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药品详细

Niclosamide(氯硝柳胺)

化学结构式图
中文名
氯硝柳胺
英文名
Niclosamide
分子式
C13H8Cl2N2O4
化学名
5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide
分子量
Average: 327.12
Monoisotopic: 325.986112168
CAS号
50-65-7
ATC分类
P02D 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Niclosamide is used for the treatment of most tapeworm infections. Helminths (worms) are multicellular organisms that infect very large numbers of humans and cause a broad range of diseases. Over 1 billion people are infected with intestinal nematodes, and many millions are infected with filarial nematodes, flukes, and tapeworms. They are an even greater problem in domestic animals.

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    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Rosenthal Philip J, “Chapter 53. Clinical Pharmacology of the Antihelminthic Drugs” (Chapter). Katzung BG: Basic & Clinical Pharmacology, 11e: http://www.accessmedicine.com/content.aspx?aID=4516635.
    2. 2010. Detailed Drug Information for the Consumer™. Greenwood Village, CO. Thomson Reuters. ISBN-10: 1-56363-575-5. ISSN: 0740-4174. STAT!Ref Online Electronic Medical Library.
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication For the treatment of tapeworm and intestinal fluke infections: Taenia saginata (Beef Tapeworm), Taenia solium (Pork Tapeworm), Diphyllobothrium latum (Fish Tapeworm), Fasciolopsis buski (large intestinal fluke). Niclosamide is also used as a molluscicide in the control of schistosomiasis.
    Pharmacodynamics Niclosamide is an antihelminth used against tapeworm infections. It may act by the uncoupling of the electron transport chain to ATP synthase. The disturbance of this crucial metabolic pathway prevents creation of adenosine tri-phosphate (ATP), an essential molecule that supplies energy for metabolism.
    Mechanism of action Niclosamide works by killing tapeworms on contact. Adult worms (but not ova) are rapidly killed, presumably due to uncoupling of oxidative phosphorylation or stimulation of ATPase activity. The killed worms are then passed in the stool or sometimes destroyed in the intestine. Niclosamide may work as a molluscicide by binding to and damaging DNA.
    Absorption Niclosamide appears to be minimally absorbed from the gastrointestinal tract—neither the drug nor its metabolites have been recovered from the blood or urine.
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Infrequent, mild, and transitory adverse events include nausea, vomiting, diarrhea, and abdominal discomfort.
    Affected organisms
    • Helminthic Microorganisms
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 230 °C PhysProp
    water solubility 1.6 mg/L (at 20 °C) TOMLIN,C (1997)
    Predicted Properties
    Property Value Source
    water solubility 7.99e-03 g/l ALOGPS
    logP 4.49 ALOGPS
    logP 3.91 ChemAxon
    logS -4.6 ALOGPS
    pKa (strongest acidic) 6.89 ChemAxon
    pKa (strongest basic) -4.4 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 95.15 ChemAxon
    rotatable bond count 3 ChemAxon
    refractivity 80.51 ChemAxon
    polarizability 28.47 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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