Sitagliptin

DPP-4 inhibitor, Antihyperglycemic agent, Incretin pathway modulator

Sitagliptin

Januvia; with metformin Janumet/Janumet XR

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Summary

Classes

DPP-4 inhibitor, Antihyperglycemic agent, Incretin pathway modulator

Common uses

Type 2 diabetes mellitus▲0▼

Pharmacy

Starting dose

100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis)

Preparations

25, 50, 100 mg tablets; combination tablets with metformin

US FDA Max

100 mg/d

Pharmacology

Routes

Oral

Onset

Postprandial glucose effect within days; HbA1c by 12 weeks

Duration

24 hours

Half-life

~12.4 hours

Bioavailability

~87% (oral)

Pregnancy

Limited data; switch to insulin where feasible.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Sitagliptin reversibly inhibits dipeptidyl peptidase-4 (DPP-4), extending the half-life of the endogenous incretins GLP-1 and GIP; the resulting glucose-dependent increase in insulin secretion and decrease in glucagon lowers fasting and postprandial glucose without significant hypoglycemia risk as monotherapy.▲0▼ Largely renally cleared, hence the eGFR-tiered dosing. Rare but well-documented signals: acute pancreatitis (uncertain causal contribution), severe joint pain, and bullous pemphigoid (class effect, especially in older Asian patients).