What are examples of sulfonylureas?

Examples of Sulfonylureas

The main commercially available sulfonylureas include gliburide (also called glibenclamide), glimepiride, gliclazide, glipizide, and gliquidone. 1

First-Generation vs. Second-Generation Agents

• First-generation sulfonylureas should generally be avoided due to their prolonged half-lives and substantially greater risk of hypoglycemia compared to second-generation agents. 2

• Second-generation sulfonylureas are preferred and include:

  • Glipizide 1
  • Glimepiride 1
  • Gliclazide 1
  • Gliburide/Glibenclamide 1, 3
  • Gliquidone 1

Preferred Agents Based on Safety Profile

• Glipizide and glimepiride are the preferred sulfonylureas due to their lower risk of hypoglycemia compared to glyburide. 1, 2

• Glyburide should be avoided in older adults due to its longer duration of action and higher risk of prolonged, severe hypoglycemia. 1, 2

• In patients with renal impairment, glipizide is the preferred agent because it lacks active metabolites and does not require dose adjustment. 2

• Gliquidone is recommended for patients with mild renal insufficiency as an alternative option. 1

Mechanism of Action

• All sulfonylureas work as insulin secretagogues, stimulating insulin release from pancreatic β-cells by binding to ATP-sensitive potassium channels. 1, 3

• They can reduce HbA1c levels by 1.0% to 1.5% when used appropriately. 1

Key Clinical Considerations

• The major adverse effect is hypoglycemia, particularly in elderly patients and those with liver or kidney dysfunction. 1

• Weight gain of approximately 2 kg is common following initiation of sulfonylurea therapy. 2

• Sulfonylureas with shorter duration of action (glipizide, glimepiride) are preferred in older adults to minimize hypoglycemia risk. 1, 2