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| Pharmacology |
Glibenclamide¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
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| Protein Binding |
Glibenclamide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Extensively bound to serum proteins
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| Absorption |
Glibenclamide¿¡ ´ëÇÑ Absorption Á¤º¸ Significant absorption within 1 hour and peak plasma levels are reached within 4 hours.
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| Pharmacokinetics |
GlibenclamideÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : ¼ºÀÎ : 2-4 ½Ã°£ À̳»
- ÀÛ¿ë Áö¼Ó ½Ã°£ : 18-24½Ã°£
- ´Ü¹é°áÇÕ : 99% ÀÌ»ó
- ´ë»ç : 80% ÀÌ»óÀÌ °£¿¡¼ ÇѰ¡Áö Ȱ¼º ´ë»çü¿Í ¸î°¡Áö ºñȰ¼º ´ë»çü·Î ´ë»çµÈ´Ù.
- ¹è¼³ : 50%°¡ ¸ð¾à¹° ȤÀº ´ë»çü·Î ½ÅÀåÀ» ÅëÇØ ¹è¼³µÊ
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| Biotransformation |
Glibenclamide¿¡ ´ëÇÑ Biotransformation Á¤º¸ 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 contribute no significant hypoglycemic action in humans as they are only weakly active.
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| Toxicity |
Glibenclamide¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral rat LD50: > 20,000 mg/kg. Oral mouse LD50: 3250 mg/kg.
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| Drug Interactions |
Glibenclamide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acebutolol The beta-blocker decreases the symptoms of hypoglycemiaAtenolol The beta-blocker decreases the symptoms of hypoglycemiaBevantolol The beta-blocker decreases the symptoms of hypoglycemiaBetaxolol The beta-blocker decreases the symptoms of hypoglycemiaBisoprolol The beta-blocker decreases the symptoms of hypoglycemiaCarteolol The beta-blocker decreases the symptoms of hypoglycemiaCarvedilol The beta-blocker decreases the symptoms of hypoglycemiaEsmolol The beta-blocker decreases the symptoms of hypoglycemiaLabetalol The beta-blocker decreases the symptoms of hypoglycemiaMetoprolol The beta-blocker decreases the symptoms of hypoglycemiaNadolol The beta-blocker decreases the symptoms of hypoglycemiaOxprenolol The beta-blocker decreases the symptoms of hypoglycemiaPenbutolol The beta-blocker decreases the symptoms of hypoglycemiaPindolol The beta-blocker decreases the symptoms of hypoglycemiaPractolol The beta-blocker decreases the symptoms of hypoglycemiaPropranolol The beta-blocker decreases the symptoms of hypoglycemiaSotalol The beta-blocker decreases the symptoms of hypoglycemiaTimolol The beta-blocker decreases the symptoms of hypoglycemiaTrisalicylate-choline The salicylate increases the effect of sulfonylureaSalsalate The salicylate increases the effect of sulfonylureaSalicylate-magnesium The salicylate increases the effect of sulfonylureaSalicylate-sodium The salicylate increases the effect of sulfonylureaBismuth Subsalicylate The salicylate increases the effect of sulfonylureaAspirin The salicylate increases the effect of sulfonylureaBosentan Increased risk of hepatic toxicityDicumarol The agent increases the effect of sulfonylureaChloramphenicol The agent increases the effect of sulfonylureaClofibrate The agent increases the effect of sulfonylureaCyclosporine The sulfonylurea increases the effect of cyclosporineDiazoxide Diazoxide/sulfonylurea: antagonism of actionGlucosamine Possible hyperglycemiaIsocarboxazid The MAO inhibitor increases the effect of the hypoglycemic agentPhenelzine The MAO inhibitor increases the effect of the hypoglycemic agentPhenylbutazone Phenylbutazone increases the effect of the hypoglycemic agentRepaglinide Similar mode of action - questionable associationRifampin Rifampin decreases the effect of sulfonylureaTranylcypromine The MAO inhibitor increases the effect of the hypoglycemic agent
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Glibenclamide¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Avoid sugar and sugary food.Take 30-60 minutes before breakfast.
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| Drug Target |
[Drug Target]
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| Description |
Glibenclamide¿¡ ´ëÇÑ Description Á¤º¸ An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide. [PubChem]
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| Drug Category |
Glibenclamide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antiarrhythmic AgentsHypoglycemic AgentsSulfonylureas
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| Smiles String Canonical |
Glibenclamide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=C(C=C(Cl)C=C1)C(=O)NCCC1=CC=C(C=C1)S(=O)(=O)NC(=O)NC1CCCCC1
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| Smiles String Isomeric |
Glibenclamide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=C(C=C(Cl)C=C1)C(=O)NCCC1=CC=C(C=C1)S(=O)(=O)NC(=O)NC1CCCCC1
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| InChI Identifier |
Glibenclamide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)/f/h25-27H
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| Chemical IUPAC Name |
Glibenclamide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide
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