Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha-cells, resulting in a reduction in hepatic glucose output.

TRADJENTA is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

5 mg orally once daily, with or without food.

Common adverse reactions:

• Nasopharyngitis (7%)
• Diarrhea (3.3%)
• Cough (2.1%)

Hypersensitivity to linagliptin or any of its components.

Pancreatitis: Reported cases including fatal ones; discontinue if suspected.

Hypoglycemia: Risk increases with concomitant use of insulin or sulfonylureas.

Hypersensitivity reactions: Includes anaphylaxis and angioedema.

Severe arthralgia: Joint pain possibly related to the drug.

Bullous pemphigoid: Blistering skin condition; requires discontinuation.

Heart failure: Observed in DPP-4 inhibitors; monitor at-risk patients.