Sulfonylureas: a new look at old therapy

Curr Diab Rep. 2014 Apr;14(4):473. doi: 10.1007/s11892-014-0473-5.


Sulfonylurea compounds were the first available oral antidiabetic agents and they remain an important tool in our quest for optimal glucose control. The sulfonylureas stimulate the release of insulin from pancreatic β-cells and have a number of extrapancreatic effects, including decreasing hepatic insulin clearance and reducing glucagon secretion in patients with type 2 diabetes. Although these agents have been the mainstay of pharmacotherapy for patients with type 2 diabetes mellitus (T2DM), their safety and clinical utility has been a matter of active debate in recent years, as their use is associated with risks of hypoglycemia and weight gain. We review the discovery and mechanisms of action of sulfonylureas, and the results of clinical trials to provide practical information on the pros and cons of their use in clinical practice. This review addresses advances in our understanding of mechanisms of action of sulfonylurea agents, their efficacy in T2DM, side effects, and impact on cardiovascular disease outcomes.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Blood Glucose / metabolism
  • Cardiovascular Diseases / drug therapy*
  • Cardiovascular Diseases / prevention & control
  • Diabetes Mellitus, Type 2 / blood
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetic Angiopathies / drug therapy*
  • Diabetic Angiopathies / prevention & control
  • Female
  • Humans
  • Hypoglycemia / drug therapy*
  • Hypoglycemia / prevention & control
  • Hypoglycemic Agents* / administration & dosage
  • Hypoglycemic Agents* / adverse effects
  • Hypoglycemic Agents* / pharmacology
  • Insulin / metabolism
  • Male
  • Risk Factors
  • Sulfonylurea Compounds* / administration & dosage
  • Sulfonylurea Compounds* / adverse effects
  • Sulfonylurea Compounds* / pharmacology
  • Treatment Outcome
  • Weight Gain / drug effects


  • Blood Glucose
  • Hypoglycemic Agents
  • Insulin
  • Sulfonylurea Compounds