Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor which is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other oral hypoglycemic agents. Linagliptin has been linked to rare instances of clinically apparent liver injury.
Linagliptin (lin" a glip' tin) is an inhibitor of dipeptidyl peptidase-4, which is the major enzyme responsible for the degradation of glucagon-like peptide-1 (GLP-1), an important gastrointestinal hormone (incretin) that increases glucose dependent insulin secretion by the pancreas. By prolonging the effect of GLP-1, linagliptin increases insulin levels and lowers blood glucose, thereby improving glycemic control in patients with type 2 diabetes. Linagliptin was approved for use in the United States in 2011 and was the third DPP-4 inhibitor introduced into clinical practice. Its current indications are for management of glycemic control in type 2 diabetes used in combination with diet and exercise, with or without other oral hypoglycemic agents or insulin. Linagliptin is available in tablets of 5 mg under the brand name Tradjenta and in fixed combinations with metformin under the name Jentadueto and with empagliflozin under the name Glyxambi. The typical dose of linagliptin in adults is 5 to 10 mg once daily. Adverse reactions to linagliptin are not common, but may include headache, nausea, allergic reactions and rash. Hypoglycemia is uncommon with linagliptin alone (<1%), but occurs in higher rates when it is combined with other oral hypoglycemic agents. Rare but potentially severe adverse events reported with linagliptin, as with most DPP-4 inhibitors, include pancreatitis (~0.2%), bullous pemphigoid, severe arthralgias and hypersensitivity reactions.
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