Sulphonylureas

Sulphonylureas

Sulphonylurea derivatives enhance the secretion of insulin from pancreatic tissue (β-cells). These drugs can block ATP-dependent potassium channels in the cell membrane of β-cells. The block of the potassium efflux causes a depolarisation of the membrane potential, resulting in an influx of calcium ions. The increase of calcium in the cytoplasm enhances the secretion of insulin. The short-acting tolbutamide,

gliclazide, and glimepiride are the most prominent sulphonylureas. The long-acting glibenclamide is not used very often, because it increases the risk of hypoglycemia.

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The policy of treating obese patients with type 2 diabetes mellitus is: first dietary control and losing weight. If this does not result in satisfactory glucose levels the use of biguanides is recommended.