DPP-4 inhibitors

DPP-4 inhibitors block dipeptidyl peptidase-4, the enzyme that quickly inactivates the gut incretin hormones GLP-1 and GIP. Active incretin levels after a meal rise two- to three-fold, boosting insulin release and lowering glucagon, but only when glucose is normal or high. On their own they therefore rarely cause hypoglycemia, and body weight does not rise.

• SitagliptinCleared mainly by the kidneys, so unlike linagliptin its dose depends on eGFR. Weight-neutral.
• LinagliptinEliminated mainly through the bile, so people with kidney disease take it without dose changes.

• Type 2 diabetes

• Inflammation of the pancreas (pancreatitis)Known forSerious
• Severe, disabling joint painKnown for
• Blistering skin disease (bullous pemphigoid)Known forSerious
• Heart failure (seen with some members of the class)Serious
• Swelling of face and throat (angioedema)Serious
• Stevens-Johnson syndrome and other skin peelingSerious
• Acute kidney injurySerious
• Colds and sore throat (nasopharyngitis)
• Headache
• Hypoglycemia with a sulfonylurea or insulin

What the class has in common. Each drug's card has its own, and Known for marks what an exam expects you to know.

• Persistent, severe pain in the abdomen, sometimes reaching the back, may mean pancreatitis: stop the drug.
• Adding one to a sulfonylurea or insulin may call for a lower dose of those to avoid hypoglycemia.
• Sitagliptin needs a lower dose when eGFR is below 45; linagliptin needs no change in kidney disease.
• Weigh the heart failure risk before starting in people with heart failure or kidney impairment.

Written for biofideX in plain words, after checking these references:

• Sitagliptin tablets: label (DailyMed)
• Linagliptin tablets: label (DailyMed)
• Sitagliptin (NHS)
• Sitagliptin (NCI Thesaurus)

For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.