DPP-4 inhibitors
Introduction
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.
FDA Approved DPP-4 Inhibitors
| Brand Name | Active Ingredient(s) |
|---|---|
| Januvia | sitagliptin |
| Janumet | sitagliptin, metformin |
| Janumet XR | sitagliptin, metformin ER |
| Onglyza | saxagliptin |
| Kombiglyze XR | saxagliptin, metformin ER |
| Tradjenta | linagliptin |
| Glyxambi | linagliptin, empagliflozin |
| Jentadueto | linagiptin, metformin |
| Nesina | alogliptin |
| Kazano | alogliptin, metformin |
| Oseni | alogliptin, pioglitazone |
Mechanism of Action
DPP-4 inhibitors inhibit the enzyme DPP-4, which is expressed on the surface of most cell types. DPP-4 deactivates other bioactive peptides, including incretins like glucagon-like peptide-1 (GLP-1). GLP-1 is secreted in the small intestines in response to nutrients, stimulating glucose-dependent insulin release from the pancreatic islets. Additionally, it decreases gastric emptying and inhibits postprandial glucagon release.
Indications
Adverse Effects
References
US Food and Drug Administration. "FDA Drug Safety Communication: FDA warns that DPP-4 inhibitors for type 2 diabetes may cause severe joint pain." FDA, 6/23/2016. http://www.fda.gov/Drugs/DrugSafety/ucm459579.htm