Forst Thomas, Pfützner Andreas
b Institute for Clinical Research and Development, Parcusstrasse 8, D-55116 Mainz, Germany.
a Institute for Clinical Research and Development, Parcusstrasse 8, D-55116 Mainz, Germany.
Expert Rev Endocrinol Metab. 2013 Jan;8(1):21-35. doi: 10.1586/eem.12.69.
Linagliptin is a pharmacologically unique, orally active, once-daily dipeptidyl peptidase-4 inhibitor indicated for the treatment of hyperglycemia in patients with Type 2 diabetes mellitus. Compared with other dipeptidyl peptidase-4 inhibitors, linagliptin has a favorable pharmacokinetic profile with a primarily nonrenal route of elimination that avoids the need for dose adjustment in patients with renal impairment. When administered as monotherapy or in combination with other antihyperglycemic drugs, linagliptin treatment leads to clinically meaningful reductions in glycated hemoglobin, fasting plasma glucose and postprandial plasma glucose levels. In addition, pancreatic β-cell function is enhanced. Linagliptin treatment is well tolerated, with weight-neutral effects and no increased risk of hypoglycemia. Of note, linagliptin treatment was associated with a significantly reduced risk of cardiovascular events in clinical trials of ≤2 years, although this finding remains to be confirmed in larger and longer clinical outcomes studies.
利格列汀是一种药理学特性独特、口服有效、每日一次的二肽基肽酶-4抑制剂，适用于治疗2型糖尿病患者的高血糖。与其他二肽基肽酶-4抑制剂相比，利格列汀具有良好的药代动力学特征，主要通过非肾脏途径消除，避免了肾功能损害患者需要调整剂量的问题。当作为单一疗法或与其他降糖药物联合使用时，利格列汀治疗可使糖化血红蛋白、空腹血糖和餐后血糖水平在临床上有意义地降低。此外，胰腺β细胞功能得到增强。利格列汀治疗耐受性良好，对体重无影响，且低血糖风险无增加。值得注意的是，在≤2年的临床试验中，利格列汀治疗与心血管事件风险显著降低相关，尽管这一发现仍有待在更大规模和更长时间的临床结局研究中得到证实。
