linagliptin, Tradjenta

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GENERIC NAME: linagliptin

BRAND NAME: Tradjenta

DRUG CLASS AND MECHANISM: Linagliptin is an oral drug that reduces blood sugar (glucose) levels in patients with type 2 diabetes. Linagliptin is a member of a class of drugs that inhibit the enzyme, dipeptidyl peptidase-4 (DPP-4). Other members of this class include sitagliptin (Januvia), and saxagliptin (Onglyza). Following a meal, incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are released from the intestine, and their levels increase in the blood. GLP-1 and GIP reduce blood glucose by increasing the production and release of insulin from the pancreas. GLP-1 also reduces blood glucose by reducing the secretion by the pancreas of the hormone, glucagon, a hormone that increases the production of glucose by the liver and raises the blood level of glucose. The net effect of increased release of GLP-1 and GIP is to reduce blood glucose levels. Linagliptin inhibits the enzyme, DPP-4, that destroys GLP-1 and GIP and thereby increases the levels and activity of both hormones. As a result, levels of GLP-1 and GIP in the blood remain higher, and blood glucose levels fall. In summary, linagliptin reduces blood glucose levels by inhibiting DPP-4 and increasing the levels of GLP-1 and GIP. Linagliptin was approved by the FDA in May 2011.



PREPARATIONS: Tablets: 5 mg

STORAGE: Tablets should be stored at room temperature, 15-30 C (59-86 F)

PRESCRIBED FOR: Linagliptin is combined with diet and exercise to improve blood glucose levels in patients with type 2 diabetes.

DOSING: Linagliptin may be taken with or without food. The recommended dose is 5 mg once daily.

DRUG INTERACTIONS: Rifampin decreases the blood concentration of linagliptin by stimulating break down of linagliptin by CYP3A4 liver enzymes. Other drugs that increase activity CYP3A4 may also reduce the blood concentration of linagliptin.

PREGNANCY: There are no adequate studies of linagliptin in pregnant women.

NURSING MOTHERS: It is unknown whether linagliptin is secreted in human breast milk.

SIDE EFFECTS AND PRECAUTIONS: The most common side effects of linagliptin are stuffy or runny nose and sore throat. Hypoglycemia may occur when linagliptin is combined with insulin or a sulfonylurea-type drug. Allergic reactions and muscle pain also may occur. Pancreatitis also has been reported.

REFERENCE: FDA prescribing information.

Last Editorial Review: 5/19/2011

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