Linagliptin
TRADJENTA
What it isDPP-4 inhibitor; type 2 diabetes.
Why this oneThe only DPP-4 inhibitor cleared mainly by the bile rather than the kidney, so it needs no dose adjustment at any level of renal function.
What limits itModest A1c reduction and no cardiovascular benefit. Rare pancreatitis and bullous pemphigoid.
FDA-approved for
- type 2 diabetes (2011)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Type 2 diabetes mellitus (adjunct to diet and exercise) | Adults | 5 mg QD | 5 mg QD | 5 mg QD |
Renal No adjustment needed
Hepatic No adjustment needed
Instructions
- Take with or without food
Cautions
- Acute pancreatitis, including fatal — discontinue promptly if suspected; not studied in history of pancreatitis
- Hypoglycemia when combined with insulin or insulin secretagogue (sulfonylurea) — consider lowering their dose
- Serious hypersensitivity (anaphylaxis, angioedema, exfoliative skin conditions), mostly within first 3 months, some after first dose — discontinue; caution if prior angioedema on another DPP-4 inhibitor
- Severe and disabling arthralgia (onset 1 day to years) — discontinue if implicated
- Bullous pemphigoid requiring hospitalization — discontinue if suspected
- Heart failure signal with other DPP-4 inhibitors — weigh risk/benefit and monitor in patients with HF risk factors
- Not recommended in type 1 diabetes (not effective)
Adverse reactions
- Nasopharyngitis (7%, most common), diarrhea, cough
- Hypoglycemia (with sulfonylurea or insulin)
- Pancreatitis; hypersensitivity (urticaria, angioedema, skin exfoliation, bronchial hyperreactivity)
- Arthralgia, myalgia; bullous pemphigoid; rash, mouth ulceration, rhabdomyolysis (postmarketing)
- Lab: uric acid and lipase increases
Pregnancy Limited human data insufficient to assess risk; no adverse developmental effects in animals near clinical exposure; poorly controlled diabetes itself raises maternal/fetal risk
Lactation No human data; present in rat milk — weigh benefits of breastfeeding against potential risk
NO BOXED WARNINGS
Principal riskLittle; rare pancreatitis
Cost, est. cash$300–$1,000/month
Generic entry2027 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent
Defining liabilityAgent-specific hypoglycemia, ketoacidosis, volume, renal or gastrointestinal toxicity.
Mechanism of action: Linagliptin ballicule
Open Linagliptin in the interactive console ↗
Memory aids: mascots and interaction avatars
DDP-4 inhibitor tea bag theme → gliptin → Lipton sweet tea (although opposite effect on blood glucose)
