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Glibenclamide

Name: Glibenclamide
Description: An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide. (PubChem) Pharmacology: Glibenclamide (INN), also known as glyburide (USAN), a second-generation sulfonylurea antidiabetic agent, appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonyl-urea hypoglycemic drugs. The combination of glibenclamide and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different but complementary mechanisms. In addition to its blood glucose lowering actions, glibenclamide produces a mild diuresis by enhancement of renal free water clearance. Glibenclamide is twice as potent as the related second-generation agent glipizide. Mechanism of action: Sulfonylureas such as glibenclamide likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin. Drug type: Approved. Small Molecule. Drug category: Antiarrhythmic Agents. Hypoglycemic Agents. Sulfonylureas
Synonym(s): Apo-Glibenclamide, Glibenclamida (INN-Spanish), Glibenclamidum (INN-Latin), Glyburide, Abbenclamide, Adiab, Azuglucon, Bastiverit, Benclamin, Betanase, Betanese 5, Calabren, Cytagon, Daonil, Debtan, Dia-basan, Diabeta, Diabiphage, Dibelet, Duraglucon, Euclamin, Euglucan, Euglucon, Euglucon 5, Euglykon, GBN 5, Gen-Glybe, Gewaglucon, Gilemal, Glamide, Glibadone, Gliban, Gliben, Gliben-Puren N, Glibenbeta, Glibenclamid AL, Glibenclamid Basics, Glibenclamid Fabra, Glibenclamid Genericon, Glibenclamid Heumann, Glibenclamid Riker M, Glibenclamid-Cophar, Glibenclamid-Ratiopharm, Glibenil, Glibens, Glibesyn, Glibet, Glibetic, Glibil, Gliboral, Glicem, Glidiabet, Glimel, Glimide, Glimidstata, Glisulin, Glitisol, Glubate, Gluben, Gluco-Tablimen, Glucobene, Glucohexal, Glucolon, Glucomid, Glucoremed, Glucoven, Glyben, Glybenclamide, Glybenzcyclamide, Glycolande, Glycomin, Glynase, Hexaglucon, Humedia, Lederglib, Libanil, Lisaglucon, Malix, Maninil, Med-Glionil, Melix, Micronase, Miglucan, Nadib, Neogluconin, Norglicem 5, Normoglucon, Novo-Glyburide, Orabetic, Pira, Praeciglucon, PresTab, Prodiabet, Renabetic, Semi-Daonil, Sugril, Suraben, Tiabet, Yuglucon
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB01016
*Id: DB01016
Related to: ATP-binding cassette sub-family A member 1, ATP-binding cassette transporter sub-family C member 8, ATP-binding cassette transporter sub-family C member 9, ATP-sensitive inward rectifier potassium channel 1, Bile salt export pump, ATP-sensitive inward rectifier potassium channel 11, Multidrug resistance-associated protein 1, Canalicular multispecific organic anion transporter 2, Cystic fibrosis transmembrane conductance regulator, G protein-activated inward rectifier potassium channel 4
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Facts about GlibenclamideRDF feed
Commenttaken from DrugBank
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB01016  +
DefinitionAn antidiabetic sulfonylurea derivative wi An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide. (PubChem) Pharmacology: Glibenclamide (INN), also known as glyburide (USAN), a second-generation sulfonylurea antidiabetic agent, appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonyl-urea hypoglycemic drugs. The combination of glibenclamide and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different but complementary mechanisms. In addition to its blood glucose lowering actions, glibenclamide produces a mild diuresis by enhancement of renal free water clearance. Glibenclamide is twice as potent as the related second-generation agent glipizide. Mechanism of action: Sulfonylureas such as glibenclamide likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin. Drug type: Approved. Small Molecule. Drug category: Antiarrhythmic Agents. Hypoglycemic Agents. Sulfonylureas Agents. Hypoglycemic Agents. Sulfonylureas
Has roleDrug  +
IdDB01016  +
LabelGlibenclamide  +
ModifiedDate14 April 2014  +
RelatedToATP-binding cassette sub-family A member 1  +, ATP-binding cassette transporter sub-family C member 8  +, ATP-binding cassette transporter sub-family C member 9  +, ATP-sensitive inward rectifier potassium channel 1  +, Bile salt export pump  +, ATP-sensitive inward rectifier potassium channel 11  +, Multidrug resistance-associated protein 1  +, Canalicular multispecific organic anion transporter 2  +, Cystic fibrosis transmembrane conductance regulator  +, and G protein-activated inward rectifier potassium channel 4  +
SuperCategoryMolecular entity  +
SynonymApo-Glibenclamide  +, Glibenclamida (INN-Spanish)  +, Glibenclamidum (INN-Latin)  +, Glyburide  +, Abbenclamide  +, Adiab  +, Azuglucon  +, Bastiverit  +, Benclamin  +, Betanase  +, Betanese 5  +, Calabren  +, Cytagon  +, Daonil  +, Debtan  +, Dia-basan  +, Diabeta  +, Diabiphage  +, Dibelet  +, Duraglucon  +, Euclamin  +, Euglucan  +, Euglucon  +, Euglucon 5  +, Euglykon  +, GBN 5  +, Gen-Glybe  +, Gewaglucon  +, Gilemal  +, Glamide  +, Glibadone  +, Gliban  +, Gliben  +, Gliben-Puren N  +, Glibenbeta  +, Glibenclamid AL  +, Glibenclamid Basics  +, Glibenclamid Fabra  +, Glibenclamid Genericon  +, Glibenclamid Heumann  +, Glibenclamid Riker M  +, Glibenclamid-Cophar  +, Glibenclamid-Ratiopharm  +, Glibenil  +, Glibens  +, Glibesyn  +, Glibet  +, Glibetic  +, Glibil  +, Gliboral  +, Glicem  +, Glidiabet  +, Glimel  +, Glimide  +, Glimidstata  +, Glisulin  +, Glitisol  +, Glubate  +, Gluben  +, Gluco-Tablimen  +, Glucobene  +, Glucohexal  +, Glucolon  +, Glucomid  +, Glucoremed  +, Glucoven  +, Glyben  +, Glybenclamide  +, Glybenzcyclamide  +, Glycolande  +, Glycomin  +, Glynase  +, Hexaglucon  +, Humedia  +, Lederglib  +, Libanil  +, Lisaglucon  +, Malix  +, Maninil  +, Med-Glionil  +, Melix  +, Micronase  +, Miglucan  +, Nadib  +, Neogluconin  +, Norglicem 5  +, Normoglucon  +, Novo-Glyburide  +, Orabetic  +, Pira  +, Praeciglucon  +, PresTab  +, Prodiabet  +, Renabetic  +, Semi-Daonil  +, Sugril  +, Suraben  +, Tiabet  +, and Yuglucon  +