Medical and Pharmacy Editor: Jay W. Marks, MD

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 the first approved member of a class of drugs that inhibit the enzyme, dipeptidyl peptidase-4 (DPP-4).

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. Sitagliptin may also be combined with metformin, rosiglitazone or pioglitazone.

DOSING: Sitagliptin may be taken with or without food. The recommended dose is 100 mg once daily either alone or in combination with metformin (Glucophage), rosiglitazone (Avandia) or pioglitazone (Actos).

DRUG INTERACTIONS: Sitagliptin may slightly increase the concentration of digoxin in the body when both drugs are being taken. Digoxin concentrations should be monitored appropriately.

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. Sitagliptin did not increase the occurrence of hypoglycemia when administered alone, with metformin or with pioglitazone in human studies.

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