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氯唑西林钠

氯唑西林钠用途

【用途一】
用作抗感染药

氯唑西林钠名称

[ CAS 号 ]:
642-78-4

[ 中文名 ]:
氯唑西林钠

[ 英文名 ]:
Cloxacillin Sodium

[中文别名 ]:

氯洒西林

[英文别名 ]:

Tegopen
Staphybiotic
Sodium cloxacillin
cloxacillin sodium hydrate
Ankerbin
Cloxapen
Austrastaph
Prevencilina P
Cloxacillin sodium salt hydrate
Sodium cloxacillin monohydrate

氯唑西林钠生物活性

[ 描述 ]:

Cloxacillin sodium 具有有效的抗菌活性,对Staphylococcus aureus 25923 的最小抑菌浓度为256 mg/L。

[ 相关类别 ]:

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 抗感染 >> 细菌

[体外研究]

氯唑西林是一种抗生素,用于研究许多细菌感染[1]。细胞活力测定[1]细胞系：株M12和M60。浓度：0.5μg/mL,培养时间：4-24h。结果：细菌数量明显减少。

[体内研究]

氯唑西林钠(50mg/kg,皮下注射)对金黄色葡萄球菌有显著的抗菌作用[3]动物模型：小鼠[2]。剂量：10mg/kg(药理分析)。给药：皮下注射。结果：10min时血浆浓度达到最大值8.4μg/mL,半衰期约15min。动物模型：用0.1ml生理盐水注射约2×106cfu细菌的小鼠右大腿肌肉无菌注射[3]。剂量：0-500 mg/kg。给药：感染后1小时在颈部皮下注射。结果：18小时后测得的存活金黄色葡萄球菌数量显著减少。

[参考文献]

[1]. J C Anderson, et al. The Effect of Incorporation of Cloxacillin in Liposomes on Treatment of Experimental Staphylococcal Mastitis in Mice. J Vet Pharmacol Ther. 1986 Sep;9(3):303-9.

[2]. W Calame, et al. Influence of Etoposide and Cyclophosphamide on the Efficacy of Cloxacillin and Erythromycin in an Experimental Staphylococcal Infection. Antimicrob Agents Chemother. 1989 Jun;33(6):980-2.

[3]. Peter H Nibbering, et al. 99mTc-Labeled UBI 29-41 Peptide for Monitoring the Efficacy of Antibacterial Agents in Mice Infected With Staphylococcus Aureus. J Nucl Med. 2004 Feb;45(2):321-6.

氯唑西林钠物理化学性质

[ 熔点 ]:
170ºC

[ 分子式 ]:
C₁₉H₁₇ClN₃NaO₅S

[ 分子量 ]:
475.878

[ 精确质量 ]:
475.058075

[ PSA ]:
140.87000

[ LogP ]:
1.54280

[ 外观性状 ]:
白色粉末

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents. Refrigerate.

[ 水溶解性 ]:
H2O: 50 mg/mL, clear, colorless

氯唑西林钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XH8750000

CHEMICAL NAME :: 4-Thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(3-(o-chlorophenyl)-5-methyl- 4-isoxazolecarboxamido)-3,3-dimethyl-7-oxo-, monosodium salt

CAS REGISTRY NUMBER :: 642-78-4

LAST UPDATED :: 199806

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C19-H17-C1-N3-O5-S.Na

MOLECULAR WEIGHT :: 434.45

WISWESSER LINE NOTATION :: T45 ANV ESTJ F1 F1 GVQ CMV- DT5NOJ C1 ER BG &-NA-

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,232,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1350 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 15,322,1965

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4200 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,232,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1660 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,232,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,232,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1170 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,232,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,232,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 916 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 31,232,1968

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1117 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,401,1995 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4495 No. of Facilities: 203 (estimated) No. of Industries: 2 No. of Occupations: 8 No. of Employees: 4409 (estimated) No. of Female Employees: 2017 (estimated)

氯唑西林钠安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
36/37/38-42/43

[ 安全声明 (欧洲) ]:
S22

[ WGK德国 ]:
2

[ RTECS号 ]:
XH8920000

[ 海关编码 ]:
2941109900

氯唑西林钠合成路线

详细合成路线

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氯唑西林钠海关

[ 海关编码 ]: 2941109900