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Linagliptin, identified by the CAS number 668270-12-0, is a medication used to improve glycemic control in adults with type 2 diabetes mellitus. It is a dipeptidyl peptidase-4 (DPP-4) inhibitor, which works by inhibiting the enzyme DPP-4, an enzyme that breaks down certain hormones in the body that help regulate blood sugar. By inhibiting DPP-4, linagliptin prolongs the action of these hormones, thereby improving blood glucose control .
The chemical formula for linagliptin is C25H28N8O2, and it has a molecular weight of 472.54. It is typically administered orally in tablet form, with common dosages being 5 mg once daily. Linagliptin can be used as monotherapy or in combination with other antidiabetic medications such as metformin or pioglitazone .
Pharmacologically, linagliptin has a long-lasting effect on DPP-4 inhibition, with a half-life of approximately 155 hours, allowing for once-daily dosing. It is extensively metabolized, with only a small portion being excreted unchanged in the urine, which makes it a suitable option for patients with renal impairment .
Linagliptin is generally well-tolerated, with a low risk of hypoglycemia when used as monotherapy. However, side effects such as nasopharyngitis, upper respiratory tract infection, and headache have been reported. Rare but serious side effects include acute pancreatitis and hypersensitivity reactions