药品详细
Sertaconazole(舍他康唑)
化学结构式图
中文名
舍他康唑
英文名
Sertaconazole
分子式
C20H15Cl3N2OS
化学名
1-{2-[(7-chloro-1-benzothiophen-3-yl)methoxy]-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole
分子量
Average: 437.77
Monoisotopic: 435.997066923
Monoisotopic: 435.997066923
CAS号
99592-32-2
ATC分类
D01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Sertaconazole nitrate is an antifungal medication of the imidazole class. It is available as a cream to treat skin infections such as athlete’s foot. [Wikipedia]
生产厂家
- Ortho dermatologics
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 |
|
| Substructures |
|
适应症
药理
| Indication | For the topical treatment of interdigital tinea pedis in immunocompetent patients 12 years of age and older, caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum. |
| Pharmacodynamics | Sertaconazole is an imidazole/triazole type antifungal agent. Sertaconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation via the inhibition of the enzyme cytochrome P450 14α-demethylase. This enzyme converts lanosterol to ergosterol, and is required in fungal cell wall synthesis. The subsequent loss of normal sterols correlates with the accumulation of 14 α-methyl sterols in fungi and may be partly responsible for the fungistatic activity of fluconazole. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. Sertaconazole exhibits in vitro activity against Cryptococcus neoformans and Candida spp. Fungistatic activity has also been demonstrated in normal and immunocompromised animal models for systemic and intracranial fungal infections due to Cryptococcus neoformans and for systemic infections due to Candida albicans. |
| Mechanism of action | Sertaconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Sertaconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis. |
| Absorption | Bioavailability is negligible. |
| Volume of distribution | Not Available |
| Protein binding | >99% to plasma |
| Metabolism |
Not Available
|
| Route of elimination | Not Available |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | ||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
|||||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
|||||||||||||||||||||||||||||||||||||||
药物相互作用
食物相互作用
Not Available
收藏