Sitagliptin
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Sitagliptin
Januvia; with metformin Janumet/Janumet XR
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Summary
Common uses
Type 2 diabetes mellitus0
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[1]
Bioavailability
~87% (oral)[1]
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)[1].
References
edit- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Januvia (sitagliptin), Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021995s041lbl.pdf