Gliclazide modified release: a critical review of pharmacodynamic, metabolic, and vasoprotective effects
Abstract
Gliclazide modified release (MR) is a new formulation of the drug gliclazide and is given once daily. The specifically designed hydrophilic matrix of gliclazide MR leads to a progressive drug release that parallels the 24-hour glycemic profile in type 2 diabetic patients. Development studies showed a sustained efficacy over 2 years coupled with a very good acceptability. Gliclazide MR acts selectively on adenosine triphosphate-dependent potassium (K(ATP)) channels of the pancreatic beta cell. No interaction with cardiovascular K(ATP) channels has been shown, indicating that the drug can be safely used in patients with ischemic heart disease. In addition, gliclazide MR shows the ability to inhibit key mechanisms in diabetic angiopathy, independently of glycemic control.
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The risk of hypoglycemia of each sulfonylurea relates to its pharmacokinetic properties and is highest with long-acting sulfonylureas such as chlorpropamide, glyburide (glibenclamide), and long-acting glipizide.
“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 [108]
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Hypoglycemia in Type 2 Diabetes
Zammitt, N. N., & Frier, B. M. (2005) · Diabetes Care · doi:10.2337/diacare.28.12.2948 · Cited by 435 · see citing works
Schernthaner, G., Grimaldi, A., Di Mario, U., Drzewoski, J., Kempler, P., Kvapil, M., Novials, A., Rottiers, R., Rutten, G. E. H. M., & Shaw, K. M. (2004) · European Journal of Clinical Investigation · doi:10.1111/j.1365-2362.2004.01381.x · Cited by 271 · see citing works
Self-citationBarnett, A. H., Krentz, A. J., Strojek, K., Sieradzki, J., Azizi, F., Embong, M., Imamoglu, S., Perušičová, J., Uličiansky, V., & Winkler, G. (2008) · Diabetes, Obesity and Metabolism · doi:10.1111/j.1463-1326.2008.00894.x · Cited by 106 · see citing works
- Authors
- Schernthaner, G.
- Affiliations
- Krankenanstalt Rudolfstiftung der Stadt Wien (AT)
- Corresponding author
- Schernthaner, Guntram
- Venue
- Metabolism
- Publisher
- Elsevier BV
- Published
- 2003-08
- Volume
- 52
- Issue
- 8 Suppl 1
- Pages
- 29-34
- ISSN
- 0026-0495 (ISSN-L)
- OpenAlex
- W2108941037
- Cited by
- 66
- References
- 49
- Citations by year
- 2026: 1 · 2024: 3 · 2023: 4 · 2022: 2 · 2021: 1 · 2020: 2 · 2019: 1 · 2018: 9 · 2017: 4 · 2016: 1 · 2015: 1 · 2014: 2 · 2013: 3 · 2012: 3
- FWCI
- 0.32
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Metabolism (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 › Surgery › Pancreatic function and diabetes
- Keywords
- gliclazide modified release, type 2 diabetes, sustained drug release, ATP-sensitive potassium channels, pancreatic beta cells, glycemic control, diabetic vascular disease, vascular protection, ischemic heart disease, drug metabolism, pharmacodynamics
- MeSH terms
- Delayed-Action Preparations, Diabetes Mellitus, Type 2, Diabetic Angiopathies, Drug Administration Schedule, Gliclazide, Humans, Hypoglycemic Agents
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