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头孢硫脒

头孢硫脒用途

【用途一】
主要用于治疗由敏感菌所致肝胆感染、泌尿系统感染、呼吸系统感染、败血症、心内膜炎和脑膜炎等病症
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头孢硫脒作用

该品为第一代头孢菌素，为中国首创用于临床。抗菌谱与头孢噻吩相似，对金葡菌、草绿色链球菌、肺炎球菌的作用较强，对肠球菌有独特的抗菌活性，主要用于金葡菌、肺炎球菌及链球菌所致呼吸道感染，胆道感染、尿路感染、妇科感染、败血症、肺炎、脑膜炎等感染。

药理毒理1．药理该品对革兰阳性菌及部分阴性菌有抗菌活性，对革兰阳性球菌的作用尤强。该品体外抗菌活性试验表明：对肺炎球菌、化脓性链球菌、金黄色葡萄球菌（MSSA菌株）、表皮葡萄球菌（MSSE菌株）和卡他布兰汉菌有较强的抗菌活性，对肺炎链球菌MIC90为0.25μg/ ml，对化脓性链球菌MIC90为0.5μg/ml，对其他3种细菌的MIC90均小于8.0μg/ml，对流感嗜血杆菌亦有较强的抗菌活性，MIC90为2.0μg/ml。对肠球菌亦显示有很强的体外抗菌活性，MIC90为2.0μg/ml。对草绿色链球菌、溶血性链球菌、非溶血性链球菌、白喉杆菌、产气荚膜杆菌、破伤风杆菌和炭疽杆菌均有良好抗菌作用。对金黄色葡萄球菌（MRSA菌株）、表皮葡萄球菌（MRSE菌株）的体外抗菌活性不如万古霉素。该品作用机制为抑制敏感菌的细胞壁合成，而产生杀菌作用。2．毒理该品小鼠静脉注射的LD50为（1.02±0.04）g/kg，腹腔注射的LD50为（1.26±0.23)g/kg。生殖毒性试验中，试验组小鼠的胎仔死亡率明显高于对照组（p<0.01）。药代动力学：该品口服不吸收，静脉滴注1.0g后，血药峰浓度（Cmax)为（68.93±6.86)mg/L，血消除半衰期（t1/2β）为（1.19±0.12)h，血药浓度-时间曲线下面积（AUC)为（94.7±9.8)mg/(L.h)，12小时尿药累计排泄率为93.1±3.2%。肌内注射1.0g后，血药峰浓度（Cmax)为（35.12±4.34)mg/L，达峰时间（tmax)为（0.78±0.08)h，半衰期为（1.38±0.21)h，血药浓度-时间曲线下面积（AUC)为（85.3±8.0)mg/(L.h)，12小时尿中药累计排泄率为84.2±5.9%。与静脉滴注相比，其绝对生物利用度为90.3±6.4%。该品注射后在体内组织分布广泛，以胆汁、肝、肺等处含量为高，不透过血-脑脊液屏障。在机体内几乎不代谢，主要从尿中排出，12小时尿中排出给药量的90%以上。肾功能减退患者，肌内注射后血清半衰期延长至13.2小时，约为正常半衰期的10倍，24小时尿中仅排出给药量的3.2%，血液透析可排出给药量的20%~30%。适应症：用于敏感菌所引起呼吸系统、肝胆系统、五官、尿路感染及心内膜炎、败血症。
用法和用量：该品口服不吸收。肌内注射：一次0.5g~1.0g,一日4次；小儿按体重一日50~100mg/kg，分3~4次给药。静脉注射：一次1g，一日2~4次；小儿按体重一日50~100mg/kg，分2~4次给药。
临用前加灭菌注射用水或氯化钠注射液适量溶解。
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头孢硫脒名称

[ CAS 号 ]:
51627-14-6

[ 中文名 ]:
头孢硫脒

[ 英文名 ]:
Cefatrizine

[中文别名 ]:

[英文别名 ]:

头孢硫脒生物活性

[ 描述 ]:

头孢曲辛(BL-S-640)是一种口服活性广谱头孢菌素抗生素。头孢曲嗪也是一种eEF2K抑制剂,在人类乳腺癌细胞中具有抗增殖活性,可诱导内质网应激,导致细胞死亡。头孢曲嗪可用于癌症和细菌感染的研究[1][2]。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡
研究领域 >> 癌症
研究领域 >> 感染
信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

eEF2K, bacterial[1][2].


[体外研究]

头孢曲嗪(0-100µM；24 h)以剂量依赖性方式对MCF-7和MDA-MB-436细胞生长产生显著的抗增殖作用[1]。头孢曲嗪(30µM；12 h)诱导乳腺癌细胞内质网应激[1]。头孢曲嗪(12、24、36 h)增加MCF-7和MDA-MB-436细胞中CHOP(ER应激诱导凋亡的标志物)的水平,并促进eEF2K调节的ER应激途径(Bip、p-PERK、XBP-1S和p-JNK)中核心蛋白的表达[1]。细胞增殖试验[1]细胞系：MCF-7,MDA-MB-436细胞浓度：0-100µM培养时间：24小时结果：在33µM和29µM时,对细胞产生显著的抗增殖作用,并导致MCF-7和MDA-MB-336细胞几乎50%的抑制。细胞活力测定[1]细胞系：MCF-7,MDA-MB-436细胞浓度：30µM培养时间：12小时结果：导致大量细胞质空泡化。

[体内研究]

头孢曲嗪(BL-S-640)(0.2、1、5、25 mg/kg；口服；每天4次,连续3天)可减少奇异芽孢杆菌囊内感染模型中膀胱和肾脏中感染生物的数量[2]。动物模型：雄性Wiss Webster小鼠(19-21g；奇异芽孢杆菌囊内感染模型)[2]。剂量：0.2、1、5、25 mg/kg给药：口服；每天4次,持续3天。结果：当剂量为1 mg/kg时,膀胱中的感染微生物数量减少到1000个以下,当剂量为0.2 mg/kg时肾脏中的感染细菌数量减少到了1000个以下。

头孢硫脒物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
948.1±65.0 °C at 760 mmHg

[ 分子式 ]:
C18H18N6O5S2

[ 分子量 ]:
462.503

[ 闪点 ]:
527.2±34.3 °C

[ 精确质量 ]:
462.078003

[ PSA ]:
225.13000

[ LogP ]:
-0.41

[ 外观性状 ]:
白色至略淡黄色粉末

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.794

[ 储存条件 ]:
库房通风低温干燥

头孢硫脒毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XI0340000
CHEMICAL NAME :
5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((amino(4-hydroxyphenyl)acetyl) amino)-8-oxo-3-((1H-1,2,3-triazol-4-ylthio)methyl)-, (6R-(6-alpha,7-beta(R)))-
CAS REGISTRY NUMBER :
51627-14-6
LAST UPDATED :
199410
DATA ITEMS CITED :
21
MOLECULAR FORMULA :
C18-H18-N6-O5-S2
MOLECULAR WEIGHT :
462.54
WISWESSER LINE NOTATION :
T46 ANV ES GUTJ CMVYZR DQ& HVQ G1S- DT5MNNJ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>6 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
4325 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>6 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>240 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>6 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
6410 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>6 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Gastrointestinal - changes in structure or function of salivary glands
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>400 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>1600 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>40 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
1500 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
3 gm/kg
TOXIC EFFECTS :
Behavioral - food intake (animal) Gastrointestinal - hypermotility, diarrhea
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
>80 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,612,1976 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
175 mg/kg
SEX/DURATION :
female 8-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,129,1976
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2800 mg/kg
SEX/DURATION :
female 8-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,129,1976
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
5600 mg/kg
SEX/DURATION :
female 8-14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,129,1976
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
175 mg/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,129,1976
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
225 mg/kg
SEX/DURATION :
female 8-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,144,1976
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
3600 mg/kg
SEX/DURATION :
female 8-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 29,144,1976
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相关药品：

推荐生产厂家/供应商：

公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

产品详情：头孢硫脒

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Cefatrizine

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥2369.0/100mg ￥需询单/1g ￥需询单/1g ￥需询单/1g

联系人：阿拉丁

产品详情：头孢他嗪

公司名：湖北魏氏化学试剂股份有限公司

区域：武汉市洪山区

价格：
￥需询单/5mg ￥需询单/25mg ￥需询单/10g ￥需询单/50g

联系人：张栋

产品详情：头孢硫脒

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