Class: Dipeptidyl Peptidase IV Inhibitor, Antidiabetic
Dosage Forms. Tablet: 25 mg, 50 mg, 100 mg
Common FDA Label Indication, Dosing, and Titration.
1. Diabetes mellitus: 100 mg po daily
Off-Label Uses. None
MOA. Sitagliptin phosphate is a dipeptidyl peptidase-4 (DPP-4) enzyme inhibitor that inhibits the degradation of incretin hormones by DPP-4, and enhances the function of GLP-1 and GIP to increase insulin release and decrease glucagon levels in the circulation in a glucose-dependent manner.
Drug Characteristics: Sitagliptin
Medication Safety Issues: Sitagliptin
Drug Interactions: Sitagliptin
Adverse Reactions: Sitagliptin
Efficacy Monitoring Parameters. Preprandial blood glucose between 70 and 130 mg/dL, HbA1c <7%.
Toxicity Monitoring Parameters. Monitor renal function and amylase periodically. Seek medical attention if severe skin rash, severe abdominal pain, muscle weakness or pain, or decreased urine production.
Key Patient Counseling Points. Monitor blood glucose in frequent intervals (2-4 times per day). Take with morning meal if once-daily dosing. Take with morning and evening meal if twice-a-day dosing. Avoid alcohol, as it increases the risk of lactic acidosis and may cause a disulfiram reaction.
Clinical Pearls. Not for use in children. Metformin is first-line therapy for Type II diabetes. Sitagliptin may be used as monotherapy in a patient with contraindications to metformin. Incritin mimetics may increase risk of pancreatitis and pancreatic duct metaplasia.