Chemical Property of CID 5702105
Chemical Property:
- Appearance/Colour:White crystalline powder
- Vapor Pressure:0mmHg at 25°C
- Melting Point:217-220°C (dec.)
- Boiling Point:1651ºC at 760 mmHg
- PKA:pKa 8.9 (Uncertain)
- Flash Point:952.3ºC
- PSA：573.64000
- LogP:2.54990
- Storage Temp.:2-8°C
- Solubility.:H2O: 50 mg/mL
- Water Solubility.:Soluble in water at 50mg/ml/n
- Hydrogen Bond Donor Count:20
- Hydrogen Bond Acceptor Count:22
- Rotatable Bond Count:29
- Exact Mass:1300.71730696
- Heavy Atom Count:90
- Complexity:2240
- Purity/Quality:
-
99%, *data from raw suppliers
Polymyxin B Sulfate USP *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xn
- Hazard Codes:Xn
- Statements:
22
- Safety Statements:
22-24/25
- MSDS Files:
-
SDS file from LookChem
Total 1 MSDS from other Authors
Useful:
- Canonical SMILES:CCC(C)CCCCC(=O)NC(CCN)C(=O)NC(C(C)O)C(=O)NC(CCN)C(=O)NC1CCNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CCN)CC2=CC=CC=C2)CC(C)C)CCN)CCN)C(C)O.OS(=O)(=O)O
- Recent EU Clinical Trials:A multicenter, open-label, randomized, active-controlled, Phase 2 study to evaluate the pharmacokinetics, efficacy, and safety of intravenous BV100 combined with Polymyxin B versus best available therapy in adult patients with ventilator-associated bacterial pneumonia suspected or confirmed to be due to carbapenem-resistant Acinetobacter baumannii
-
Indications
Polymyxin B sulfate is similar with polymyxin E, and has either bacteriostatic or bactericidal effect on various kinds of gram-negative bacteria, such as Escherichia coli, Pseudomonas aeruginosa, Escherichia coli deputy, Klebsiella pneumoniae, acidophilus, Bordetella pertussis and Shigella dysentery. It is mainly applied to the treatment of infection in wounds, the urinary tract, eyes, ears, and bronchus caused by Pseudomonas aeruginosa and other kinds of pseudomonas. It can also be applied for treating sepsis, peritonitis, and severe infection caused by aminoglycoside-resistant, third generation cephalosporins-resistant bacteria and Pseudomonas aeruginosa or other sensitive strains, such as bacteremia, endocarditis, pneumonia, and burn infection. Polymyxin B is one of a group of cyclic polypeptides elaborated by
Bacillus polymyxa. The drug is a surface-active agent. It is thought to alter the
lipoprotein membrane of bacteria so that it no longer functions as an effective
barrier, thereby allowing the cell contents to escape. Polymyxin B is effective against
Pseudomonas, E. coli, and other gram-negative bacteria except the Proteus and
Serratia species. It has little effect on gram-positive organisms.
-
Drug Interactions
We should avoid apply it in combination with drugs causing significant damage to the kidneys, skeletal muscle relaxants, aminoglycoside antibiotics, and anesthetic drugs with significant effect of muscle relaxation (such as enflurane). Also we should avoid simultaneous intravenous administration of quinine, and magnesium. Combining polymyxin B sulfate with sulfa drugs, rifampicin, and semi-synthetic penicillin has a better efficacy than single application in treating severe infections resistant Gram-negative bacteria.
The above information is edited by the lookchem of Dai Xiongfeng.
-
Uses
Biochemical studies.
Polymyxin B is a kind of anti-Gram-negative poly-peptide antibiotics which can alter membrane structure allowing small molecules leakage and inhibit the growth of Gram-negative bacteria. It has bactericidal effect on Escherichia coli through binding to the lipid A portion of bacterial lipopolysaccharide. Mechanism of action: bind and interfere with the permeability o the cellular membrane. Anti-bacteria spectrum: gram negative bacteria. antibacterial Antibiotic with bactericidal action on E. coli. Binds to the lipid A portion of bacterial lipopolysaccharides. Induces pore formation in the membranes of cortex cells from excised sorghum roots. Mixtu
re of Polymyxin B1 and B2 sulfate.
Biological potency (dry basis): >6000U/mg. Polymyxin B sulfate is used as topical antibiotic agent, often used in combination with neomycin; products include ointments, creams, eye, and ear drops.
-
Description
The polymyxins are cationic peptides originally isolated from B. polymyxa. They bind and kill Gram-negative bacteria. The B series of polymyxins consist of a cyclic heptapeptide and a tripeptide side chain acylated at the amino terminus by a fatty acid. Polymyxin B (sulfate) is a mixture of at least four closely related components, polymyxin B1 to B4, with polymyxin B1 and B2 being the two major components. Polymyxin B (sulfate) has rapid in vitro bactericidal activity against major multidrug-resistant Gram-negative bacteria, such as P. aeruginosa, A. baumannii, and K. pneumoniae.
-
Clinical Use
Polymyxin B is produced by fermentation of Bacillus polymyxa. It is separated from a mixture of related
cyclic peptides and is primarily active against Gram-negative microorganisms. It apparently binds to
phosphate groups in bacterial cytoplasmic membranes and disrupts their integrity. It is used IM or IV as a
sulfate salt to treat serious urinary tract infections, meningitis, and septicemia, primarily caused by
Pseudomonas aeruginosa, but some other Gram-negative bacteria also will respond. Irrigation of the urinary
bladder with solutions of polymyxin B sulfate is employed as well by some to reduce the incidence of
infections subsequent to installation of indwelling catheters. Additionally, it is used ophthalmically to treat
infections by P. aeruginosa. When given parenterally, the drug is neuro- and nephrotoxic and, therefore, is
employed only after other drugs have failed.
