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

# Sitagliptin

The first DPP-4 inhibitor: an oral tablet that protects the body's own incretins, with low hypoglycemia risk and no weight gain.

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: A10BH01

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

ⓘ The figure shows sitagliptin (labelled in the entry as a beta-amino acid inhibitor) in the active site of human DPP-4.

**Target in 3D:** Dipeptidyl peptidase-4 (DPP-4). PDB structure 1X70 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/1X70) · Drag to rotate · pinch to zoom

## Mechanism of action

Sitagliptin is a competitive, reversible inhibitor of DPP-4. With the enzyme blocked, active GLP-1 and GIP rise after meals, insulin secretion increases and glucagon falls, only while glucose is high. The effect on HbA1c is moderate.

- 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, well absorbed.

**Metabolism**
Little metabolism.

**Elimination**
Mostly unchanged in urine, so the dose is lowered in kidney impairment.

**Half-life**
Allows once-daily use.

## Indications

- Type 2 diabetes, with diet and exercise, alone or with metformin and other drugs [Type 2 diabetes mellitus →](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

## Adverse effects

### Common

- Upper respiratory infection, sore throat, headache
- 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
- Heart failure (class warning)

## Contraindications

- Hypersensitivity to sitagliptin (anaphylaxis, angioedema)
- Not for type 1 diabetes or ketoacidosis

## Key interactions

**Insulin or sulfonylureas**
Higher risk of hypoglycemia.

**GLP-1 receptor agonists**
Not combined: same pathway, no extra benefit.

## What is monitored

- Kidney function before starting and periodically
- HbA1c
- Symptoms of pancreatitis

## 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 too limited to judge the risk; insulin is the usual choice.

## Memory aid

Gliptins guard the incretins: DPP-4 is the 'scissors' that cut GLP-1, and sitagliptin hides the scissors. No new hormone, just the body's own lasting longer.

## Test yourself

Think of the answer, then tap the question to see it.

## Why does sitagliptin need adjustment in kidney disease?

It is cleared mainly unchanged by the kidney, so levels rise when filtration falls.

## Which skin disease is a class warning for DPP-4 inhibitors?

Bullous pemphigoid: tense blisters that may need hospital care; the drug is stopped.

## Is weight gain expected with sitagliptin?

No. DPP-4 inhibitors are weight-neutral.

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## Related drugs

- [Linagliptin](https://durgical.com/en/pharmacology/linagliptin/)
- [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: [Sitagliptin: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a606023.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [DailyMed - SITAGLIPTIN tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=58e23b30-451c-f451-e063-6394a90a35a7) (DailyMed (U.S. National Library of Medicine), 2026); [HUMAN DIPEPTIDYL PEPTIDASE IV IN COMPLEX WITH A BETA AMINO ACID INHIBITOR](https://www.rcsb.org/structure/1X70) (RCSB Protein Data Bank, 2005); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A10BH01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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