Question
Dipeptidyl Peptidase 4 inhibitors
Answer
DPP-4 inhibitors (“gliptins”) are oral hypoglycemic agents.
MOA: DPP-4 inhibitor (e.g. sitagliptin) → inhibits dipeptidyl peptidase-4 → preserves endogenous incretin hormones (GLP-1, GIP) that DPP-4 would normally rapidly degrade → glucose-dependent enhancement of insulin release and suppression of glucagon — active mainly when glucose is already elevated, mirroring incretins’ own physiological glucose-dependence.
Examples: Sitagliptin, Vildagliptin, Linagliptin.
Uses: type 2 diabetes mellitus, as monotherapy or combined with metformin.
Adverse effects: low hypoglycemia risk (a specific advantage over sulfonylureas, given the glucose-dependent mechanism), nasopharyngitis, headache, rare pancreatitis, joint pain.