Adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus as monotherapy or as combination therapy.
Adults: PO 100 mg once daily.
Renal Function Impairment
Moderate renal impairment (CrCl 30 to less than 50 mL/min): PO 50 mg once daily.
Severe renal impairment (CrCl less than 30 mL/min) or ESRD requiring hemodialysis or peritoneal dialysis: PO 25 mg once daily. Administer without regard to the timing of hemodialysis.
Sitagliptin is a dipeptidyl peptidase-4 inhibitor that is thought to act in type 2 diabetes by slowing the inactivation of incretin hormones.
CNS: Headache (1%).
EENT: Nasopharyngitis (5%).
GI: Diarrhea (3%); abdominal pain (2%); nausea (1%); acute pancreatitis, hepatic enzyme elevations (postmarketing).
HYPERSEN: Hypersensitivity reactions, including anaphylaxis, angioedema, cutaneous vasculitis, exfoliative skin conditions (including Stevens-Johnson syndrome), rash, and urticaria (postmarketing)
RESP: Upper respiratory tract infection (5%).
Sitagliptin plasma concentrations may be increased modestly (approximately 68%), which is not expected to be clinically important.
Digoxin plasma concentrations may be increased slightly (approximately 18%); no dosage adjustment is recommended.
Sulfonylurea (eg, tolbutamide)
A lower dose of the sulfonylurea may be needed to reduce the risk of hypoglycemia.
Therapeutic Classification: antidiabetics
Pharmacologic Classification: enzyme inhibitors
Absorption: 87% absorbed following oral administration.
Metabolism/Excretion: 79% excreted unchanged in urine, minor metabolism.
Half-life: 12.4 hr.
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