68401-82-1

• 常用中文名：头孢唑肟钠
• 常用英文名：Ceftizoxime Sodium
• CAS号：68401-82-1
• 分子式：C₁₃H₁₂N₅NaO₅S₂
• 分子量：405.385
• 相关类别： 原料药 抗生素类药物 头孢菌素类药
• 发布时间：2018-04-05 08:00:00
• 更新时间：2024-01-02 13:55:29
• 头孢唑肟钠对大肠埃希菌、肺炎克雷伯菌、奇异变形杆菌等肠杆菌科细菌有强大抗菌作用，铜绿假单胞菌等假单胞菌属和不动杆菌属对该品敏感性差。头孢唑肟钠对流感嗜血杆菌和淋病奈瑟球菌有良好抗菌作用。对金黄色葡萄球菌和表皮葡萄球菌的作用较第一、第二代头孢菌素为差，耐甲氧西林金黄色葡萄球菌和肠球菌属对该品耐药，各种链球菌对该品均高度敏感。消化球菌、消化链球菌和部分拟杆菌属等厌氧菌对该品多呈敏感，艰难梭菌对该品耐药。
• 通过抑制细菌细胞壁粘肽的生物合成而达到杀菌作用。

名称

• 中文名: 头孢唑肟钠
• 英文名: ceftizoxime sodium
• 中文别名: (6R,7R)-7-[[2,3-二氢-2-亚氨基-4-噻唑基)(甲氧亚氨基)乙酰基]氨基]-8-氧代-5-硫杂-1-氮杂二环[4.2.0]辛-2-烯-2-羧酸钠盐; 7-[(2-氨基-4-噻唑基)-2-甲氧亚胺基-乙酰氨基]-8-氧-5-硫杂-1-氮杂二环[4,2,0]-2-辛烯-2-羧酸单钠盐; 益保世灵
• 英文别名: Ceftizon; MFCD01682036; Ceftix; Ceftizoxime Sodium; fr-13,479; ceftizoxim-natrium; 5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[(2Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)-1-oxoethyl]amino]-8-oxo-, monosodium salt, (6R,7R)-; Cefizox; Eposerin; 5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[(2Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino)-1-oxoethyl]amino]-8-oxo-, sodium salt, (6R,7R)- (1:1); fk749; Sodium (6R,7R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate; Epocelin; Ceftizoxime (sodium)

物化性质

• 分子式: C₁₃H₁₂N₅NaO₅S₂
• 分子量: 405.385
• 精确质量: 405.017761
• PSA: 203.58000
• 外观性状: 白色至淡黄色结晶粉末
• 储存条件: -20℃

生物活性

• 描述: Ceftizoxime sodium (SKF-88373) 是第三代抗生素, 有效抗革兰氏阴性和革兰氏阳性菌, Ceftizoxime结合青霉素结合蛋白(PBPs)和抑制细菌细胞壁的合成。
• 相关类别:
  信号通路 >> 抗感染 >> 细菌
  研究领域 >> 感染
• 靶点:

  Antibacterial

• 体外研究: 头孢唑肟是第三代头孢菌素,可用于肠胃外给药。与其他第三代头孢菌素不同,头孢唑肟中的整个C-3侧链已被去除,以防止水解酶失活。它的性质非常类似头孢噻肟,但不受新陈代谢的影响。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : XI0368000 CHEMICAL NAME : 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(((2-amino-4-thiazolyl)- (methoxyimino)acetyl)amino)-8-oxo-, monosodium salt, (6R-(6-alpha,7-beta(Z)))- CAS REGISTRY NUMBER : 68401-82-1 LAST UPDATED : 199306 DATA ITEMS CITED : 18 MOLECULAR FORMULA : C13-H12-N5-O5-S2.Na MOLECULAR WEIGHT : 405.41 WISWESSER LINE NOTATION : T46 ANV ES GUTJ GVO CMVYUNO1&- ET5N CSJ BZ &-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 : >10 gm/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: 30,1669,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 8130 mg/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Lungs, Thorax, or Respiration - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >10 gm/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: 30,1669,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 5570 mg/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Lungs, Thorax, or Respiration - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >10 gm/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: 30,1669,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 8930 mg/kg TOXIC EFFECTS : Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Lungs, Thorax, or Respiration - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >10 gm/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: 30,1669,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 5150 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 24,905,1982 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >3200 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Cardiac - cardiomyopathy including infarction REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : >3200 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: 30,1669,1980 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : >3200 mg/kg TOXIC EFFECTS : Behavioral - muscle weakness Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 29120 mg/kg/13W-I TOXIC EFFECTS : Blood - hemorrhage Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Skin and Appendages - dermatitis, other (after systemic exposure) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 58240 mg/kg/26W-I TOXIC EFFECTS : Blood - hemorrhage Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Skin and Appendages - dermatitis, other (after systemic exposure) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 58240 mg/kg/26W-I TOXIC EFFECTS : Blood - hemorrhage Skin and Appendages - dermatitis, other (after systemic exposure) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 8960 mg/kg/4W-I TOXIC EFFECTS : Blood - hemorrhage Skin and Appendages - dermatitis, other (after systemic exposure) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphokinase REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 10 gm/kg SEX/DURATION : male 9 week(s) pre-mating female 2 week(s) pre-mating - 22 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1669,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 27 gm/kg SEX/DURATION : male 9 week(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) 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: 34,466,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 1100 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : 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: 34,466,1981

安全

• 危害码 (欧洲): Xi
• 风险声明 (欧洲): 36/37/38
• 安全声明 (欧洲): 26
• 海关编码: 2941905990

海关

海关编码	2941905990