Medications and Drugs
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.
Reference: FDA Prescribing Information
Last Editorial Review: 4/25/2007
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
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