Dipeptidyl peptidase 4 (DPP-4) inhibitors are a group of oral hypoglycemic agents used to manage Type 2 Diabetes Mellitus, which is a significant risk factor for coronary disease, heart failure, stroke, and many other cardiovascular conditions.
DPP-4 inhibitors, known as gliptins, are a class of oral diabetic medications to treat type 2 diabetes mellitus in adults.
DPP-4 inhibitors include sitagliptin, saxagliptin, linagliptin, vildagliptin and alogliptin. The drugs act through incretin hormones, which are gut hormones responsible for glucose homeostasis after oral food intake.
Apart from hypoglycemic effects, this class of drugs possesses antihypertensive effects, anti-inflammatory effects, antiapoptotic effects, and immunomodulatory effects on the heart, kidneys, and blood vessels independent of the incretin pathway. These drugs could also be used in kidney and liver transplant recipients with new-onset diabetes after transplantation (NODAT) due to all these benefits.
They can be used as monotherapy or add-on therapy with other medications. Options for add-on therapy include metformin, sulfonylureas, thiazolidinediones, or insulin.
All the DPP-4 inhibitors are administered orally, once or twice (divided dose) daily, before (preferably) or after meals.
Gliptins are associated with a low incidence of adverse events, including hypoglycemia, and have weight-neutral effects. However, the risk of hypoglycemia increases when used in conjunction with sulfonylureas (SU), as SU is known to cause hypoglycemia.
DPP-4 inhibitors did not show an increased risk of cardiovascular death, non-fatal myocardial infarction, or non-fatal stroke when compared to placebo in patients with type 2 diabetes.
“Saxagliptin” had an association with an increased rate of hospitalization for heart failure.
“Sitagliptin and Saxagliptin” are known to cause upper respiratory tract infection, nasopharyngitis, headache, urinary tract infection & arthralgia. Some Gliptins shows hypersensitivity reactions such as anaphylaxis and angioedema.
Sitagliptin was also associated with Stevens-Johnson syndrome in postmarketing reports.
There are some reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing variants but it remains unproven till now and not observed in post market surveillance. So Gliptins should be used with caution in pancreatitis patients.
Gliptins are contraindicated in Type 1 diabetes and Diabetic Ketoacidosis (DKA). Dose adjustment is also needed in renal insufficiency patients.