- Dipeptidyl Peptidase-4 Inhibitors (gliptans) are a class of oral hypoglycemics that block DPP-4. This leads to an increase in the activity of incretins, which inhibit glucagon release, which in turn increase insulin secretion and slow gastric emptying, ultimately decreasing blood glucose levels. These drugs are commonly used in the treatment of type 2 diabetes.
- Generally used as second or third line treatment for type 2 diabetes mellitus. They may be used as monotherapy or combined therapy.
FDA Approved DPP-4 Inhibitors
|Brand Name||Active Ingredient(s)|
|Janumet XR||sitagliptin, metformin ER|
|Kombiglyze XR||saxagliptin, metformin ER|
Mechanism of Action
- Inhibit DPP-4, an enzyme expressed on surface of most cell types
- DPP-4 deacctivates other bioactive peptides, including incretins such as glucagon-like peptide-1 (GLP-1).
- GLP-1 is secreted in response to nutrients, stimulating glucose-dependent insulin release from pancreatic beta-cells, which in turn decreases blood sugar levels.
- Also decreases gastric emptying and inhibits postprandial glucagon release
- In controlled studies of sitagliptin (as monotherapy and combination therapy), overall incidence of adverse reactions/discontinuation similar to placebo
- Most commonly reported adverse reactions include nasopharyngitis, URI, HA
- Postmarketing surveillance found association with sitagliptin and development of acute pancreatitis
- Confounding variables such as diabetes, hypercholesterolemia, hypertriglyceridemia, obesity
- Also postmarketing reports of serious allergic reactions (including anaphylactoid reactions, angioedema, SJS)
- Studies of other drugs in this class additionally report lymphopenia, cough, peripheral edema, transaminitis, and hypertension.
- Other side effects reported in patients taking this class of medication include joint pain