Linagliptin

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Information about Linagliptin

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.

Liver safety of Linagliptin

Linagliptin has been linked to rare instances of clinically apparent liver injury.

Mechanism of action of Linagliptin

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

FDA approval information for Linagliptin

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.

Dosage and administration for Linagliptin

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.

Side effects of Linagliptin

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.

Antidiabetics


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