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药品详细

Cefotiam(头孢替安)

化学结构式图
中文名
头孢替安
英文名
Cefotiam
分子式
C18H23N9O4S3
化学名
(6R,7R)-7-[2-(2-amino-1,3-thiazol-4-yl)acetamido]-3-[({1-[2-(dimethylamino)ethyl]-1H-1,2,3,4-tetrazol-5-yl}sulfanyl)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
分子量
Average: 525.628
Monoisotopic: 525.103512339
CAS号
61622-34-2
ATC分类
J01D Other Beta- lactam Antibacterials
药物类型
small molecule
阶段
approved
商品名
Ceradon;
同义名
Cefotiam hydrochloride;Cefotiamum [INN-Latin];CTM;
基本介绍

One of the cephalosporins that has a broad spectrum of activity against both gram-positive and gram-negative microorganisms. [PubChem]

生产厂家
  • Takeda chemical industries ltd
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Muller R, Bottger C, Wichmann G: Suitability of cefotiam and cefuroxime axetil for the perioperative short-term prophylaxis in tonsillectomy patients. Arzneimittelforschung. 2003;53(2):126-32. Pubmed
  2. Kolben M, Mandoki E, Ulm K, Freitag K: Randomized trial of cefotiam prophylaxis in the prevention of postoperative infectious morbidity after elective cesarean section. Eur J Clin Microbiol Infect Dis. 2001 Jan;20(1):40-2. Pubmed
  3. Shimizu S, Chen KR, Miyakawa S: Cefotiam-induced contact urticaria syndrome: an occupational condition in Japanese nurses. Dermatology. 1996;192(2):174-6. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Carboxylic Acids and Derivatives
  • Cephalosporins
Substructures
  • Ethers
  • Hydroxy Compounds
  • Acetates
  • Amino Ketones
  • Carboxylic Acids and Derivatives
  • Aliphatic and Aryl Amines
  • Beta Lactams
  • Enamines
  • Tetrazoles
  • Thiazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Cephalosporins
  • Lactams
  • Imines
  • Azetidines
  • Cyanamides
适应症
antibacterials 抗细菌;
药理
Indication For treatment of severe infections caused by susceptible bacteria.
Pharmacodynamics Cefotiam is a third generation beta-lactam cephalosporin antibiotic. It has broad spectrum activity against Gram positive and Gram negative bacteria. It does not have activity against Pseudomonas aeruginosa. Cefotiam works by inhibiting bacterial cell wall biosynthesis.
Mechanism of action The bactericidal activity of cefotiam results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs).
Absorption Rapidly absorbed following intramuscular injection. Bioavailability is 60% following intramuscular injection.
Volume of distribution Not Available
Protein binding 40%
Metabolism
Not Available
Route of elimination Not Available
Half life Approximately 1 hour.
Clearance Not Available
Toxicity Adverse effects following overdosage include nausea, vomiting, epigastric distress, diarrhea, and convulsions.
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility Soluble Not Available
logP -2.1 Not Available
Predicted Properties
Property Value Source
water solubility 1.29e+00 g/l ALOGPS
logP -0.33 ALOGPS
logP -3.1 ChemAxon
logS -2.6 ALOGPS
pKa (strongest acidic) 2.79 ChemAxon
pKa (strongest basic) 8.36 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 10 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 172.46 ChemAxon
rotatable bond count 10 ChemAxon
refractivity 142.34 ChemAxon
polarizability 49.87 ChemAxon
药物相互作用
食物相互作用
Not Available

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