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药品详细

Polymyxin B Sulfate(多粘菌素B硫酸盐)

化学结构式图
中文名
多粘菌素B硫酸盐
英文名
Polymyxin B Sulfate
分子式
C56H98N16O13
化学名
N-[3-amino-1-({1-[(3-amino-1-{[6,9,18-tris(2-aminoethyl)-15-benzyl-3-(1-hydroxyethyl)-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosan-21-yl]carbamoyl}propyl)carbamoyl]-2-hydroxypropyl}carbamoyl)propyl]-6-methyloctanamide
分子量
Average: 1203.4767
Monoisotopic: 1202.749927302
CAS号
1405-20-5
ATC分类
A07A 未知;J01X Other Antibacterials;S01A 抗感染药;S02A 未知;S03A 未知
药物类型
small molecule
阶段
approved
商品名
Aerosporin;Poly-RX;
同义名
Polymixin B sulfate;Polymyxin B sulfate salt;Polymyxin B sulphate;
基本介绍

Polymyxin B sulfate is a mixture of polymyxins B1 and B2, obtained from Bacillus polymyxa strains. They are basic polypeptides of about eight amino acids and have cationic detergent action on cell membranes. Polymyxin B is used for infections with gram-negative organisms, but may be neurotoxic and nephrotoxic. All gram-positive bacteria, fungi, and the gram-negative cocci, N. gonorrhea and N. menigitidis, are resistant. It is appropriate for treatment of infections of the urinary tract, meninges, and blood stream, caused by susceptible strains of Pseudomonas aeruginosa.

生产厂家
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Glaxosmithkline
  • Paddock laboratories inc
  • X gen pharmaceuticals inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Yuan Z, Tam VH: Polymyxin B: a new strategy for multidrug-resistant Gram-negative organisms. Expert Opin Investig Drugs. 2008 May;17(5):661-8. Pubmed
  2. Zavascki AP, Goldani LZ, Li J, Nation RL: Polymyxin B for the treatment of multidrug-resistant pathogens: a critical review. J Antimicrob Chemother. 2007 Dec;60(6):1206-15. Epub 2007 Sep 17. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes Not Available
Substructures Not Available
适应症
antibacterials 抗细菌;
药理
Indication For treatment of infections of the urinary tract, meninges, and blood stream, caused by susceptible strains of Pseudomonas aeruginosa.
Pharmacodynamics Polymyxin B sulfate is a mixture of polymyxins B1 and B2, obtained from Bacillus polymyxa strains. They are basic polypeptides of about eight amino acids and have cationic detergent action on cell membranes. Polymyxin B is used for infections with gram-negative organisms, but may be neurotoxic and nephrotoxic. All gram-positive bacteria, fungi, and the gram-negative cocci, N. gonorrhea and N. menigitidis, are resistant.
Mechanism of action Polymyxin B sulfate has a bactericidal action against almost all gram-negative bacilli except the Proteus group. Polymyxin B sulfate interacts with the lipopolysaccharide of the cytoplasmic outer membrane of Gram-negative bacteria, altering membrane permeability and causing cell death. It does not need to enter the cell.
Absorption Not absorbed from the normal alimentary tract.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination The drug is excreted slowly by the kidneys.
Half life Not Available
Clearance Not Available
Toxicity Overdose can cause stomach pains, vomiting, and diarrhea.
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility 25 mg/mL Not Available
logP -4.861 Not Available
Predicted Properties
Property Value Source
water solubility 7.44e-02 g/l ALOGPS
logP -0.89 ALOGPS
logP -7.2 ChemAxon
logS -4.2 ALOGPS
pKa (strongest acidic) 11.57 ChemAxon
pKa (strongest basic) 10.23 ChemAxon
physiological charge 5 ChemAxon
hydrogen acceptor count 18 ChemAxon
hydrogen donor count 18 ChemAxon
polar surface area 490.66 ChemAxon
rotatable bond count 29 ChemAxon
refractivity 313.22 ChemAxon
polarizability 129.71 ChemAxon
药物相互作用
Drug Interaction
Vecuronium Polymyxin B may increase the neuromuscular blocking action of Vecuronium. Risk of respiratory depression and apnea. Consider alternate therapy or monitor for prolonged neuromuscular blocking effects, such as respiratory paralysis.
食物相互作用
Not Available

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