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. DPP-4 Inhibitors
  7. Thiazolidinediones (TZDs)
  8. Meglitinides
  9. Metformin
  10. Sulfonylureas
  11. SGLT2 Inhibitors


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