25.15 : 二肽基肽酶 4 抑制剂

Dipeptidyl peptidase 4, or DPP-4 inhibitors, called gliptins inhibit incretin hormone inactivation.

These drugs bind to DPP-4,  increasing the levels of active GIP and GLP-1 hormones.

This improves insulin secretion and reduces glucagon levels, remedying fasting and postprandial hyperglycemia without directly affecting insulin sensitivity, gastric motility, or satiety.

Some examples of this class include sitagliptin, saxagliptin, linagliptin, and vildagliptin.

When used alone, DPP-4 inhibitors decrease A1c levels by an average of 0.8%. However, when combined with other hypoglycemics, they cause a total decrease in A1c levels by 1.3%

Linagliptin undergoes extensive plasma protein binding and hepatobiliary clearance. Saxagliptin is metabolized by hepatic microsomal enzymes and requires dosage adjustment when coadministered with strong CYP3A4 inhibitors.

Although these agents are well tolerated, they rarely show adverse effects, such as heart failure risks, severe joint pain, and pancreatitis.