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|
| Mechanism of Action |
Gliclazide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Gliclazide binds to the beta cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the beta cells. This opens voltage-dependent calcium channels in the beta cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.
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| Pharmacology |
Gliclazide¿¡ ´ëÇÑ Pharmacology Á¤º¸ Gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates beta cells of the islet of Langerhans in the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall it potentiates insulin release and improves insulin dynamics.
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| Protein Binding |
Gliclazide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Gliclazide¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 11 hours (Campbell DB et al.,Diabetes Res Clin Pract.;14:S21-36)
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| Absorption |
Gliclazide¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly and well absorbed but may have wide inter- and intra-individual variability.
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| Pharmacokinetics |
GliclazideÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : ´ëºÎºÐÀÌ À§Àå°ü¿¡¼ Èí¼öµÈ´Ù.
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : ¼ºÀÎ : 4 ½Ã°£
- ºÐÆ÷ : ºÐÆ÷¿ëÀû : 25 L
- ´Ü¹é°áÇÕ : 95% (85-97%)
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- ¹Ý°¨±â : 10½Ã°£ (6-14 ½Ã°£)
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| Biotransformation |
Gliclazide¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
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| Toxicity |
Gliclazide¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=3000 mg/kg (orally in mice)
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| Drug Interactions |
Gliclazide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acebutolol The beta-blocker decreases the symptoms of hypoglycemiaAtenolol The beta-blocker decreases the symptoms of hypoglycemiaBetaxolol The beta-blocker decreases the symptoms of hypoglycemiaBevantolol 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 hypoglycemiaAspirin The salicylate increases the effect of sulfonylureaBismuth Subsalicylate The salicylate increases the effect of sulfonylureaSalicylate-magnesium The salicylate increases the effect of sulfonylureaSalicylate-sodium The salicylate increases the effect of sulfonylureaSalsalate The salicylate increases the effect of sulfonylureaTrisalicylate-choline The salicylate increases the effect of sulfonylureaRepaglinide Similar mode of action - questionable associationRifampin Rifampin decreases the effect of sulfonylureaTranylcypromine The MAO inhibitor increases the effect of the hypoglycemic agentPhenelzine The MAO inhibitor increases the effect of the hypoglycemic agentIsocarboxazid The MAO inhibitor increases the effect of the hypoglycemic agentPhenylbutazone Phenylbutazone increases the effect of the hypoglycemic agentGlucosamine Possible hyperglycemiaDicumarol The agent increases the effect of sulfonylureaChloramphenicol The agent increases the effect of sulfonylureaClofibrate The agent increases the effect of sulfonylurea
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Gliclazide¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid alcohol.
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| Drug Target |
[Drug Target]
|
| Description |
Gliclazide¿¡ ´ëÇÑ Description Á¤º¸ An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion. [PubChem]
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| Dosage Form |
Gliclazide¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet OralTablet, extended release Oral
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| Drug Category |
Gliclazide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Hypoglycemic AgentsSulfonylureas
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| Smiles String Canonical |
Gliclazide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN1CC2CCCC2C1
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| Smiles String Isomeric |
Gliclazide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN1C[C@@H]2CCC[C@@H]2C1
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| InChI Identifier |
Gliclazide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)/f/h16-17H
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| Chemical IUPAC Name |
Gliclazide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea
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