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QuickView for Glyburide (compound)

Name: Glyburide
PubChem Compound ID: 10625062
Description: An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
Molecular formula: C23H28ClN3O5S
Molecular weight: 496.012 g/mol
Name: Glyburide
Name (isomeric): DB01016
Drug Type: small molecule
Description: An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
Apo-Glibenclamide; Glibenclamidum [INN-Latin]; Glibenclamida [INN-Spanish]; Glibenclamide
Brand: Benclamin, Glibenclamid Riker M., Dia-basan, Tiabet, Orabetic, Glimel, Glynase, Gen-Glybe, Gewaglucon, Glibesyn, Libanil, Glibil, Glibet, Glucomid, Hexaglucon, Duraglucon, Gliben, Glitisol, Glibadone, Glisulin, Glidiabet, Sugril, Nadib, Glybenclamide, Glyben, Adiab, Humedia, Glimide, Glybenzcyclamide, Micronase, Glibenclamid Fabra, Gliban, Glucoven, Glibenclamid-Ratiopharm, GBN 5, Malix, Gliben-Puren N, Euglucon 5, Gliboral, Glimidstata, Glycolande, Gluben, Glicem, Debtan, Glucobene, Glubate, Euglykon, Betanase, Calabren, Novo-Glyburide, Glucolon, Euglucon, Cytagon, Yuglucon, Glibenclamid-Cophar, Glibens, Euglucan, Glibetic, Norglicem 5, Betanese 5, Glibenclamid Basics, Glibenbeta, Gilemal, Glycomin, PresTab, Lisaglucon, Glucoremed, Gluco-Tablimen, Miglucan, Glibenclamid Genericon, Semi-Daonil, Neogluconin, Diabeta, Glibenclamid AL, Dibelet, Bastiverit, Praeciglucon, Daonil, Glamide, Melix, Euclamin, Suraben, Lederglib, Glibenclamid Heumann, Glibenil, Glucohexal, Pira, Maninil, Azuglucon, Med-Glionil, Diabiphage, Prodiabet, Renabetic, Normoglucon, Abbenclamide
Brand name mixture: Glucovance(Metformin + Glibenclamide)
Category: Hypoglycemic Agents, Antiarrhythmic Agents, Sulfonylureas
CAS number: 10238-21-8
Indication: Indicated as an adjunct to diet to lower the blood glucose in patients with NIDDM whose hyperglycemia cannot be satisfactorily controlled by diet alone.
Glyburide, a second-generation sulfonylurea antidiabetic agent, lowers 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...
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Mechanism of Action:
Sulfonylureas such as glyburide bind to ATP-sensitive potassium channels 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...
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Absorption: Significant absorption within 1 hour and peak plasma levels are reached in 2 to 4 hours. Onset of action occurs within one hour.
Protein binding: Unchanged drug is ~99% bound to serum proteins; 4-trans-hydroxyglyburide is greater than 97% bound to serum proteins. Protein binding is primarily nonionic making glyburide and is less likely to displace or be displaced by drugs that bind via an ionic mechanism.
Biotransformation: Primarily hepatic (mainly cytochrome P450 3A4). The major metabolite is the 4-trans-hydroxy derivative. A second metabolite, the 3-cis-hydroxy derivative, also occurs. These metabolites do not contribute clinically significant hypoglycemic action in humans as they are only weakly active; however, retention of 4-trans-hydroxyglyburide may prolong the hypoglycemic effect of the agent in those with severe renal impairment.
Route of elimination: Glyburide is excreted as metabolites in the bile and urine, approximately 50% by each route. This dual excretory pathway is qualitatively different from that of other sulfonylureas, which are excreted primarily in the urine.
Half Life: 1.4-1.8 hours (unchanged drug only); 10 hours (metabolites included). Duration of effect is 12-24 hours.
Clearance: 78 ml/hr/kg in healthy adults. Clearance may be substantially decreased in those with severe renal impairment.
Toxicity: Oral rat LD50: > 20,000 mg/kg. Oral mouse LD50: 3250 mg/kg.
Affected organisms: Humans and other mammals
Food interaction:
Avoid alcohol.
Take 30-60 minutes before breakfast.
Drug interaction:
DicumarolDicumarol may increase the effect of sulfonylurea, glibenclamide.
Acetylsalicylic acidAcetylsalicylic acid increases the effect of the sulfonylurea, glibenclamide.
Trisalicylate-cholineThe salicylate, trisalicylate-choline, increases the effect of the sulfonylurea, glibenclamide.
OxprenololThe beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Bismuth SubsalicylateThe salicylate, bismuth subsalicylate, increases the effect of the sulfonylurea, glibenclamide.
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