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Comparison of the Effects of Three Sulfonylureas on in vivo Insulin Action
- Source :
- Arzneimittelforschung. 51:459-464
- Publication Year :
- 2011
- Publisher :
- Georg Thieme Verlag KG, 2011.
-
Abstract
- To clarify the diversity in hypoglycemic actions of sulfonylureas, chronic effects of three sulfonylureas were compared on in vivo insulin-induced glucose uptake in peripheral tissues. After oral administration of glimepiride (CAS 93479-97-1), glibenclamide (CAS 10238-21-8), gliclazide (CAS 21187-98-4), or saline as control, two-step euglycemic clamp procedures were performed. During physiological hyperinsulinemia induced by 6 mU/kg/min insulin infusion, metabolic clearance rates (MCR) of glucose of the glimepiride-administered group (GP) significantly (p0.01) increased to 153% of the saline-administered group (SA). There was no significant statistical difference between the glibenclamide-administered group (GC), gliclazide-administered group (GZ) and SA. During 30 mU/kg/min clamps that lead to maximal insulin action, MCR of either GP or GC were significantly higher than those of SA (128% and 141%, p0.05 and p0.01, respectively). MCR of GZ were lower than those of GC (80%, p0.05), and showed no significant difference from those of SA. These data indicate that glimepiride activates insulin binding levels to a greater degree than the other two sulfonylureas, and that glibenclamide and glimepiride activate post-receptor binding mechanisms in peripheral tissues much more than gliclazide. These results suggest that hypoglycemic actions of sulfonylureas at the extra pancreatic levels vary with the nature of each reagent.
- Subjects :
- Blood Glucose
Male
medicine.medical_specialty
Glucose uptake
medicine.medical_treatment
Glibenclamide
In vivo
Oral administration
Hyperinsulinism
Internal medicine
Drug Discovery
medicine
Animals
Hypoglycemic Agents
Insulin
Gliclazide
Rats, Wistar
Pancreatic hormone
Dose-Response Relationship, Drug
business.industry
Body Weight
Rats
Glimepiride
Sulfonylurea Compounds
Endocrinology
Glucose Clamp Technique
business
human activities
medicine.drug
Subjects
Details
- ISSN :
- 16167066 and 00044172
- Volume :
- 51
- Database :
- OpenAIRE
- Journal :
- Arzneimittelforschung
- Accession number :
- edsair.doi.dedup.....2caec90d1395e8f1cdd4a6f475184f83