中国药房2026，Vol.37Issue(3)：407-412,6.DOI:10.6039/j.issn.1001-0408.2026.03.23
钙调磷酸酶抑制剂诱导药物性高血糖的机制及临床研究进展
Mechanism and clinical research progress of calcineurin inhibitor-induced hyperglycemia
摘要
Abstract
Calcineurin inhibitor(CNI)is potent immunosuppressive agents and serve as cornerstone therapies in the treatment of organ transplantation and autoimmune diseases,with cyclosporine A and tacrolimus being the representative drugs.Long-term use of CNI can lead to drug-induced hyperglycemia,severely affecting patients'prognosis.The pathogenesis involves multilevel pathological alterations:at the pancreatic β-cell level,CNI directly damage β-cell by inducing calcium overload,oxidative stress,and mitochondrial dysfunction,suppressing the expression of key insulin synthesis factors and promoting apoptosis;in peripheral tissues,CNI interfere with insulin receptor substrate phosphorylation and inhibit the phosphatidylinositol 3 kinase/protein kinase B signaling pathway,resulting in decreased glucose uptake and insulin resistance;additionally,CNI can also induce β-cell injury by suppressing the secretion and receptor signal transduction of glucagon-like peptide-1,as well as by activating the nuclear factor kappa B pathway to promote inflammatory responses.Clinical studies demonstrate that the incidence of CNI-associated hyperglycemia is closely related to drug type,dosage,and individual patient factors.For high-risk patients,dose adjustment of CNI,switching to agents with lower metabolic toxicity when necessary,and selection of appropriate glucose-lowering regimens based on glycemic levels are recommended.Future research should further elucidate the molecular mechanisms of CNI metabolic toxicity and optimize individualized pharmacotherapy strategies to improve long-term patient outcomes.关键词
药物性高血糖/钙调磷酸酶抑制剂/他克莫司/环孢素A/胰岛素抵抗/胰岛β细胞Key words
drug-induced hyperglycemia/calcineurin inhibitor/tacrolimus/cyclosporine A/insulin resistance/pancreatic β-cell分类
医药卫生引用本文复制引用
鲁素娜,闵秋霞,文茜,张玲..钙调磷酸酶抑制剂诱导药物性高血糖的机制及临床研究进展[J].中国药房,2026,37(3):407-412,6.基金项目
云南省第一人民医院临床医学研究中心开放项目(No.2023YJZX-YX05) （No.2023YJZX-YX05）
昆明医科大学硕士研究生教育创新基金项目(No.2025S186) （No.2025S186）
