Dipeptidyl peptidase 4(DPP4) inhibitors are oral antidiabetic drugs approved to manage type 2 diabetes mellitus. Saxagliptin is a substrate of CYP3A4/5 enzymes while other DPP4 inhibitors such as sitagliptin, linaglip...Dipeptidyl peptidase 4(DPP4) inhibitors are oral antidiabetic drugs approved to manage type 2 diabetes mellitus. Saxagliptin is a substrate of CYP3A4/5 enzymes while other DPP4 inhibitors such as sitagliptin, linagliptin, gemigliptin and teneligliptin are weak substrates of CYP3A4. DPP4 inhibitors have also been identified as substrates of P-gp. Hence, the drugs inhibiting or inducing CYP3A4/5 enzymes and/or P-gp can alter the pharmacokinetics of DPP4 inhibitors. This review is aimed to identify the drugs interacting with DPP4 inhibitors. The plasma concentrations of saxagliptin have been reported to be increased significantly by the concomitant administration of ketoconazole or diltiazem while no significant interactions between various DPP4 inhibitors and drugs like warfarin, digoxin or cyclosporine have been identified.展开更多
Traditional Chinese medicines(TCMs)have been used to prevent and treat various diseases for thousands of years.Promoting efficacy and reducing toxicity by the compatibility theory of TCMs has attracted increasing atte...Traditional Chinese medicines(TCMs)have been used to prevent and treat various diseases for thousands of years.Promoting efficacy and reducing toxicity by the compatibility theory of TCMs has attracted increasing attention,especially for the toxicity of herbs.Studies have pointed out the interactions between the active compounds of herbs and transporters in the detoxification process of toxic compounds.Here,we summarize data on five toxic herbs commonly used in TCMs and their related efflux transporters to reduce toxicity to offer a scientific rationale for the compatibility principle of TCMs and provide guidance for the rational clinical use of TCMs.展开更多
文摘Dipeptidyl peptidase 4(DPP4) inhibitors are oral antidiabetic drugs approved to manage type 2 diabetes mellitus. Saxagliptin is a substrate of CYP3A4/5 enzymes while other DPP4 inhibitors such as sitagliptin, linagliptin, gemigliptin and teneligliptin are weak substrates of CYP3A4. DPP4 inhibitors have also been identified as substrates of P-gp. Hence, the drugs inhibiting or inducing CYP3A4/5 enzymes and/or P-gp can alter the pharmacokinetics of DPP4 inhibitors. This review is aimed to identify the drugs interacting with DPP4 inhibitors. The plasma concentrations of saxagliptin have been reported to be increased significantly by the concomitant administration of ketoconazole or diltiazem while no significant interactions between various DPP4 inhibitors and drugs like warfarin, digoxin or cyclosporine have been identified.
基金We thank for the funding support from the Science and Technology Development Fund,Macao SAR(No.0040/2020/A and No.0075/2019/AMJ).
文摘Traditional Chinese medicines(TCMs)have been used to prevent and treat various diseases for thousands of years.Promoting efficacy and reducing toxicity by the compatibility theory of TCMs has attracted increasing attention,especially for the toxicity of herbs.Studies have pointed out the interactions between the active compounds of herbs and transporters in the detoxification process of toxic compounds.Here,we summarize data on five toxic herbs commonly used in TCMs and their related efflux transporters to reduce toxicity to offer a scientific rationale for the compatibility principle of TCMs and provide guidance for the rational clinical use of TCMs.
