudo-worsening of kidney function poses patients at unnecessary risks.© 2024 The Author(s). Clinical Pharmacology & Therapeutics published by Wiley Periodicals LLC on behalf of American Society for Clinical Pharmacology and Therapeutics.