Medicine & USMLE

DPP-4 Inhibitors

Diabetes Drugs
  1. Insulin Overview
  2. Rapid Acting Insulin
  3. Short Acting Insulin
  4. Intermediate Acting Insulin
  5. Long Acting Insulin
  6. Metformin
  7. Sulfonylureas
  8. Meglitinides
  9. Thiazolidinediones (TZDs)
  10. DPP-4 Inhibitors
  11. Incretin Mimetics
  12. SGLT2 Inhibitors
  13. Alpha Glucosidase Inhibitors
  14. Pramlintide


DPP-4 inhibitors help treat type 2 diabetes mellitus. They are commonly called the “gliptins” because the drug names all end in -gliptin. Sitagliptin, Linagliptin, and Saxagliptin are all examples of DPP-4 inhibitors. These drugs work by increasing insulin release and decreasing glucagon release. Side effects of DPP-4 inhibitors may include headache, upper respiratory infections, pancreatitis, and serious skin reactions.

Key Points

  • DPP-4 Inhibitors (Dipeptidyl peptidase 4 Inhibitors)
    • Drug Name
      • -gliptin Ending
        • Sitagliptin (Januvia)
        • Linagliptin (Tradjenta)
        • Saxagliptin (Onglyza)
    • Mechanism
      • Promotes insulin release
        • Stimulates beta cells in the pancreas to release more insulin
      • Decreases glucagon release
        • The hormone glucagon raises blood glucose levels, so by decreasing glucagon release, pramlintide helps lower blood glucose levels
    • Clinical Use
      • Treats Type 2 Diabetes Mellitus (DM)
        • The end result of DPP-4 Inhibitors is a decrease in blood glucose levels in patients with type 2 diabetes mellitus
    • Side Effects
      • Causes pancreatitis
        • Notify provider of abdominal pain
      • Causes headache
        • Common side effect
      • Causes serious skin reactions
        • E.g. urticaria, Stevens-Johnson Syndrome (SJS), hypersensitivity, rash
      • Causes upper respiratory infections (URI)
        • E.g. nasopharyngitis
      • Hypoglycemia when combined with other antidiabetic medications
        • On its own, DPP-4 inhibitors don’t have a high risk of hypoglycemia. But when combined with other diabetes drugs (i.e. insulin, sulfonylureas) the risk of hypoglycemia goes up significantly