Linagliptin
Tradjenta | Trajenta
Overview
DPP-4 inhibitor for type 2 diabetes. Unique among gliptins for primarily non-renal elimination, requiring no dose adjustment in kidney disease.
Indications
- Type 2 diabetes mellitus (adjunct to diet and exercise)
Contraindications
- Type 1 diabetes
- Diabetic ketoacidosis
- History of hypersensitivity to linagliptin
Classification
Mechanism of Action
Inhibits dipeptidyl peptidase-4 (DPP-4), preventing degradation of incretin hormones GLP-1 and GIP, enhancing insulin secretion and suppressing glucagon in a glucose-dependent manner.
Pharmacodynamics
Reduces HbA1c by 0.5-0.8%. Does not cause hypoglycemia as monotherapy. Weight-neutral.
Pharmacokinetics
- Absorption
- Absolute bioavailability ~30%. Not affected by food.
- Distribution
- Extensive tissue distribution. Binds extensively to DPP-4 in tissues.
- Metabolism
- Minimal. Not a CYP substrate. Primarily excreted unchanged.
- Excretion
- Fecal (80%), renal (5%). No dose adjustment for renal or hepatic impairment.
- Half-life
- >100 hours (effective half-life 12 hours)
- Bioavailability
- ~30%
- Protein Binding
- 70-80% (concentration-dependent)
Dosage
Typical dosage: 5mg once daily
Available Forms
- Tablet
Side Effects
Common
- Nasopharyngitis
- Cough
- Headache
Serious
- Pancreatitis
- Bullous pemphigoid
- Severe joint pain
Rare
- Anaphylaxis
- Angioedema
- Hepatic failure
Drug Interactions
Strong P-gp/CYP3A4 inducer reduces linagliptin exposure. Consider alternative diabetes medication.
Increased hypoglycemia risk. May need to reduce insulin/SU dose.
Warnings
Pregnancy
Category B
Toxicity
Wide therapeutic index. Overdose unlikely to be life-threatening.
Overdose
Treatment: supportive care. Not removed by hemodialysis.
References
Looking for patient-friendly information? Visit RemedyDoor for easy-to-read guides about this medication.