< 生产厂家价格 >

头孢硫脒

头孢硫脒用途

Cefathiamidine 是第一代头孢菌素抗菌剂,用于治疗由易感细菌引起的感染。Cefathiamidine 对细菌具有广泛的抗菌活性,可用于治疗呼吸道、肝脏、五官感觉、尿路感染以及心内膜炎和败血症。

点击显示

头孢硫脒名称

[ CAS 号 ]:
33075-00-2

[ 中文名 ]:
头孢硫脒

[ 英文名 ]:
Cefathiamidine

[中文别名 ]:

[英文别名 ]:

头孢硫脒生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Bacterial[1]

[体外研究]

研究了头孢硫脒对粪链球菌和粪链球菌的体外抗菌活性,并与其它β-内酰胺类药物进行了比较。56株粪链球菌均被2mg/L头孢硫脒抑制。头孢硫脒和氨苄西林对10株粪链球菌的MBCs测定表明,MBC/MIC比值大于64。当头孢硫脒和氨苄西林的浓度大于MIC时,粪链球菌的杀灭率降低。以2 mg/L头孢硫脒或4 mg/L氨苄青霉素杀灭最快。随着1毫克/升庆大霉素的加入,这种矛盾的杀菌效果被消除。时间杀伤研究表明,氨基糖苷和β-内酰胺的联合作用可在6小时内杀死99.9%的细胞[2]。

[体内研究]

头孢硫脒不经口服吸收,因此通过肠外途径(静脉或肌肉注射)给药。头孢硫脒广泛分布于大多数体液和组织中,但不能通过血脑屏障。头孢硫脒的蛋白质结合能力为23%,90%以上的头孢硫脒由肾脏无变化地排出[1]。

[参考文献]

[1]. Zhi LJ, et al. Population pharmacokinetics and dosing optimization of cefathiamidine in children with hematologic infection. Drug Des Devel Ther. 2018 Apr 17;12:855-862.

[2]. Chen HY, et al. The killing effects of cefathiamidine or ampicillin alone and in combination with gentamicin against enterococci. J Antimicrob Chemother. 1983 Jul;12(1):19-26.

头孢硫脒物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 分子式 ]:
C₁₉H₂₈N₄O₆S₂

[ 分子量 ]:
472.579

[ 精确质量 ]:
472.145020

[ PSA ]:
188.00000

[ LogP ]:
2.67

[ 外观性状 ]:
粉末

[ 折射率 ]:
1.653

[ 储存条件 ]:
-20℃

头孢硫脒毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XI0373000

CHEMICAL NAME :: 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(2-((N,N'-diisopropylamidino)thio) acetamido)-3-(hydroxymethyl)-8-oxo-, acetate

CAS REGISTRY NUMBER :: 33075-00-2

LAST UPDATED :: 199406

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C19-H28-N4-O6-S2

MOLECULAR WEIGHT :: 472.63

WISWESSER LINE NOTATION :: T46 ANV ES GUTJ CMV1SYMY1&1&UNY1&1 G1OV1 HVQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1260 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CMJODS Chinese Medical Journal (Beijing, English Edition). (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1975- Adopted vol. no. 92 in 1979. Volume(issue)/page/year: 92,26,1979

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 720 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CMJODS Chinese Medical Journal (Beijing, English Edition). (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1975- Adopted vol. no. 92 in 1979. Volume(issue)/page/year: 92,26,1979