Pharmacology · Antidiabetic Drugs (Oral Hypoglycemics, Insulins)

Tirzepatide, approved for type 2 diabetes and obesity, is a 'twincretin.' Which receptors does it simultaneously agonize?

  • A GLP-1 and glucagon receptors
  • B GIP and GLP-2 receptors
  • C GLP-1 and GIP (glucose-dependent insulinotropic polypeptide) receptors
  • D GLP-1 and NPY-Y2 receptors
Correct answer: C. GLP-1 and GIP (glucose-dependent insulinotropic polypeptide) receptors

Explanation

Tirzepatide is a dual GLP-1/GIP receptor agonist (twincretin). By agonizing both GIP and GLP-1 receptors, it achieves greater glucose-dependent insulin secretion, glucagon suppression, gastric emptying delay, and appetite reduction than GLP-1 mono-agonists like semaglutide. GIP receptor agonism in adipose tissue also improves lipid partitioning. Clinical trials (SURPASS program) showed superior HbA1c lowering and weight loss compared to semaglutide, establishing tirzepatide as the most efficacious approved antidiabetic agent.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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