Clinical Pharmacology of Sulfonylureas

  • L. Groop
  • G. Neugebauer
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 119)


In vitro studies using the perfused rat pancreas and in vivo studies using the hyperglycemic clamp have demonstrated that sulfonylureas stimulate insulin secretion in a biphasic fashion (Loubatieres 1957; Malaisse et al. 1972; Grodsky et al. 1977; Groop et al. 1987b). The insulinotropic effect of sulfonylureas is augmented by glucose, and sulfonylureas have therefore been proposed to increase B-cell sensitivity to glucose and non-glucose stimuli rather than to increase the synthesis of insulin by the pancreatic B cell (Basabe et al. 1976; Pfeifer et al. 1980; Dunbar and Foá 1974; Grodsky et al. 1977). Sulfonylureas close ATP-dependent potassium channels, which, in turn, results in depolarization of the B cell and influx of calcium (Sturgess et al. 1985; Boyd AE III 1988). The final result is stimulation of insulin secretion. Sulfonylureas bind to receptor-like structures on the B cell, which may be closely linked to or be part of the potassium channels (Schmid-Antomarchi et al. 1987; Gaines et al. 1988; Siconolfi-Baez et al. 1990). The binding capacity of different sulfonylureas reflects their ability to stimulate insulin secretion.


Insulin Secretion Clinical Pharmacology NIDDM Patient Magnesium Hydroxide Sulfonylurea Therapy 
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© Springer-Verlag Berlin Heidelberg 1996

Authors and Affiliations

  • L. Groop
  • G. Neugebauer

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