Linagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Linagliptin may be used as monotherapy or in combination with other common antidiabetic medications including Metformin, Sulfonylurea, Pioglitazone, or Insulin. As a replacement therapy it is suitable when Metformin therapy is not appropriate due to intolerance or do not provide adequate glycemic control as monotherapy or other antidiabetic drugs are to be discontinued due to renal or hepatic impairment.
Dipeptidyl Peptidase-4 (DPP-4) inhibitor
Linagliptin is indicated to improve glycemic control in patients with type 2 diabetes mellitus. Linagliptin is an inhibitor of DPP-4 (dipeptidyl peptidase-4), an enzyme that degrades the incretin hormones GLP-1 (glucagon like peptide-1) and GIP (glucose dependent insulinotropic polypeptide). Thus, Linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin from pancreatic beta (β) cells in a glucose-dependent manner and decreasing the secretion of glucagon from pancreatic alpha (α) cells in the circulation.
The recommended dose of Linagliptin is 5 mg once daily and can be taken with or without food. If added with Metformin, the dose of Metformin should be maintained and Linagliptin administered concomitantly. When used in combination with Sulfonylurea, a lower dose of Sulfonylurea may be considered to reduce the risk of hypoglycemia.
Linagliptin is a weak competitive and a weak to moderate mechanism-based inhibitor of CYP isozyme CYP3A4, but does not inhibit other CYP isozymes. The risk for clinically meaningful interactions by other medicinal products on linagliptin is low and in clinical studies linagliptin had no clinically relevant effect on the pharmacokinetics of metformin, glyburide, simvastatin, warfarin, digoxin or oral contraceptives.
Linagliptin is contraindicated to patients hypersensitive to Linagliptin or any of the excipients. When used with an Insulin secretagogue (e.g., sulfonylurea) or Insulin, consider lowering the dose of the Insulin secretagogue or Insulin to reduce the risk of hypoglycemia. If pancreatitis is suspected, Linagliptin should be discontinued. There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with Linagliptin or any other antidiabetic drug.
Treatment with Linagliptin is well tolerated; some of the less common side effects are nasopharyngitis and hypoglycemia.
Pregnancy: There are no adequate and well-controlled studies in pregnant women. Linagliptin tablets should be used during pregnancy only if the potential benefit of mother justifies the potential risk of the fetus. Nursing mothers: Caution should be exercised when Linagliptin is administered to a nursing woman.
Keep in a dry place away from light and heat. Keep out of the reach of children.
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