The Medical Letter on Drugs and Therapeutics
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Exenatide (Byetta) for Type 2 Diabetes

Exenatide injection (Byetta – Amylin/Lilly), a synthetic peptide that stimulates release of insulin from pancreatic beta cells, has been approved by the FDA as adjunctive therapy for patients with type 2 diabetes who have not achieved optimal glycemic control on metformin (Glucophage, and others), a sulfonylurea, such as glyburide (DiaBeta, and others), or both. Exenatide is not indicated for use with insulin.

MECHANISM OF ACTION — Several peptide hormones (incretins) are released from cells in the gastrointestinal tract in response to food. Glucagon-like peptide-1 (GLP-1) is one of these. Exenatide is a GLP-1 agonist (incretin mimetic); it potentiates insulin secretion, inhibits secretion of glucagon, slows gastric emptying and promotes satiety. In patients with diabetes, this results in modest lowering of fasting glucose and marked reduction of postprandial levels. Animal studies have ... more      

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