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药品详细

Sulfathiazole(磺胺噻唑)

化学结构式图
中文名
磺胺噻唑
英文名
Sulfathiazole
分子式
C9H9N3O2S2
化学名
4-amino-N-(1,3-thiazol-2-yl)benzene-1-sulfonamide
分子量
Average: 255.317
Monoisotopic: 255.013617927
CAS号
72-14-0
ATC分类
J01E 未知;D06B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Sulfathiazole is a short-acting sulfa drug. It used to be a common oral and topical antimicrobial until less toxic alternatives were discovered. It is still occasionally used, sometimes in combination with sulfabenzamide and sulfacetamide.

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    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication Sulfathiazole is effective against a wide range of gram positive and gram negative pathogenic microorganisms. Although no longer used in humans, it is used in cattle.
    Pharmacodynamics Not Available
    Mechanism of action Not Available
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Metabolism of sulfonamide drugs in animals includes conjugation at the N4-position (acetyl, sulfate, glucuronic acid, and glucose), conjugation at the N1-position (sulfate and glucuronic acid), removal of the p-amino group (formation of the desamino metabolite), ring hydroxylation, and conjugation of the ring hydroxylation products. Dietary nitrite enhances the production of the desamino metabolite of sulfathiazole. The intermediate leading to the desamino metabolite of sulfamethazine is weakly mutagenic in the Ames test (Nelson et al., 1987; Paulson et al., 1987).
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Acute oral toxicity (LD50): 4500 mg/kg [Mouse].
    Affected organisms Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 189 °C PhysProp
    water solubility 373 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
    logP 0.05 HANSCH,C ET AL. (1995)
    pKa 7.2 BUDAVARI,S ET AL. (1996)
    Predicted Properties
    Property Value Source
    water solubility 9.21e-01 g/l ALOGPS
    logP 0.88 ALOGPS
    logP 0.98 ChemAxon
    logS -2.4 ALOGPS
    pKa (strongest acidic) 6.93 ChemAxon
    pKa (strongest basic) 2.04 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 85.08 ChemAxon
    rotatable bond count 2 ChemAxon
    refractivity 62.27 ChemAxon
    polarizability 23.96 ChemAxon
    药物相互作用
    Drug Interaction
    Methenamine mandelate Possible crystallization of urates with this combination
    Methotrexate The sulfamide increases the toxicity of methotrexate
    食物相互作用
    Not Available

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