Top 300 Pharmacy Drug Cards


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.

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