Comparative effects of glimepiride and glibenclamide on blood glucose, C-peptide and insulin concentrations in the fasting and postprandial state in normal man
Abstract
A single-center, randomised, placebo- controlled, cross-over study was conducted to characterize the new sulfonylurea glimepiride and to compare its profile of action with the second generation sulfonylurea glibenclamide. The total duration of each experiment was 5 hours. At zero time an i.v. injection of 2 and 4 mg glimepiride, 1 mg glibenclamide or placebo was given i.v. to 24 healthy volunteers. Blood samples were collected for three hours after the injection (0-3 hours, preprandial experiment). At 3 hours, a standard mixed meal was given (20%, of a 30 Kcal/Kg Body Weight diet) and blood samples were collected for 2 more hours (postprandial experiment). Pre-prandially (0-3 hrs) blood glucose (expressed as the area under the curve divided by the time) was significantly lower (p < 0.0001) after the administration of 2 and 4 mg glimepiride (3.8 +/- 0.22 and 3.5 +/- 0.3 mM respectively) compared to placebo (4.63 +/- 0.31 mM), but not compared to glibenclamide. Insulin and C-peptide were not different after glimepiride or glibenclamide. Both glimepiride and glibenclamide had similar effects on insulin secretion. Post-prandially (3-5 hrs) blood glucose was significantly higher after glibenclamide (6.54 +/- 0.8 mM) (p < 0.0001) than after 2 mg glimepiride (5.75 +/- 0.5 mM). Despite this C-peptide was significantly higher (p < 0.002) glibenclamide (5.7 +/- 1.5 ng/ml) compared to glimepiride (5.1 +/- 1.3 ng/ml); the trend was the same for insulin but the results were not significan…
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Glimepiride, a long-acting sulfonylurea, may partly fulfil the role of a sulfonylurea with good glycemic control and low risk of hypoglycemia as it has a lower affinity for the β-cell receptor than glyburide, and its insulin secretory capacity is lower in both the fasting and postprandial states.
“Glimepiride, a long-acting sulfonylurea, may partly fulfil this role as it has a lower affinity for the -cell receptor than glyburide (117), and its insulin secretory capacity is lower in both the fasting (118) and postprandial (119) states.”
From Hypoglycemia in Type 2 Diabetes (2005) · cites this paper as [119]
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Cited by 20
- Authors
- Raptis, S., Hatziagelaki, E., Dimitriadis, G., Draeger, K., Pfeiffer, C., & Raptis, A.
- Affiliations
- National and Kapodistrian University of Athens (GR)
- Venue
- Experimental and Clinical Endocrinology & Diabetes
- Publisher
- Georg Thieme Verlag KG
- Published
- 2009-07-14
- Volume
- 107
- Issue
- 06
- Pages
- 350-355
- ISSN
- 0947-7349 (ISSN-L)
- 1439-3646
- OpenAlex
- W2000466010
- Cited by
- 20
- References
- 0
- Citations by year
- 2023: 1 · 2017: 1 · 2016: 1 · 2015: 1 · 2014: 1 · 2012: 1
- FWCI
- 0.48
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Experimental and Clinical Endocrinology & Diabetes (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Health Sciences › Medicine › Surgery › Pancreatic function and diabetes
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Management and Research
- Keywords
- glimepiride, glibenclamide, sulfonylureas, blood glucose, C-peptide, insulin secretion, postprandial hyperglycemia, fasting blood glucose, oral glucose tolerance, healthy volunteers, drug comparison, insulin sensitivity, beta-cell function, mixed meal tolerance test, intravenous administration, hypoglycemia risk, type 2 diabetes treatment
- MeSH terms
- Adolescent, Adult, Blood Glucose, C-Peptide, Double-Blind Method, Fasting, Food, Glyburide, Humans, Hypoglycemic Agents, Insulin, Kinetics, Male, Middle Aged, Placebos, Sulfonylurea Compounds, Cross-Over Studies
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