sitagliptin; Januvia

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GENERIC NAME: sitagliptin

BRAND NAME: Januvia

DRUG CLASS AND MECHANISM: Sitagliptin is an oral drug that reduces blood sugar (glucose) levels in patients with type 2 diabetes. Sitagliptin is a member of a class of drugs that inhibit the enzyme, dipeptidyl peptidase-4 (DPP-4) and are therefore called DPP-4 inhibitors. Other members of the class include saxagliptin (Onglyza) and linagliptin (Tradjenta) 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. Sitagliptin inhibits the enzyme, DPP-4, that destroys GLP-1 and GIP and thereby increases the levels and activity of both hormones. As a result, blood glucose levels fall. In summary, sitagliptin reduces blood glucose levels by inhibiting DPP-4 and increasing the levels of GLP-1 and GIP. Sitagliptin was approved by the FDA in October 2006.

GENERIC AVAILABLE: No

PRESCRIPTION: Yes

PREPARATIONS: Tablets: 25, 50, and 100 mg

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

PRESCRIBED FOR: Sitagliptin is combined with diet and exercise to improve blood glucose levels in patients with type 2 diabetes. It also may be combined with other types of oral drugs for diabetes or insulin.

DOSING: Sitagliptin may be taken with or without food. The recommended dose is 100 mg once daily. Renal function should be assessed prior to starting sitagliptin and periodically during treatment. The dose of sitagliptin should be modified based on renal function.

DRUG INTERACTIONS: Sitagliptin may slightly increase the concentration of digoxin (Lanoxin) in the body when both drugs are being taken. Digoxin concentrations should be monitored appropriately. The occurrence of low blood glucose increases when sitagliptin is combined with a sulfonylurea (for example, glyburide [Micronase, Diabeta, Glynase, Prestab]) or insulin. The dose of insulin or sulfonylurea should be reduced.

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

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

SIDE EFFECTS AND PRECAUTIONS: The most common side effects of sitagliptin are upper respiratory tract infection and headache. Sitagliptin also is associated with abdominal pain, nausea and diarrhea. There have been reports of fatal and non-fatal pancreatitis following use of sitagliptin. Acute kidney failure and severe hypersensitivity reactions have also been reported during treatment with sitagliptin.

Reference: FDA Prescribing Information


Last Editorial Review: 3/14/2012




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