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药品详细

Butoconazole(布康唑)

化学结构式图
中文名
布康唑
英文名
Butoconazole
分子式
C19H17Cl3N2S
化学名
1-[4-(4-chlorophenyl)-2-[(2,6-dichlorophenyl)sulfanyl]butyl]-1H-imidazole
分子量
Average: 411.776
Monoisotopic: 410.017802365
CAS号
64872-77-1
ATC分类
G01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Butoconazole is an imidazole antifungal used in gynecology.

生产厂家
  • Bayer healthcare llc
  • Kv pharmaceutical co
  • Roche palo alto llc
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
  • Benzene and Derivatives
  • Halobenzenes
Substructures
  • Ethers
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Imidazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Cyanamides
适应症
药理
Indication For the local treatment of vulvovaginal candidiasis (infections caused by Candida)
Pharmacodynamics Butoconazole is an imidazole derivative that has fungicidal activity in vitro against Candida spp. and has been demonstrated to be clinically effective against vaginal infections due to Candida albicans. Candida albicans has been identified as the predominant species responsible for vulvovaginal candidasis.
Mechanism of action The exact mechanism of the antifungal action of butoconazole is unknown, however, it is presumed to function as other imidazole derivatives via inhibition of steroid synthesis. Imidazoles generally inhibit the conversion of lanosterol to ergosterol via the inhibition of the enzyme cytochrome P450 14α-demethylase, resulting in a change in fungal cell membrane lipid composition. This structural change alters cell permeability and, ultimately, results in the osmotic disruption or growth inhibition of the fungal cell.
Absorption Following vaginal administration of butoconazole nitrate vaginal cream, 2% to 3 women, 1.7% (range 1.3-2.2%) of the dose was absorbed on average.
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 Oral, rat: LD50 = >1720 mg/kg.
Affected organisms
  • Fungi, yeast and protozoans
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point ~159°C with decomposition (nitrate salt) Not Available
water solubility Nitrate salt: 0.26 mg/ml (practically insoluble) Not Available
logP 6.7 Not Available
Predicted Properties
Property Value Source
water solubility 8.18e-04 g/l ALOGPS
logP 6.7 ALOGPS
logP 6.55 ChemAxon
logS -5.7 ALOGPS
pKa (strongest basic) 6.78 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 1 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 17.82 ChemAxon
rotatable bond count 7 ChemAxon
refractivity 108.99 ChemAxon
polarizability 41.01 ChemAxon
药物相互作用
食物相互作用
Not Available

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