药品详细
Tinidazole(替硝唑)
化学结构式图
中文名
替硝唑
英文名
Tinidazole
分子式
C8H13N3O4S
化学名
1-[2-(ethanesulfonyl)ethyl]-2-methyl-5-nitro-1H-imidazole
分子量
Average: 247.272
Monoisotopic: 247.062676609
Monoisotopic: 247.062676609
CAS号
19387-91-8
ATC分类
J01X Other Antibacterials;P01A 未知
药物类型
small molecule
阶段
approved
商品名
Fasigyn;Tindamax;
同义名
tinidazole;
基本介绍
A nitroimidazole antitrichomonal agent effective against Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia infections. [PubChem]
生产厂家
- Mission pharmacal co
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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
antibacterials 抗细菌;
药理
| Indication | For the treatment of trichomoniasis caused by T. vaginalis in both female and male patients. Also for the treatment of giardiasis caused by G. duodenalis in both adults and pediatric patients older than three years of age and for the treatment of intestinal amebiasis and amebic liver abscess caused by E. histolytica in both adults and pediatric patients older than three years of age. |
| Pharmacodynamics | Tinidazole is a synthetic antiprotozoal agent. Tinidazole demonstrates activity both in vitro and in clinical infections against the following protozoa: Trichomonas vaginalis, Giardia duodenalis (also termed G. lamblia), and Entamoeba histolytica. Tinidazole does not appear to have activity against most strains of vaginal lactobacilli. |
| Mechanism of action | Tinidazole is a prodrug and antiprotozoal agent. The nitro group of tinidazole is reduced in Trichomonas by a ferredoxin-mediated electron transport system. The free nitro radical generated as a result of this reduction is believed to be responsible for the antiprotozoal activity. It is suggested that the toxic free radicals covalently bind to DNA, causing DNA damage and leading to cell death. The mechanism by which tinidazole exhibits activity against Giardia and Entamoeba species is not known, though it is probably similar. |
| Absorption | Rapidly and completely absorbed under fasting conditions. Administration with food results in a delay in Tmax of approximately 2 hours and a decline in Cmax of approximately 10% and an AUC of 901.6 ± 126.5 mcg hr/mL. |
| Volume of distribution |
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| Protein binding | Plasma protein binding of tinidazole is 12%. |
| Metabolism |
Hepatic, mainly via CYP3A4. Tinidazole, like metronidazole, is significantly metabolized in humans prior to excretion. Tinidazole is partly metabolized by oxidation, hydroxylation and conjugation. Tinidazole is the major drug-related constituent in plasma after human treatment, along with a small amount of the 2-hydroxymethyl metabolite.
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| Route of elimination | Tinidazole crosses the placental barrier and is secreted in breast milk. Tinidazole is excreted by the liver and the kidneys. Tinidazole is excreted in the urine mainly as unchanged drug (approximately 20-25% of the administered dose). Approximately 12% of the drug is excreted in the feces. |
| Half life | Elimination half-life is 13.2 ± 1.4 hours. Plasma half-life is 12 to 14 hours. |
| Clearance | Not Available |
| Toxicity | There are no reported overdoses with tinidazole in humans. In acute studies with mice and rats, the LD 50 for mice was generally > 3,600 mg/kg for oral administration and was > 2,300 mg/kg for intraperitoneal administration. In rats, the LD 50 was > 2,000 mg/kg for both oral and intraperitoneal administration. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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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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