Mechanism of Action: Tirzepatide is a synthetic peptide agonist of both the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor, enhancing glucose-dependent insulin secretion, slowing gastric emptying, and reducing appetite.
Indications & Off-Label Uses: FDA-approved for type 2 diabetes mellitus and chronic weight management. Off-label uses may include targeted obesity management in patients without diabetes and experimental metabolic optimization for body composition and cardiometabolic health. Evidence for these off-label uses is emerging but limited.
FDA Status: Approved for type 2 diabetes and weight management; other uses are off-label.
Clinical Evidence: Clinical trials demonstrate significant reductions in HbA1c, body weight, and cardiovascular risk factors in patients with type 2 diabetes and obesity. Evidence in non-diabetic populations for performance, anti-aging, or general metabolic optimization is limited.
Safety & Monitoring: Common adverse effects include nausea, vomiting, diarrhea, and constipation. Rare but serious risks include pancreatitis, gallbladder disease, and potential thyroid C-cell tumors (based on animal studies). Monitoring of glycemic control, gastrointestinal symptoms, and other metabolic parameters is recommended.
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