Which medications in the drug class Antidiabetics, Glucagonlike Peptide-1 Agonists are used in the treatment of Type 2 Diabetes Mellitus?

Updated: Oct 23, 2019
  • Author: Romesh Khardori, MD, PhD, FACP; Chief Editor: George T Griffing, MD  more...
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Answer

Antidiabetics, Glucagonlike Peptide-1 Agonists

Glucagonlike peptide–1 (GLP-1) agonists mimic the endogenous incretin GLP-1, stimulating glucose-dependent insulin release (as opposed to oral insulin secretagogues, which may cause non–glucose-dependent insulin release and hypoglycemia), reducing glucagon, and slowing gastric emptying.

Semaglutide (Ozempic, Rybelsus)

When blood glucose is high, semaglutide, a GLP-1 receptor agonist, lowers it by stimulating insulin secretion and reducing glucagon secretion. It may be administered as a once daily oral tablet or a weekly SC injection.

Exenatide injectable solution (Byetta)

Exenatide is a GLP-1 agonist that improves glycemic control in patients with type 2 diabetes mellitus. Like endogenous incretins, it enhances glucose-dependent insulin secretion by pancreatic beta cells, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying. The drug's 39–amino acid sequence partially overlaps that of the human incretin GLP-1.

Exenatide is indicated as adjunctive therapy to improve glycemic control in patients with type 2 diabetes who have not achieved glycemic control with metformin or a sulfonylurea. The solution is an immediate-release product administered by SC injection twice daily.

Exenatide injectable suspension (Bydureon, Bydureon BCise)

The injectable suspension is administered SC once weekly. The patient does not need to have undergone treatment with Byetta (short-acting exenatide injectable solution) prior to initiating therapy with the injectable suspension. Treatment with Byetta should be discontinued if it is already being used when Bydureon or Bydureon BCise (autoinjector) therapy is started.

Liraglutide (Victoza, Saxenda)

Liraglutide is a once-daily SC injectable GLP-1 receptor agonist that stimulates G-protein in pancreatic beta cells. It increases intracellular cyclic adenosine monophosphate (cAMP), leading to insulin release in the presence of elevated glucose concentrations. Liraglutide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. In addition, evidence from the LEADER clinical trial resulted in liraglutide’s approval for risk reduction of major cardiovascular events (cardiovascular death, nonfatal myocardial infarction, and nonfatal stroke) in adults with type 2 diabetes mellitus and established cardiovascular disease.

It is also indicated for children aged 10 years or older with type 2 diabetes mellitus.

The drug has not been studied in combination with prandial insulin.

Liraglutide is not recommended as first-line pharmacologic therapy, because of potential serious adverse effects. Liraglutide is contraindicated in patients with a history or family history of medullary thyroid carcinoma or multiple endocrine neoplasia syndrome type 2, as dose- and duration-dependent thyroid C-cell tumors have occurred in animal studies of liraglutide.

In addition, clinical studies suggest that liraglutide may cause pancreatitis, although conclusive evidence has not been established. Nevertheless, patients should be monitored for unexplained, persistent, severe abdominal pain, with or without vomiting, and liraglutide should be discontinued if pancreatitis is suspected.

Note that the brand Saxenda is not indicated for the treatment of type 2 diabetes mellitus. Used as an adjunct to a reduced-calorie diet and increased physical activity, Saxenda is indicated for chronic weight management in adults with a BMI of 30 kg/m2 or greater (obesity) or adults with a BMI of 27-29.9 kg/m2 (overweight) and one or more weight-associated conditions (eg, hypertension, type 2 diabetes, dyslipidemia). Saxenda may also be prescribed for persons with overweight and a risk factor for type 2 diabetes. Do not use Saxenda in combination with another GLP-1 agonist or with insulin.

Albiglutide (Tanzeum)

Albiglutide is a once-weekly SC injectable GLP-1 receptor agonist indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It may be used with other antidiabetic agents, although a dose reduction may be needed for insulin secretagogues (eg, sulfonylureas) or insulin if coadministered. GLP-1 receptor agonists augment glucose-dependent insulin secretion.

Dulaglutide (Trulicity)

Dulaglutide is a glucagonlike peptide-1 (GLP-1) agonist that acts as an incretin mimetic. It increase insulin secretion in the presence of elevated blood glucose, delays gastric emptying to decrease postprandial glucose, and decreases glucagon secretion. It is administered as a once-weekly SC injection. It is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Lixisenatide (Adlyxin)

GLP-1 agonist indicated as adjunctive therapy to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It is administered as a once daily SC injection.


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