Trade Names:Januvia- Tablets 25 mg- Tablets 50 mg- Tablets 100 mg
Sitagliptin is a dipeptidyl peptidase-4 inhibitor that is believed to act in type 2 diabetes by slowing the inactivation of incretin hormones.
Sitagliptin is rapidly absorbed, with 100 mg reaching a C max of 950 nM in 1 to 4 h. The bioavailability is approximately 87%.
Vd is approximately 198 L. Plasma protein binding is 38%.
Metabolism by CYP3A4 and, to a lesser degree, CYP2C8 is a minor pathway in the Cl of sitagliptin.
Terminal t ½ is approximately 12.4 h. Approximately 13% is excreted in feces and 87% in urine via active tubular secretion (79% as unchanged drug). Sitagliptin is a substrate for organic anion transport.
Adjunct to diet and exercise in type 2 diabetes mellitus as monotherapy or in combination with metformin or a thiazolidinedione (eg, rosiglitazone) when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
PO 100 mg once daily with or without food.Renal Function ImpairmentAdults
PO Moderate renal function impairment (CrCl 30 to less than 50 mL/min): 50 mg once daily. Severe renal function impairment (CrCl less than 30 mL/min): 25 mg once daily.
Store at 59° to 86°F.
Sitagliptin plasma concentrations may be increased modestly (approximately 68%), which is not expected to be clinically important.Digoxin
Digoxin plasma levels may be increased slightly (approximately 18%); no dosage adjustment is recommended.
None well documented.
Headache (at least 5%).
Nasopharyngitis (at least 5%).
Diarrhea (3%); nausea (1%).
Upper respiratory tract infection (at least 5%).
Category B .
Safety and efficacy not established.
Dosage adjustments are needed in patients with moderate or severe renal function impairment.
Mean increases in QTc interval of 8 msec, which were not considered clinically important, were observed at a dose of 800 mg. There is no experience with doses above 800 mg.
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