药品详细
Terconazole(特康唑)
化学结构式图
中文名
特康唑
英文名
Terconazole
分子式
C26H31Cl2N5O3
化学名
1-(4-{[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)-4-(propan-2-yl)piperazine
分子量
Average: 532.462
Monoisotopic: 531.180395297
Monoisotopic: 531.180395297
CAS号
67915-31-5
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
Terconazole is an anti-fungal medication, primarily used to treat vaginal fungal infections. [Wikipedia]
生产厂家
- Altana inc
- Nycomed us inc
- Ortho mcneil janssen pharmaceutical inc
- Ortho mcneil janssen pharmaceuticals inc
- Perrigo new york inc
- Taro pharmaceuticals usa inc
封装厂家
- A-S Medication Solutions LLC
- Dept Health Central Pharmacy
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- E. Fougera and Co.
- Lake Erie Medical and Surgical Supply
- Nycomed Inc.
- Ortho Mcneil Janssen Pharmaceutical Inc.
- Ortho-McNeil-Janssen Pharmaceuticals Inc.
- Perrigo Co.
- Pharmaderm
- Pharmedix
- Physicians Total Care Inc.
- Rebel Distributors Corp.
- Stat Rx Usa
- Taro Pharmaceuticals USA
- Watson Pharmaceuticals
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 candidiasis (a yeast-like fungal infection) of the vulva and vagina. |
| Pharmacodynamics | Terconazole is a triazole antifungal agent available for intravaginal use. It is structurally related to imidazole-derivative antifungal agents, although terconazole and other triazoles have 3 nitrogens in the azole ring. By inhibiting the 14-alpha-demethylase (lanosterol 14-alpha-demethylase), Terconazole inhibits ergosterol synthesis. Depletion of ergosterol in fungal membrane disrupts the structure and many functions of fungal membrane leading to inhibition of fungal growth. |
| Mechanism of action | Terconazole may exert its antifungal activity by disrupting normal fungal cell membrane permeability. Terconazole and other triazole antifungal agents inhibit cytochrome P450 14-alpha-demethylase in susceptible fungi, which leads to the accumulation of lanosterol and other methylated sterols and a decrease in ergosterol concentration. Depletion of ergosterol in the membrane disrupts the structure and function of the fungal cell leading to a decrease or inhibition of fungal growth. |
| Absorption | Following intravaginal administration of terconazole in humans, absorption ranged from 5-8% in three hysterectomized subjects and 12-16% in two non-hysterectomized subjects with tubal ligations |
| Volume of distribution | Not Available |
| Protein binding | 94.9% |
| Metabolism |
Systemically absorbed drug appears to be rapidly and extensively metabolized. Terconazole primarily undergoes oxidatative N- and O-dealkylation, dioxolane ring cleavage, and conjugation.
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| Route of elimination | Following oral (30 mg) administration of 14C-labelled terconazole, excretion of radioactivity was both by renal (32-56%) and fecal (47-52%) routes. |
| Half life | 6.9 hours (range 4.0-11.3) |
| Clearance | Not Available |
| Toxicity | The oral LD50 values were found to be 1741 and 849 mg/kg for the male and female in rat. |
| 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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