Sitagliptin

Category: pharmacological

Aliases: Januvia, MK-0431

Pharmacological Mechanism

Competitive, reversible DPP-4 (dipeptidyl peptidase-4) inhibitor — blocks degradation of the endogenous incretins GLP-1 and GIP, raising their plasma levels 2–3× and potentiating glucose-dependent insulin release plus glucagon suppression. Weight-neutral, low hypoglycaemia risk (glucose-dependent action). CV-neutral (TECOS trial).

Half-Life (t½)

PO: 10.4h

Dosing Guidelines

• PO: Typical 100mg (Range: 100 - 100 mg)

Target Organ Systems

• endocrine

Interactions

• Metformin
• Semaglutide / GLP-1 RAs