74578-69-1

• 常用中文名：头孢曲松钠
• 常用英文名：Ceftriaxone sodium
• CAS号：74578-69-1
• 分子式：C₁₈H₁₆N₈Na₂O₇S₃
• 分子量：598.544
• 相关类别： 原料药 抗生素类药物 头孢菌素类药
• 发布时间：2018-09-11 12:21:24
• 更新时间：2024-01-02 14:40:09
• Ceftriaxone钠盐是抗细菌感染的抗生素。
• 该药品为半合成的第三代头孢菌素，对大多数革兰阳性菌和阴性菌都有强大抗菌活性，抗菌谱包括绿脓杆菌、大肠杆菌、肺炎杆菌、流感嗜血杆菌、产气肠细菌、变形杆菌属、双球菌属及金葡菌等。该药品对β内酰胺酶稳定。 
  临床主要用于敏感菌感染的脑膜炎、肺炎、皮肤软组织感染、腹膜炎、泌尿系统感染、淋病、肝胆感染、外科创伤，败血症及生殖器感染等。已作为治疗淋病的第一线药物。

名称

• 中文名: 头孢曲松钠
• 英文名: Ceftriaxone sodium
• 中文别名: [6R-[6alpha,7beta(Z)]]-3-[[(1,2,5,6-四氢-2-甲基-5,6-二氧代-1,2,4-三嗪-3-基)硫]甲基]-7-[[(2-氨基-4-噻唑基](甲氧亚氨基)乙酰基]氨基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸钠盐
• 英文别名: (6R,7R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(méthoxyimino)acétyl]amino}-3-{[(6-hydroxy-2-méthyl-5-oxo-2,5-dihydro-1,2,4-triazin-3-yl)sulfanyl]méthyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ène-2-carboxylate de sodium; 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-3-[[(1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio]methyl]-, sodium salt, (6R,7R)- (1:1); Sodium (6R,7R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-{[(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)sulfanyl]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate; Ceftriaxone disodium; Disodium (6R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-{[(2-methyl-6-oxido-5-oxo-2,5-dihydro-1,2,4-triazin-3-yl)sulfanyl]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate; 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]-3-[[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio]methyl]-8-oxo-, monosodium salt, (6R,7R)-; x13-9904; rocephin; ceftriaxone; 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]-3-[[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio]methyl]-8-oxo-, sodium salt, (6R,7R)- (1:1); 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]-3-[[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio]methyl]-8-oxo-, sodium salt, (6R)- (1:2); Natrium-(6R,7R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-{[(6-hydroxy-2-methyl-5-oxo-2,5-dihydro-1,2,4-triazin-3-yl)sulfanyl]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylat; Longaceph; 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-3-[[(1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio]methyl]-, sodium salt, (6R)- (1:2); cefatriaxonehydrate; MFCD00865013; sodium (6R,7R)-7-{[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-{[(6-hydroxy-2-methyl-5-oxo-2,5-dihydro-1,2,4-triazin-3-yl)sulfanyl]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate; cephtriaxone; Ceftriaxone sodium; ro13-9904; EINECS 277-930-0; ceftriaxone disodium salt; ceftriazone disodium salt; Ceftriaxone (sodium salt)

物化性质

• 分子式: C₁₈H₁₆N₈Na₂O₇S₃
• 分子量: 598.544
• 精确质量: 598.009949
• PSA: 296.63000
• 储存条件: 2-8C

生物活性

• 描述: Ceftriaxone钠盐是抗细菌感染的抗生素。
• 相关类别:
  信号通路 >> 抗感染 >> 细菌
  研究领域 >> 感染
• 参考文献:

  [1]. Lee, S.G., et al., Mechanism of ceftriaxone induction of excitatory amino acid transporter-2 expression and glutamate uptake in primary human astrocytes. J Biol Chem, 2008. 283(19): p. 13116-23.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : XI0368800 CAS REGISTRY NUMBER : 74578-69-1 LAST UPDATED : 199512 DATA ITEMS CITED : 12 MOLECULAR FORMULA : C18-H16-N8-O7-S3.2Na.7/2H2-O MOLECULAR WEIGHT : 661.63 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Human - infant DOSE/DURATION : 16 mg/kg/3D-I TOXIC EFFECTS : Brain and Coverings - meningeal changes Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - body temperature increase REFERENCE : CPEDAM Clinical Pediatrics (Philadelphia). (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1962- Volume(issue)/page/year: 32,360,1993 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Multiple routes SPECIES OBSERVED : Human - woman DOSE/DURATION : 640 mg/kg/32D-I TOXIC EFFECTS : Gastrointestinal - nausea or vomiting Blood - agranulocytosis Nutritional and Gross Metabolic - body temperature increase REFERENCE : IJMDAI Israel Journal of Medical Sciences. (POB 1435, Jerusalem 91013, Israel) V.1- 1965- Volume(issue)/page/year: 29,52,1993 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Multiple routes SPECIES OBSERVED : Human - man DOSE/DURATION : 800 mg/kg/49D-I TOXIC EFFECTS : Blood - agranulocytosis Blood - changes in leukocyte (WBC) count REFERENCE : IJMDAI Israel Journal of Medical Sciences. (POB 1435, Jerusalem 91013, Israel) V.1- 1965- Volume(issue)/page/year: 29,52,1993 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 : 49ZAA4 "Ceftriaxon (Rocephin) ein Neues Parenterales Cephalosporin, Hahnenklee - Symposion, 9th, 1981," Dettli, L., et al. eds., Harz, Fed. Rep. Ger., S8-10, 1982 Volume(issue)/page/year: -,91,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 49ZAA4 "Ceftriaxon (Rocephin) ein Neues Parenterales Cephalosporin, Hahnenklee - Symposion, 9th, 1981," Dettli, L., et al. eds., Harz, Fed. Rep. Ger., S8-10, 1982 Volume(issue)/page/year: -,91,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1900 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 49ZAA4 "Ceftriaxon (Rocephin) ein Neues Parenterales Cephalosporin, Hahnenklee - Symposion, 9th, 1981," Dettli, L., et al. eds., Harz, Fed. Rep. Ger., S8-10, 1982 Volume(issue)/page/year: -,91,1982 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 : 49ZAA4 "Ceftriaxon (Rocephin) ein Neues Parenterales Cephalosporin, Hahnenklee - Symposion, 9th, 1981," Dettli, L., et al. eds., Harz, Fed. Rep. Ger., S8-10, 1982 Volume(issue)/page/year: -,91,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 49ZAA4 "Ceftriaxon (Rocephin) ein Neues Parenterales Cephalosporin, Hahnenklee - Symposion, 9th, 1981," Dettli, L., et al. eds., Harz, Fed. Rep. Ger., S8-10, 1982 Volume(issue)/page/year: -,91,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 2200 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 33,783,1980 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 51450 mg/kg/42D-I TOXIC EFFECTS : Skin and Appendages - dermatitis, other (after systemic exposure) Related to Chronic Data - death REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 18,1751,1984 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 42875 mg/kg/5W-I TOXIC EFFECTS : Gastrointestinal - other changes Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 18,1793,1984 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 21840 mg/kg/13W-I TOXIC EFFECTS : Liver - change in gall bladder structure or function Related to Chronic Data - death REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 18,1855,1984

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