Sulfonylureas generalized structure

The generalized structure of sulfonylureas

Sulfonylureas (or sulphonylureas) are a class of antidiabetics used in the treatment of type 2 diabetes mellitus (T2DM) that induce insulin release by the β cells of the pancreas via binding to the sulfonylurea receptors (SUR). SURs are expressed on the ATP-sensitive potassium channels (KATP), sulfonylureas inhibit the activity of KATP channels which, in turn, leads to the secretion of insulin.[1] They are amongst the oldest oral antidiabetic agents available for the treatment of T2DM, along with metformin and also, like metformin they constitute the first-line drug therapies used to treat T2DM.

Clinical purpose and useEdit

Their purpose, like other antidiabetic agents, is to lower blood glucose levels and like most antidiabetic agents they have been found effective in preventing microvascular, but not macro- or non-vascular complications of T2DM.[2] In fact there is some evidence to support the idea that it might increase the risk of macrovascular[3] and cancer-related complications.[4]

Nowadays the second-generation sulfonylureas (SGSs) are significantly more frequently used than their first-generation counterparts, in fact, in Australia and New Zealand the only available sulfonylureas are second-generation agents. SGSs have a few advantages over the first-generation sulfonylureas (FGSs): one, they are more potent, two their dosing is usually more convenient at once or twice daily and three their side effects, including their interaction with alcohol tends to be less problematic.[5]


First-generation sulfonylureas include:

  • Tolbutamide

Second-generation sulfonylureas include:


2D structure of glibenclamide


3D animated structure of glibenclamide[note 1]


  1. This is an animated structure, click the structure to see a rotating version of it

Reference listEdit

  1. Powers, AC; D'Alessio, D (2011). "Chapter 43. Endocrine Pancreas and Pharmacotherapy of Diabetes Mellitus and Hypoglycemia". In Brunton, LL; Chabner, BA; Knollmann, BC. Goodman & Gilman's The Pharmacological Basis of Therapeutics. AccessMedicine (New York, USA: McGraw-Hill). Retrieved 28 September 2014. 
  2. Kar, P; Holt, RI (June 2008). "The effect of sulphonylureas on the microvascular and macrovascular complications of diabetes.". Cardiovascular Drugs and Therapy 22 (3): 207–13. PMID 18288596. doi:10.1007/s10557-008-6090-2. 
  3. Phung, OJ; Schwartzman, E; Allen, RW; Engel, SS; Rajpathak, SN (October 2013). "Sulphonylureas and risk of cardiovascular disease: systematic review and meta-analysis.". Diabetic Medicine 30 (10): 1160–71. PMID 23663156. doi:10.1111/dme.12232. 
  4. Thakkar, B; Aronis, KN; Vamvini, MT; Shields, K; Mantzoros, CS (July 2013). "Metformin and sulfonylureas in relation to cancer risk in type II diabetes patients: a meta-analysis using primary data of published studies.". Metabolism 62 (7): 922–34. PMID 23419783. doi:10.1016/j.metabol.2013.01.014. 
  5. "Second Generation Sulfonylureas". LiverTox. Bethesda, USA: U.S. National Library of Medicine. 10 September 2014. Retrieved 1 October 2014. 

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