Classifications: hormone modifier; antidiabetic agent; dipeptidyl peptidase-4 (dpp-4) inhibitor; incretin modifier; Therapeutic:antidiabetic; incretin modifier; dpp-4 inhibitor
Pregnancy Category: B
25 mg, 50 mg, and 100 mg tablets
Sitagliptin slows inactivation of incretin hormones [e.g., glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic
polypeptide (GIP)] that are released by the intestine. As plasma glucose rises, incretin hormones stimulate release of insulin
from the pancreas, and GLP-1 also lowers glucagon secretion, resulting in reduced hepatic glucose production.
Sitagliptin elevates the level of incretin hormones, thus increasing insulin secretion and reducing glucagon secretion.
Sitagliptin lowers both fasting and postprandial plasma glucose levels.
Adjunct treatment of type 2 diabetes mellitus in combination with exercise and diet.
Type I diabetes mellitus, diabetic ketoacidosis. Safety and efficacy in children <18 y are not known.
Moderate to severe renal impairment, renal failure, hemodialysis; older adults; pregnancy (category B), lactation.
Route & Dosage
|Type 2 Diabetes Mellitus
Adult: PO 100 mg/d
Clcr >30 mL/min and <50 mL/min: 50 mg/d
<30 mL/min: 25 mg/d
- May be given without regard to meals.
- Note that dosage adjustment is recommended for moderate to severe renal impairment.
- Store at 20°25° C (68°77° F).
Adverse Effects (≥1%)CNS:
Nasopharyngitis, upper respiratory tract infection.
Sitagliptin may increase digoxin
87% absorbed. Peak:
14 h. Distribution:
38% protein bound. Metabolism:
20% metabolized in the liver. Elimination:
Primarily renal (87%) with minor elimination in the kidneys. Half-Life:
Assessment & Drug Effects
- Monitor for and report S&S of significant GI distress, including NV&D.
- Monitor for S&S of hypoglycemia when used in combination with a sulfonylurea drug or insulin.
- Lab tests: Baseline and periodic Clcr; periodic fasting and postprandial plasma glucose and HbA1C.
- Monitor blood levels of digoxin with concurrent therapy.
Patient & Family Education
- Follow directions for taking the drug (see Administration).
- Note: When taken alone to control diabetes, sitagliptin is unlikely to cause hypoglycemia because it only works when your
blood sugar is rising.