Linagliptin
A once-daily DPP-4 inhibitor for type 2 diabetes that needs no dose change in kidney or liver impairment.
Drug card
- Class
- DPP-4 inhibitor
- How it works
- Blocking the enzyme DPP-4, so gut incretin hormones last longer
- Used for
- Type 2 diabetes
- Known for
- Inflammation of the pancreas (pancreatitis)
- Blistering skin disease (bullous pemphigoid)
- Its name
- -gliptin means a DPP-4 inhibitor (gliptin)
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does linagliptin work?
Linagliptin binds DPP-4 reversibly and selectively, sparing DPP-8 and DPP-9, so active GLP-1 and GIP rise and insulin goes up and glucagon down when glucose is high. It has a xanthine-like purine-dione structure. About 90% leaves the body unchanged, mostly through the bile and gut rather than the urine, so kidney function does not alter its dose.
Like other 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.
Uses
What is linagliptin used for?
- Type 2 diabetes
Side effects
Side effects of linagliptin
- Inflammation of the pancreas (pancreatitis)Known forSerious
- Blistering skin disease (bullous pemphigoid)Known forSerious
- Colds and sore throat (nasopharyngitis)
- Diarrhea
- Cough
- Severe allergic reaction (anaphylaxis)Serious
- Swelling of face and throat (angioedema)Serious
- Peeling skin reactions (exfoliative skin conditions)Serious
- Severe, disabling joint pain
- Heart failure (a class warning)Serious
- Hypoglycemia with a sulfonylurea or insulin
- Muscle breakdown (rhabdomyolysis), rareSerious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Strong P-gp or CYP3A4 inducers such as rifampicin cut its effect; another treatment is advised.
- Stop it if pancreatitis is suspected.
- Hypoglycemia risk rises with a sulfonylurea or insulin, more so with insulin in severe kidney impairment.
Good to know: Eliminated mainly through the bile, so people with kidney disease take it without dose changes.
Remember it
A way to remember it
Gliptins guard GLP-1.
DPP-4 normally inactivates GLP-1 and GIP within minutes. Blocking it keeps them active, and because their effect depends on glucose, hypoglycemia is rare unless a sulfonylurea or insulin is added.
Written for biofideX
Its name
-gliptin means DPP-4 inhibitor (gliptin)
Sitagliptin, linagliptin, saxagliptin and vildagliptin block dipeptidyl peptidase-4, so incretin hormones such as GLP-1 last longer.
- Every drug name stem
Its class
DPP-4 inhibitors
Other DPP-4 inhibitors with a card:
Easily mixed up with GLP-1 receptor agonists, SGLT2 inhibitors and sulfonylureas.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
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.
Diabetes
Linagliptin is one of 14 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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