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药品详细

Gliclazide (格列齐特 )

化学结构式图
中文名
格列齐特
英文名
Gliclazide
分子式
Not Available
化学名
1-[(4-methylbenzene)sulfonyl]-3-{octahydrocyclopenta[c]pyrrol-2-yl}urea
分子量
Average: 323.411
Monoisotopic: 323.130362243
CAS号
21187-98-4
ATC分类
A10B Oral Blood Glucose Lowering Drugs, Excl. Insulins
药物类型
small molecule
阶段
商品名
Diamicron;Glimicron;Nordialex;
同义名
1-(3-Azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea;1-(Hexahydrocyclopenta(c)pyrrol-2(1H)-yl)-3-(p-tolylsulfonyl)urea;Gliclazida [INN-Spanish];Gliclazidum [INN-Latin];N-(4-Methylbenzenesulfonyl)-N'-(3-azabicyclo(3.3.0)oct-3-yl)urea;
基本介绍

An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    Form Route Strength
    Tablet Oral
    Tablet, extended release Oral
    规格
    Unit description Cost Unit
    Diamicron 80 mg Tablet 0.42 USD tablet
    Apo-Gliclazide 80 mg Tablet 0.23 USD tablet
    Gliclazide 80 mg Tablet 0.23 USD tablet
    Mylan-Gliclazide 80 mg Tablet 0.23 USD tablet
    Novo-Gliclazide 80 mg Tablet 0.23 USD tablet
    Pms-Gliclazide 80 mg Tablet 0.23 USD tablet
    Diamicron Mr 30 mg Sustained-Release Tablet 0.16 USD tablet
    Apo-Gliclazide Mr 30 mg Sustained-Release Tablet 0.15 USD tablet
    化合物类型
    Type small molecule
    Classes
    • Sulfonylureas
    Substructures
    • Sulfonylureas
    • Sulfonyls
    • Pyrrolidines
    • Benzene and Derivatives
    • Benzenesulfonamides
    • Heterocyclic compounds
    • Aromatic compounds
    • Sulfonamides
    • Semicarbazides
    • Hydrazine Derivatives
    适应症
    药理
    Indication For the treatment of diabetes mellitus
    Pharmacodynamics 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.
    Mechanism of action 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.
    Absorption Rapidly and well absorbed but may have wide inter- and intra-individual variability.
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism

    Hepatic

    Enzyme Metabolite Reaction Km Vmax
    Cytochrome P450 2C9 7-Hydroxygliclazide 7-hydroxylation
    Cytochrome P450 2C9 6-Hydroxygliclazide 7-hydroxylation
    Cytochrome P450 2C9 Methylhydroxygliclazide
    Cytochrome P450 2C19 Methylhydroxygliclazide
    Route of elimination Not Available
    Half life 11 hours (Campbell DB et al.,Diabetes Res Clin Pract.;14:S21-36)
    Clearance Not Available
    Toxicity LD50=3000 mg/kg (orally in mice)
    Affected organisms
    • Humans and other mammals
    Pathways
    Pathway Name SMPDB ID
    Smp00461 Gliclazide Pathway SMP00461
    理化性质
    Properties
    State solid
    Melting point 181 oC
    Experimental Properties
    Property Value Source
    logP 2.6 PhysProp
    Predicted Properties
    Property Value Source
    water solubility 1.90e-01 g/l ALOGPS
    logP 1.52 ALOGPS
    logP 1.73 ChemAxon Molconvert
    logS -3.23 ALOGPS
    pKa 14.13 ChemAxon Molconvert
    hydrogen acceptor count 4 ChemAxon Molconvert
    hydrogen donor count 2 ChemAxon Molconvert
    polar surface area 78.51 ChemAxon Molconvert
    rotatable bond count 2 ChemAxon Molconvert
    refractivity 83.88 ChemAxon Molconvert
    polarizability 34.22 ChemAxon Molconvert
    药物相互作用
    Drug Interaction
    Acebutolol Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
    Acetylsalicylic acid Acetylsalicylic acid increases the effect of the sulfonylurea, gliclazide.
    Atenolol The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
    Betaxolol The beta-blocker, betaxolol, may decrease symptoms of hypoglycemia.
    Bevantolol The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
    Bismuth Subsalicylate The salicylate, bismuth subsalicylate, increases the effect of the sulfonylurea, gliclazide.
    Bisoprolol The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
    Carteolol The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.
    Carvedilol The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia.
    Chloramphenicol Chloramphenicol may increase the effect of sulfonylurea, gliclazide.
    Clofibrate Clofibrate may increase the effect of sulfonylurea, gliclazide.
    Dicumarol Dicumarol may increase the effect of sulfonylurea, gliclazide.
    Esmolol The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
    Glucosamine Possible hyperglycemia
    Labetalol The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
    Magnesium salicylate The salicylate, magnesium salicylate, increases the effect of the sulfonylurea, gliclazide.
    Metoprolol The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia.
    Nadolol The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
    Oxprenolol The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
    Penbutolol The beta-blocker, penbutolol, may decrease symptoms of hypoglycemia.
    Phenylbutazone Phenylbutazone increases the effect of the hypoglycemic agent
    Pindolol The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
    Practolol The beta-blocker, practolol, may decrease symptoms of hypoglycemia.
    Propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia.
    Rifampin Rifampin may decrease the effect of sulfonylurea, gliclazide.
    Salicylate-sodium The salicylate, salicylate-sodium, increases the effect of the sulfonylurea, gliclazide.
    Salsalate The salicylate, salsalate, increases the effect of the sulfonylurea, gliclazide.
    Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of gliclazide. Monitor for changes in fasting and postprandial blood sugars.
    Sotalol The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.
    Timolol The beta-blocker, timolol, may decrease symptoms of hypoglycemia.
    Trisalicylate-choline The salicylate, trisalicylate-choline, increases the effect of the sulfonylurea, gliclazide.
    食物相互作用
    • Avoid alcohol.
    • Take without regard to meals.

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