Medication Review: Describe The Mechanism of Action of Tirzepatide

April 2026

Explore the mechanism of action of tirzepatide in this comprehensive medication review led by Bharati Bhardwaja, PharmD, from Kaiser Permanente Colorado. This video breaks down how tirzepatide, a first-in-class dual incretin receptor agonist, targets both glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors to improve metabolic outcomes. Learn how this once-weekly injectable therapy is FDA-approved for improving glycemic control in patients with Type 2 Diabetes and for chronic weight management in adults with obesity or overweight with comorbidities, including its role in treating obstructive sleep apnea.

This educational module provides a detailed, clinically relevant overview of tirzepatide’s effects across multiple organ systems. Discover how GLP-1 receptor activation reduces appetite, slows gastric emptying, enhances insulin secretion, and decreases glucagon release, while GIP receptor agonism further supports insulin regulation, improves tolerability, and enhances fat metabolism. The combined incretin effect results in improved insulin sensitivity, reduced inflammation in adipose tissue, decreased hepatic glucose production, and meaningful weight loss outcomes. Ideal for healthcare professionals and advanced practice providers, this video offers valuable insights into the pharmacology, therapeutic benefits, and real-world applications of tirzepatide in metabolic disease management.

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