Summary
Glibenclamide, a “second generation” sulfonylurea, produced the same pattern of insulin release from the perfused rat pancreas as did tolbutamide. The stimulatory effect was closely dependent on the glucose concentration present. Both agents enhanced insulin secretion at 5–10 mM glucose, whereas no additional insulin was released when maximally stimulating levels of glucose (20 and 30 mM) were present. The concentrations of glibenclamide stimulating insulin release were 100–400 times lower than equieffective levels of tolbutamide. At glucose levels of 3 or 8 mM, however, glibenclamide did not liberate significantly more insulin from the pancreas than did tolbutamide. Thus the differences of tolbutamide and glibenclamide were quantitative rather than qualitative. Although the active concentrations differed the effects produced were comparable.
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Aumüller, W., Bänder, A., Heerdt, R., Muth, K., Pfaff, W., Schmidt, F. H., Weber, H., Weyer, R.: Ein neues hochwirksames orales Antidiabetikum. Arzneim.-Forsch. (Drug Res.) 16, 1640–1641 (1966)
Basabe, J. C., Farina, J. M. S., Chieri, R. A.: Studies in the dynamics and mechanism of glibenclamide-induced insulin secretion. Horm. Métab. Res. 8, 413–419 (1976)
Bosboom, R. S., Zweens, J., Bouman, P. R.: Effects of feeding and fasting on the insulin secretory response to glucose and sulfonylureas in intact rats and isolated perfused rat pancreas. Diabetologia 9, 243–250 (1973)
Fußgänger, R. D., Goberna, R., Hinz, M., Jaros, P., Karsten, C., Pfeiffer, E. F., Raptis, S.: Comparative studies on the dynamics of insulin secretion following HB 419 and tolbutamide of the perfused isolated rat pancreas and the perifused isolated pieces and islets of rat pancreas. Horm. Metab. Res. 1, Suppl., 34–40 (1969)
Grodsky, G. M., Batts, A. A., Bennett, L. L., Vcella, C., McWilliams, N. B., Smith, D. F.: Effects of carbohydrates on secretion of insulin from isolated rat pancreas. Am. J. Physiol. 205, 638–644 (1963)
Haydú, P., Kohler, K. F., Schmidt, F. H., Spingler, H.: Physikalisch-chemische und analytische Untersuchungen an HB 419. Arzneim.-Forsch. 19, 1381–1386 (1969).
Haupt, E., Köberich, W., Beyer, J., Schöffling, K.: Pharmacodynamic aspects of tolbutamide, glibenclamide, glibonuride, and glisoxepide. Diabetologia 7, 449–460 (1971)
Hellman, B.: Potentiating effects of drugs on the binding of glibenclamide to pancreatic beta cells. Metabolism 23, 839–846 (1974)
Joost, H. G., Beckmann, J., Holze, S., Lenzen, S., Poser, W., Hasselblatt, A.: Inhibition of insulin and glucagon release from the perfused rat pancreas by cyproheptadine. Diabetologia 12, 201–206 (1976)
Loubatières, A., Mariani, M. M., Chapal, J.: Insulino-sécrétion étudièe sur le pancréas isolé et perfusé du rat. I. Synergie entre glucose et sulfamides hypoglycémiants. Diabetologia 6, 457–466 (1970)
Mehnert, H., Karg, E.: Glibenclamid, ein neues orles Antidiabeticum der Sulfonylharnstoffreihe. Dtsch. Med. Wochenschr. 94, 819–824 (1969)
Raptis, S., Pfeiffer, E. F.: Sulfonylharnstoffe der 1. und 2. Generation. Therapiewoche 21, 578–590 (1971)
Raptis, S., Rau, R. M., Schröder, K. E., Faulhaber, J. D., Pfeiffer, E. F.: Comparative study of insulin secretion following repeated administration of glucose, tolbutamide, and glibenclamide in diabetic and non-diabetic human subjects. Horm. Metab. Res. 1, Suppl. 65–72 (1969)
Schöffling, K., Petzold, R., Althoff-Zucker, C., Beyer, J., Retiene, K., Böhle, E., Kunkel, W.: Klinische Erfahrungen mit dem oralen Antidiabeticum HB 419 (Glibenclamid). Arzneim.-Forsch. (Drug Res.) 19, 1439–1445 (1969)
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Joost, H.G., Hasselblatt, A. Insulin release by tolbutamide and glibenclamide. Naunyn-Schmiedeberg's Arch. Pharmacol. 306, 185–188 (1979). https://doi.org/10.1007/BF00507101
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DOI: https://doi.org/10.1007/BF00507101