药品详细
Sulfoxone(地砜)
化学结构式图
中文名
地砜
英文名
Sulfoxone
分子式
C14H16N2O6S3
化学名
{[4-({4-[(sulfinomethyl)amino]benzene}sulfonyl)phenyl]amino}methanesulfinic acid
分子量
Average: 404.482
Monoisotopic: 404.017048324
Monoisotopic: 404.017048324
CAS号
144-75-2
ATC分类
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Sulfoxone is a water-soluble sulfone used as an antileprosy drug. It has been used with limited success in the treatment of dermatitis herpetiformis.
生产厂家
- Abbott laboratories pharmaceutical products div
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For the treatment of leprosy and dermatitis herpetiformis |
| Pharmacodynamics | Sulfoxone is a sulfonamide antibiotic. The sulfonamides are synthetic bacteriostatic antibiotics with a wide spectrum against most gram-positive and many gram-negative organisms. However, many strains of an individual species may be resistant. Sulfonamides inhibit multiplication of bacteria by acting as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism cycle. Bacterial sensitivity is the same for the various sulfonamides, and resistance to one sulfonamide indicates resistance to all. Most sulfonamides are readily absorbed orally. However, parenteral administration is difficult, since the soluble sulfonamide salts are highly alkaline and irritating to the tissues. The sulfonamides are widely distributed throughout all tissues. High levels are achieved in pleural, peritoneal, synovial, and ocular fluids. Although these drugs are no longer used to treat meningitis, CSF levels are high in meningeal infections. Their antibacterial action is inhibited by pus. |
| Mechanism of action | Sulfoxone is a competitive inhibitor of bacterial enzyme dihydropteroate synthetase. The normal substrate for the enzyme, para-aminobenzoic acid (PABA) cannot bind as usual. The inhibited reaction is necessary in these organisms for the synthesis of folic acid. |
| Absorption | Rapidly absorbed. |
| Volume of distribution | Not Available |
| Protein binding | 69% |
| Metabolism |
Hepatic.
|
| Route of elimination | Not Available |
| Half life | 3-8 hours |
| Clearance | Not Available |
| Toxicity | Oral, rat LD50: 7000 mg/kg |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
食物相互作用
Not Available
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