The DOI matches its Crossref record; 310 of the 310 references it cites were found in a registry or an index.
The Role of Sulphonylureas in the Management of Type 2 Diabetes Mellitus
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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“Glyburide is associated with significantly more episodes of severe hypoglycemia than gliclazide (112) because its hypoglycemic effects last for 24 h (111) as a consequence of the presence of active metabolites (111,113).”
From Hypoglycemia in Type 2 Diabetes (2005) · cites this paper as [111]
In the citing paper
“The risk of hypoglycemia of each sulfonylurea relates to its pharmacokinetic properties (104 -108) and is highest with long-acting sulfonylureas such as chlorpropamide, glyburide (glibenclamide), and long-acting glipizide (101,109 -111).”
From Hypoglycemia in Type 2 Diabetes (2005) · cites this paper as [111]
Citations
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Cited by
Sorted by citations
Type 2 diabetes: principles of pathogenesis and therapy
Stumvoll, M., Goldstein, B. J., & van Haeften, T. W. (2005) · The Lancet · doi:10.1016/s0140-6736(05)61032-x · Cited by 2,662
Hypoglycemia in Type 2 Diabetes
Zammitt, N. N., & Frier, B. M. (2005) · Diabetes Care · doi:10.2337/diacare.28.12.2948 · Cited by 435
Pharmacology and therapeutic implications of current drugs for type 2 diabetes mellitus
Tahrani, A. A., Barnett, A. H., & Bailey, C. J. (2016) · Nature Reviews Endocrinology · doi:10.1038/nrendo.2016.86 · Cited by 398
Avoiding hypoglycemia: a key to success for glucose-lowering therapy in type 2 diabetes
Ahren, B. (2013) · Vascular Health and Risk Management · doi:10.2147/vhrm.s33934 · Cited by 148
Paneni, F., & Lüscher, T. F. (2017) · The American Journal of Cardiology · doi:10.1016/j.amjcard.2017.05.015 · Cited by 83
Metadata
- Authors
- Rendell, M.
- Corresponding author
- Rendell, Marc
- ORCID
- Rendell, Marc
- Venue
- Drugs
- Published
- 2004
- Volume
- 64
- Issue
- 12
- Pages
- 1339-1358
- ISSN
- 0012-6667 (ISSN-L)
- 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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