Pharmacology · DPP-4 inhibitors (gliptins)
Linagliptin !
A DPP-4 inhibitor cleared mainly through bile, so it needs no kidney adjustment. Low hypoglycemia risk, no weight change.
Updated 2026-11-01
The figure shows linagliptin in the active site of human DPP-4.
Mechanism of action
Linagliptin is a xanthine-based DPP-4 inhibitor that binds the enzyme tightly. Active GLP-1 and GIP last longer after meals, raising insulin and lowering glucagon in a glucose-dependent way.
- Blocks the DPP-4 enzyme in plasma and on cells
- Active GLP-1 and GIP last longer after meals
- More insulin and less glucagon when glucose is high
- Glucose falls without weight change
Pharmacokinetics
- Absorption
- Oral, with or without food.
- Elimination
- Mostly unchanged through bile and feces (enterohepatic route); very little in urine.
Indications
- Type 2 diabetes, with diet and exercise, including people with kidney impairment Type 2 diabetes mellitus →
Adverse effects
Common
- Nasopharyngitis
- Cough
- Hypoglycemia when combined with insulin or a sulfonylurea
Contraindications
- Hypersensitivity to linagliptin
- Not for type 1 diabetes or ketoacidosis
Key interactions
- Rifampicin and other strong P-gp or CYP3A4 inducers
- Can reduce its effect; another treatment is preferred.
- St John's wort
- May reduce its effect.
- Insulin or sulfonylureas
- Higher risk of hypoglycemia.
What is monitored
- HbA1c
- Symptoms of pancreatitis, skin blisters or joint pain
Administration and safety
- Oral tablet, once a day, with or without food.
- Not given together with a GLP-1 receptor agonist.
Nursing care
- Before: kidney function, history of pancreatitis and heart failure.
- During: abdominal pain, skin blisters, joint pain, swelling or breathlessness.
- Capillary glucose when combined with insulin or a sulfonylurea.
Pregnancy and breastfeeding
Data in pregnancy are limited; insulin is the usual choice.
Test yourself
Think of the answer, then tap the question to see it.
What is special about how linagliptin is eliminated?
It leaves mainly unchanged through bile and feces, so no dose change is needed in kidney impairment.
Which antibiotic can make linagliptin less effective?
Rifampicin, a strong inducer of P-glycoprotein and CYP3A4.
Can linagliptin be combined with semaglutide?
It is not: both act on the GLP-1 axis, so the combination adds little.
Related drugs
Related conditions
← Back to the class: DPP-4 inhibitors (gliptins)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Linagliptin: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); DailyMed - LINAGLIPTIN tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); Crystal structure of complex of human DPP4 and inhibitor (RCSB Protein Data Bank, 2007); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.