Effects of Glimepiride on Insulin and Glucagon Release from Isolated Rat Pancreas at Different Glucose Concentrations

Overview

Journal Acta Diabetol

Specialty Endocrinology

Date 1996 Mar 1

PMID 8777281

Citations 3

Authors

F Gregorio

F Ambrosi

S Cristallini

P Filipponi

F Santeusanio

Affiliations

Soon will be listed here.

Abstract

The effects of glimepiride, the newest sulphonylureic compound, on pancreatic insulin and glucagon secretion were studied using the classical, isolated, perfused rat pancrease model. The influence of four different environmental glucose conditions (during a glycaemic stimulus with glucose increasing from 5 to 8.33 mM and at stable 0, 5 and 2.22 mM glucose levels) on the effects of glimepiride was also assessed. At a pharmacological concentration glimepiride strongly stimulated beta-cell activity, producing a characteristic biphasic insulin release with a sharp first-phase secretory peak, followed by a prolonged and sustained second phase. Environmental glucose concentrations markedly influenced the extent, but not the pattern of glimepiride-induced insulin secretion, as hormone release dropped significantly when the glucose level was reduced. Glimepiride failed to influence alpha-cell activity at any of the environmental glycaemic levels.

Citing Articles

Egr-1 decreases adipocyte insulin sensitivity by tilting PI3K/Akt and MAPK signal balance in mice.

Yu X, Shen N, Zhang M, Pan F, Wang C, Jia W EMBO J. 2011; 30(18):3754-65.

PMID: 21829168 PMC: 3173797. DOI: 10.1038/emboj.2011.277.

The role of sulphonylureas in the management of type 2 diabetes mellitus.

Rendell M Drugs. 2004; 64(12):1339-58.

PMID: 15200348 DOI: 10.2165/00003495-200464120-00006.

Glimepiride. A review of its use in the management of type 2 diabetes mellitus.

Langtry H, Balfour J Drugs. 1998; 55(4):563-84.

PMID: 9561345 DOI: 10.2165/00003495-199855040-00007.

References

Gregorio F, Ambrosi F, Cristallini S, Pedetti M, Filipponi P, Santeusanio F . Therapeutical concentrations of tolbutamide, glibenclamide, gliclazide and gliquidone at different glucose levels: in vitro effects on pancreatic A- and B-cell function. Diabetes Res Clin Pract. 1992; 18(3):197-206. DOI: 10.1016/0168-8227(92)90146-i. View

Bolli G, De Feo P, Perriello G, De Cosmo S, Compagnucci P, Santeusanio F . Mechanisms of glucagon secretion during insulin-induced hypoglycemia in man. Role of the beta cell and arterial hyperinsulinemia. J Clin Invest. 1984; 73(4):917-22. PMC: 425102. DOI: 10.1172/JCI111315. View

Muller G, Satoh Y, Geisen K . Extrapancreatic effects of sulfonylureas--a comparison between glimepiride and conventional sulfonylureas. Diabetes Res Clin Pract. 1995; 28 Suppl:S115-37. DOI: 10.1016/0168-8227(95)01089-v. View

Akkan A, Marchand J, Malaisse W . Effects of glimepiride and glibenclamide on insulin and glucagon secretion by the perfused rat pancreas. Biochem Pharmacol. 1991; 42(8):1634-7. DOI: 10.1016/0006-2952(91)90435-8. View

Gregorio F, Ambrosi F, Filipponi P, Cristallini S, Santeusanio F . Glucose modulates the amount, but not the kinetics, of insulin released by sulfonylureas. J Diabetes Complications. 1994; 8(4):204-12. DOI: 10.1016/1056-8727(94)90045-0. View

Tsalikian E, Dunphy T, Bohannon N, Lorenzi M, Gerich J, FORSHAM P . The effect of chronic oral antidiabetic therapy on insulin and glucagon responses to a meal. Diabetes. 1977; 26(4):314-21. DOI: 10.2337/diab.26.4.314. View

Gerich J . Oral hypoglycemic agents. N Engl J Med. 1989; 321(18):1231-45. DOI: 10.1056/NEJM198911023211805. View

Leahy J, Bonner-Weir S, Weir G . Beta-cell dysfunction induced by chronic hyperglycemia. Current ideas on mechanism of impaired glucose-induced insulin secretion. Diabetes Care. 1992; 15(3):442-55. DOI: 10.2337/diacare.15.3.442. View

Filipponi P, Gregorio F, Cristallini S, Ferrandina C, Nicoletti I, Santeusanio F . Selective impairment of pancreatic A cell suppression by glucose during acute alloxan-induced insulinopenia: in vitro study on isolated perfused rat pancreas. Endocrinology. 1986; 119(1):408-15. DOI: 10.1210/endo-119-1-408. View

10.

Groop L . Sulfonylureas in NIDDM. Diabetes Care. 1992; 15(6):737-54. DOI: 10.2337/diacare.15.6.737. View

11.

Scharff R, Wool I . CONCENTRATION OF AMINO ACIDS IN RAT MUSCLE AND PLASMA. Nature. 1964; 202:603-4. DOI: 10.1038/202603a0. View

12.

Pek S, FAJANS S, FLOYD Jr J, Knopf R, CONN J . Failure of sulfonylureas to suppress plasma glucagon in man. Diabetes. 1972; 21(4):216-23. DOI: 10.2337/diab.21.4.216. View

13.

Maruyama H, HISATOMI A, Orci L, GRODSKY G, Unger R . Insulin within islets is a physiologic glucagon release inhibitor. J Clin Invest. 1984; 74(6):2296-9. PMC: 425424. DOI: 10.1172/JCI111658. View

14.

Kramer W, Oekonomopulos R, Punter J, SUMM H . Direct photoaffinity labeling of the putative sulfonylurea receptor in rat beta-cell tumor membranes by [3H]glibenclamide. FEBS Lett. 1988; 229(2):355-9. DOI: 10.1016/0014-5793(88)81155-4. View

15.

Samols E, Tyler J, MIALHE P . Suppression of pancreatic glucagon release by the hypoglycaemic sulphonylureas. Lancet. 1969; 1(7587):174-6. DOI: 10.1016/s0140-6736(69)91189-1. View

16.

Eriksson J, Ekstrand A, Saloranta C, Widen E, Schalin C, Groop L . Early metabolic defects in persons at increased risk for non-insulin-dependent diabetes mellitus. N Engl J Med. 1989; 321(6):337-43. DOI: 10.1056/NEJM198908103210601. View

17.

DeFronzo R . Lilly lecture 1987. The triumvirate: beta-cell, muscle, liver. A collusion responsible for NIDDM. Diabetes. 1988; 37(6):667-87. DOI: 10.2337/diab.37.6.667. View

18.

Kramer W, Muller G, Girbig F, Gutjahr U, Kowalewski S, Hartz D . Differential interaction of glimepiride and glibenclamide with the beta-cell sulfonylurea receptor. II. Photoaffinity labeling of a 65 kDa protein by [3H]glimepiride. Biochim Biophys Acta. 1994; 1191(2):278-90. DOI: 10.1016/0005-2736(94)90178-3. View

19.

Badian M, Korn A, Lehr K, Malerczyk V, Waldhausl W . Determination of the absolute bioavailability of glimepiride (HOE 490), a new sulphonylurea. Int J Clin Pharmacol Ther Toxicol. 1992; 30(11):481-2. View

20.

Draeger E . Clinical profile of glimepiride. Diabetes Res Clin Pract. 1995; 28 Suppl:S139-46. DOI: 10.1016/0168-8227(95)01072-l. View