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Glibenclamide, also known as glyburide, is an antidiabetic drug in a class of medications known as sulfonylureas, closely related to sulfonamide antibiotics. It was developed in 1966 in a cooperative study between Boehringer Mannheim (now part of Roche ) and Hoechst (now part of Sanofi-Aventis ).
1 Medical uses
2 Side effects and contraindications
3 Mechanism of action
5 Trade names
6 See also
It is used in the treatment of type 2 diabetes.
It is not as good as either metformin or insulin in those who have gestational diabetes.
Side effects and contraindications
This medication is a major cause of medication-induced hypoglycemia. The risk is greater than with other sulfonylureas. Cholestatic jaundice is noted.
Glibenclamide may be not recommended in those with G6PD deficiency, as it may cause acute hemolysis.
Mechanism of action
The medication works by binding to and inhibiting the ATP-sensitive potassium channels (K ATP ) inhibitory regulatory subunit sulfonylurea receptor 1 (SUR1) in pancreatic beta cells. This inhibition causes cell membrane depolarization, opening voltage-dependent calcium channels. This results in an increase in intracellular calcium in the pancreatic beta cell and subsequent stimulation of insulin release.
After a cerebral ischemic insult, the blood–brain barrier is broken and glibenclamide can reach the central nervous system. Glibenclamide has been shown to bind more efficiently to the ischemic hemisphere.
Glibenclamide improves outcome in animal stroke models by preventing brain swelling
Glibenclamide is available as a generic, is manufactured by many pharmaceutical companies and is sold in doses of 1.25, 2.5 and 5 mg under many brand names including Gliben-J, Daonil, Diabeta, Euglucon, Gilemal, Glidanil, Glybovin, Glynase, Maninil, Micronase and Semi-Daonil. It is also available in a fixed-dose combination drug with metformin that is sold under various trade names, e.g. Bagomet Plus, Benimet, Glibomet, Gluconorm, Glucored, Glucovance, Metglib and many others.
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