利格列汀药理学特征剖析.ppt

Linagliptin是唯一一个无需剂量调整，每日一次的DPP-IV抑制剂，可用于肾功能全期。 So it is clear that patients with diabetes have an especially high rate of declining renal function. As renal fiunction decline, clearance of renally excreted medicines is altered, and dose adjustment is usually required, or in some cases the drug is contraindicated and alternative medication must be used. This slide shows the use of various glucose lowering therapies in patients at different levels of renal function. *click* As renal function declines below 60, some drugs are contraindicated – these include sitagliptin, and metformin. *click* with CKD stage 3, as GFR declines below 60, acarbose and the injectable GLP-1 analogue exenatide may still be used but exenatide requires dose adjustment. *click* The injectable GLP-1 analgoue Liraglutide, and the SUs glimepiride and glicacide may be used when GFR is severely reduced below 30, but the SUs require dose adjustment. *click* When using insulin in a patient with declining renal function, the dose must also be adjusted. *click* Beyond this, there are few options for patients with kidney failure requiring dialysis. *click* The new DPP-4 inhibitor, due to its primarily non-renal route of excretion, may be used in declining renal function without changing the dose. *click* So as you see, renal function is an important factor that affects the choice of drug for the individual, and chronic kideney disease will usually result in the need for dose reduction for many patients with tyoe 2 diabetes. Adapted from: Schernthaner G, et al. Nephrol Dial Transplant. 2011;26(2):454–7. (in press) 同时，虽然欧唐宁90％通过肝脏排泄，但是对于任何肝功能不全的患者也不需要调整剂量。 这是在一项开放标签、平行组、单中心药代动力学研究中，纳入了轻度(n = 8)、中度(n = 9)或重度(n = 8)肝功能不全和健康 (n = 8)患者，比较服用5mg欧唐宁?达稳态的不同肝功能患者平均曲线下面积。结果显示，轻度、中度及重度肝功能不全患者AUC与健康人群相比不增加药物暴露倍数，证实不同肝功能不全患者服用欧唐宁?无需调整剂量或增加药物监测。 * 再看肝功能不全的药物使用情况，在口服药物治疗中，轻度肝功能损害的时候，部分药物已经使用受限或需减少剂量；在中、重度肝功能不全的情况下，大多数药物都被限制使用。 新型的DPP-4抑制剂欧唐宁?不受肝功能限制，无需调整剂量。 所以，欧唐宁?可应用于不同肾功能和肝功能状态的患者，无需调整剂量。 吡格列酮：严重肝功能障碍患者禁用