Glibenclamide is a second generation sulfonylurea hypoglycemic drug which acts by increasing the sensitivity of peripheral tissues to insulin and stimulating release of insulin from beta cells in the pancreas.
The hypoglycemic effect of the drug persists due to the inhibition of hepatic glucose production and increased sensitivity to any available insulin.
The duration of action of glibenclamide is 10 to 24 hours after a single morning dose in patients with diabetes.
Pharmacokinetics: Approximately 1.5 to 2 hours after oral intake, 90% of glibenclamide is absorbed from an empty stomach. Absorption of the drug is said to be decreased by food. Food with fibers may decrease absorption by as much as 50%.
Glibenclamide, as a weak-acid anion, is 97% bound to plasma albumin. Hence, weak acid drugs may displace glibenclamide.
The volume of distribution of glibenclamide is 0.16 L/kg.
The drug is metabolized mainly in the liver with very low hypoglycemic activity. The half-life of glibenclamide is 1.5 to 5 hours.
                                
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