Which medications in the drug class Antidiabetics, Glucagon-like Peptide-1 Agonists are used in the treatment of Insulin Resistance?

Updated: Aug 07, 2019
  • Author: Samuel T Olatunbosun, MD, FACP, FACE; Chief Editor: George T Griffing, MD  more...
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Antidiabetics, Glucagon-like Peptide-1 Agonists

These agents are incretin mimetics. They are analogues of human glucagonlike peptide-1 (GLP-1) and they act as GLP-1 receptor agonists to increase insulin secretion in the presence of elevated blood glucose. These agents delay gastric emptying to decrease postprandial glucose and they also decrease glucagon secretion.

Exenatide (Bydureon, Byetta)

Exenatide, a 39-amino acid incretin mimetic peptide derived from Gila monster hormone exendin-4, is structurally similar to GLP-1. Approved by the FDA for treatment of type 2 diabetes, it enhances glucose-mediated insulin secretion in the beta cell, decreases the pathologic hypersecretion of glucagon in the alpha cell, slows gastric emptying, and induces satiety. It improves postprandial and fasting hyperglycemia without a significant risk of hypoglycemia and promotes weight loss, resulting in increased insulin sensitivity.

The suspension form of exenatide allows once-weekly dosing by subcutaneous administration. Clinical trials observed a statistically significant improvement in HBA1c levels and fasting plasma glucose levels with the long-acting exenatide once-weekly subcutaneous injection compared with the twice-daily subcutaneous injection.

Liraglutide (Victoza)

Liraglutide is an incretin mimetic agent that elicits GLP-1 receptor agonist activity. It activates the GLP-1 receptor by stimulating G-protein in pancreatic beta cells. It also increases intracellular cyclic AMP, leading to insulin release in the presence of elevated glucose concentrations. It produces weight loss, hence an increase in insulin sensitivity.

Liraglutide was originally approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

In December 2014, the FDA approved the drug liraglutide (Saxenda) for the treatment of obesity. It is approved for use in adults with a BMI of 30 or greater (obesity) or adults with a BMI of 27 or greater (overweight) who have at least one weight-related condition such as hypertension, type 2 diabetes, or dyslipidemia.

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