Linagliptin
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Linagliptin
Tradjenta; with metformin Jentadueto
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Summary
Pharmacy
Starting dose
5 mg PO once daily (no renal dose adjustment, unlike sitagliptin)
Preparations
5 mg tablets; combination with metformin
US FDA Max
5 mg/d
Pharmacology
Routes
Oral
Onset
Postprandial glucose effect within days; HbA1c by 12 weeks
Duration
24 hours
Half-life
~12 hours (effective); terminal much longer[1]
Bioavailability
~30% (oral)[1]
Pregnancy
Limited data; switch to insulin where feasible.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Linagliptin 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 Unlike other gliptins, linagliptin is predominantly biliary-cleared rather than renal, making it the only DPP-4 inhibitor that does not require dose adjustment in CKD — its clinical niche. Class adverse effects (pancreatitis signal, severe joint pain, bullous pemphigoid) apply[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Tradjenta (linagliptin), Boehringer Ingelheim, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/201280s029lbl.pdf