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[Pharmacology](https://durgical.com/en/pharmacology/) · [DPP-4 inhibitors (gliptins)](https://durgical.com/en/pharmacology/classes/dpp-4-inhibitors/)

# 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

- Class: [DPP-4 inhibitors (gliptins)](https://durgical.com/en/pharmacology/classes/dpp-4-inhibitors/)
- Enzyme: Dipeptidyl peptidase-4 (DPP-4)
- ATC code: A10BH05

✂**Dipeptidyl peptidase-4 (DPP-4)**Linagliptin

ⓘ The figure shows linagliptin in the active site of human DPP-4.

**Target in 3D:** Dipeptidyl peptidase-4 (DPP-4). PDB structure 2RGU (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/2RGU) · Drag to rotate · pinch to zoom

## 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 →](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

## Adverse effects

### Common

- Nasopharyngitis
- Cough
- Hypoglycemia when combined with insulin or a sulfonylurea

### Serious (rare, important)

- Acute pancreatitis
- Serious allergic reactions: anaphylaxis, angioedema, Stevens–Johnson syndrome
- Bullous pemphigoid
- Severe, disabling joint pain

## 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.

## Memory aid

Linagliptin leaves by the 'liver line' (bile), not the kidney: one gliptin you do not adjust for kidney function.

## 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.

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## Related drugs

- [Sitagliptin](https://durgical.com/en/pharmacology/sitagliptin/)
- [Saxagliptin](https://durgical.com/en/pharmacology/saxagliptin/)
- [Vildagliptin](https://durgical.com/en/pharmacology/vildagliptin/)

## Related conditions

- [Type 2 diabetes mellitus](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

[← Back to the class: DPP-4 inhibitors (gliptins)](https://durgical.com/en/pharmacology/classes/dpp-4-inhibitors/)

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](https://medlineplus.gov/druginfo/meds/a611036.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [DailyMed - LINAGLIPTIN tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cbdbd4b2-c07b-00e1-e053-2995a90a5fc9) (DailyMed (U.S. National Library of Medicine), 2026); [Crystal structure of complex of human DPP4 and inhibitor](https://www.rcsb.org/structure/2RGU) (RCSB Protein Data Bank, 2007); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A10BH05) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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