Endocrine & Metabolic/DPP-4 inhibitor

DPP-4 inhibitors

also: gliptin · sitagliptin · linagliptin

Overview

Oral, weight-neutral incretin enhancers for T2DM — well tolerated and usable in renal impairment (linagliptin).

Mechanism

Inhibit dipeptidyl peptidase-4, the enzyme that degrades endogenous GLP-1 → modestly raise incretin levels → glucose-dependent insulin secretion. Weight-neutral, oral.

Indications

Type 2 diabetes (oral add-on, esp. if hypoglycaemia/weight a concern or renal impairment)

The agents

Sitagliptinrenally cleared

oral OD

Dose-reduce in renal impairment.

Linagliptinhepatically cleared

oral OD

No dose adjustment needed in renal impairment — useful at low eGFR.

Adverse effects

Generally well toleratedcommon

Pancreatitis (rare)serious

Arthralgiacommon

Cautions & contraindications

History of pancreatitisall

Do not combine with a GLP-1 agonistall

Same incretin pathway.

Interactions

Additive hypoglycaemia with sulfonylureas/insulin

Monitoring & kinetics

HbA1c; renal function (sitagliptin dosing)

Oral OD; weight-neutral.

Choosing it

true

Source: NICE NG28 — T2DM · BNF — DPP-4 inhibitors