Cited by 308Diabetes Treatment and ManagementDiabetes Management and ResearchPancreatic function and diabetes

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The Role of Sulphonylureas in the Management of Type 2 Diabetes Mellitus

Rendell, Marc·2004·Drugs

DOI 10.2165/00003495-200464120-00006

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Abstract

The sulphonylureas act by triggering insulin release from the pancreatic beta cell. A specific site on the adenosine triphosphate (ATP)-sensitive potassium channels is occupied by sulphonylureas leading to closure of the potassium channels and subsequent opening of calcium channels. This results in exocytosis of insulin. The meglitinides are not sulphonylureas but also occupy the sulphonylurea receptor unit coupled to the ATP-sensitive potassium channel. Glibenclamide (glyburide), gliclazide, glipizide and glimepiride are the primary sulphonylureas in current clinical use for type 2 diabetes mellitus. Glibenclamide has a higher frequency of hypoglycaemia than the other agents. With long-term use, there is a progressive decrease in the effectiveness of sulphonylureas. This loss of effect is the result of a reduction in insulin-producing capacity by the pancreatic beta cell and is also seen with other antihyperglycaemic agents. The major adverse effect of sulphonylureas is hypoglycaemia. There is a theoretical concern that sulphonylureas may affect cardiac potassium channels resulting in a diminished response to ischaemia. There are now many choices for initial therapy of type 2 diabetes in addition to sulphonylureas. Metformin and thiazolidinediones affect insulin sensitivity by independent mechanisms. Disaccharidase inhibitors reduce rapid carbohydrate absorption. No single agent appears capable of achieving target glucose levels in the majority of patients with type 2 diabetes. Combinations of agents are successful in lowering glycosylated haemoglobin levels more than with a single agent. Sulphonylureas are particularly beneficial when combined with agents such as metformin that decrease insulin resistance. Sulphonylureas can also be given with a basal insulin injection to provide enhanced endogenous insulin secretion after meals. Sulphonylureas will continue to be used both primarily and as part of combined therapy for most patients with type 2 diabetes.

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Authors: Rendell, M.
Corresponding author: Rendell, Marc
ORCID: Rendell, Marc
Venue: Drugs
Publisher: Springer Science and Business Media LLC
Published: 2004
Volume: 64
Issue: 12
Pages: 1339-1358
ISSN: 0012-6667 (ISSN-L)
DOI: 10.2165/00003495-200464120-00006
OpenAlex: W2000845410
Cited by: 308
References: 310
Citations by year: 2026: 5 · 2025: 7 · 2024: 7 · 2023: 9 · 2022: 5 · 2021: 11 · 2020: 9 · 2019: 10 · 2018: 16 · 2017: 13 · 2016: 19 · 2015: 17 · 2014: 19 · 2013: 21 · 2012: 22
FWCI: 2.42
Type: journal article
Language: en
Open access: closed
Locations: Drugs (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Management and Research
Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Pancreatic function and diabetes
Keywords: sulfonylureas, type 2 diabetes, insulin secretion, ATP-sensitive potassium channels, sulfonylurea receptor, glibenclamide, gliclazide, glipizide, glimepiride, hypoglycemia, meglitinides, metformin, thiazolidinediones, combination therapy, glycosylated haemoglobin, basal insulin, insulin resistance
MeSH terms: Benzamides, Clinical Trials as Topic, Diabetes Mellitus, Type 2, Drug Therapy, Combination, Humans, Hypoglycemic Agents, Insulin, Sulfonylurea Compounds, Treatment Failure

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The Role of Sulphonylureas in the Management of Type 2 Diabetes Mellitus

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