Glibenclamide

Glibenclamide is used to lower the blood sugar level in patients with type 2 diabetes mellitus, which is not controlled by diet and exercise alone. It is not as good as either metformin or insulin in those who have gestational diabetes. == Side effects ==

Frequently reported side effects include: nausea, heartburn, weight gain, and bloating. The medication is also a major cause of medication-induced hypoglycemia. The risk is greater than with other sulfonylureas. == Contraindications ==

Glibenclamide may be not recommended in those with G6PD deficiency, as it may cause acute hemolysis. Pregnancy and breastfeeding It is generally not recommended during pregnancy but can be used during breastfeeding. == Mechanism of action ==

The medication, a sulfonylurea, works by binding to and inhibiting the ATP-sensitive potassium channels (KATP) 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 stroke, 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. Moreover, under ischemic conditions SUR1, the regulatory subunit of the KATP- and the NCCa-ATP-channels, is expressed in neurons, astrocytes, oligodendrocytes, endothelial cells and by reactive microglia. ==History==

It was developed in 1966 in a cooperative study between Boehringer Mannheim (now part of Roche) and Hoechst (now part of Sanofi-Aventis). == Society and culture ==

Brand names Glibenclamide is available as a generic medication, is manufactured by many pharmaceutical companies and is sold 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. == References ==