Linagliptin

A DPP-4 inhibitor uniquely safe for diabetic patients with kidney disease.

What is Linagliptin?

Linagliptin is an oral antidiabetic drug belonging to the DPP-4 inhibitor class, used in type 2 diabetes mellitus.

Unlike other DPP-4 inhibitors, it does not require dose adjustment in renal disease.

History & Background

Linagliptin was developed to provide effective glycemic control while being safe in patients with chronic kidney disease.

Chemical Structure & Properties

• IUPAC name: 8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-ynyl)-3-methyl-1-(4-methylquinazolin-2-yl)-3,7-dihydro-1H-purine-2,6-dione
• Molecular formula: C₂₅H₂₈N₈O₂
• Molar mass: 472.54 g/mol
• Functional groups: Xanthine core, amine, heterocyclic rings

Mechanism of Action

Linagliptin lowers blood glucose by:

• Inhibiting the DPP-4 enzyme
• Increasing GLP-1 and GIP hormones
• Enhancing glucose-dependent insulin secretion
• Reducing glucagon secretion

Pharmacokinetics

• Absorption: Rapid oral absorption
• Peak plasma time: ~1.5 hours
• Half-life: ~100 hours (terminal)
• Metabolism: Minimal hepatic metabolism
• Excretion: Feces (major route)

Medical Uses

• Type 2 diabetes mellitus
• Patients with renal impairment
• Combination therapy with metformin or insulin

Dosage Guidelines

Adults: 5 mg once daily

Renal impairment: No dose adjustment needed

⚠️ Low risk of hypoglycemia when used alone.

Side Effects

• Nasopharyngitis
• Cough
• Headache
• Rare pancreatitis

Warnings & Precautions

• Monitor for pancreatitis symptoms
• Not indicated for type 1 diabetes
• Use caution with insulin combinations

Drug Interactions

• Rifampicin (reduces effect)
• Insulin or sulfonylureas (↑ hypoglycemia risk)

Frequently Asked Questions

Is linagliptin safe in kidney disease? – Yes.

Does it cause hypoglycemia? – Rare.

Does it cause weight gain? – No.

Can it be combined with metformin? – Yes.

⚠️ Educational content only. Not a substitute for professional medical advice.