1405-20-5 Usage
Description
Polymyxin B sulfate is a mixture of cationic peptides originally isolated from Bacillus polymyxa, consisting of a cyclic heptapeptide and a tripeptide side chain acylated at the amino terminus by a fatty acid. It is a nearly odorless, white to buff powder, freely soluble in water, and slightly soluble in alcohol. 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.
Uses
Used in Antibacterial Applications:
Polymyxin B sulfate is used as an antibiotic with bactericidal action on E. coli. It binds to the lipid A portion of bacterial lipopolysaccharides, inducing pore formation in the membranes of cortex cells and altering membrane structure, which allows small molecules leakage and inhibits the growth of Gram-negative bacteria.
Used in Topical Antibiotic Applications:
Polymyxin B sulfate is used as a topical antibiotic agent, often used in combination with neomycin. It is commonly found in products such as ointments, creams, eye, and ear drops.
Used in Biochemical Studies:
Polymyxin B sulfate is also utilized in biochemical research for studying its mechanism of action, which involves binding and interfering with the permeability of the cellular membrane of Gram-negative bacteria.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, Polymyxin B sulfate is used as an active ingredient in the development of antibiotics targeting multidrug-resistant Gram-negative bacteria due to its rapid in vitro bactericidal activity.
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.
Indications
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.
Dosage
1. Intravenous injection: Adults and children with normal renal function: 1.5 to 2.5 mg per kilogram of body weight per day (for per kg body weight, generally apply not more than 2.5 mg), divide into 2 times with 1 time every 12 hours of infusion. Dilute every 50mg of the product with 500 mL of 5% glucose solution and further add drop wise. Babies with normal renal function can tolerate a amount of 4 mg/day per kilogram of body weight.
2. Intramuscular injection: Adults and children: apply 2.5 to 3 mg per kilogram of body weight; apply in divided doses with applying 1 time every 4 to 6 hours. For baby, the dosage can be 4 mg per day per kilogram of body weight. For new born children, we can apply to 4.5 mg per time per kilogram of body weight.
3. intrathecal injection (for Pseudomonas aeruginosa meningitis): Each mL of drug solution prepared by the sodium chloride injection contains 5mg. Adults and children with over 2 years of age, apply 5 mg daily; after application of 3 to 4 days, change one time every other day, and continue for at least 2 weeks until the result of cerebrospinal fluid culture becomes negative and the sugar inspection becomes normal. For children less than 2 years of age, apply 2mg 1 time per day for continuous 3 to 4 days (or 2.5mg per every other day); after that, apply 2.5mg every other day, until the test becomes normal.
4. The ophthalmic solution concentration: 1~2.5mg per milliliter.
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.
Injection polymyxin B sulfate manufacturer
Shanghai “Xin Xianfeng” Pharmaceutical Co., Ltd. Zhunzi H31022973
Shanghai No. 1 Biochemical Pharmaceutical Co., Ltd. Zhunzi H31022631
Precautions
1. Pregnant and lactating women, children, patients with severe kidneys damage and severe kidney dysfunction should either take with caution or reduce the administrated amount.
2. this product has relative large toxicity and a poor efficacy in treating deep tissue infection. It is also not the primary choice of drug for treating any kinds of infection.
3. intravenous injection may lead to respiratory depression and thus should generally not used. Half of the amount in daily dose should subject to intravenous drip, and can’t subject to disposable rapid bolus avoid extensive neuromuscular blockade.
4. it shouldn’t be used in combination with drugs with other renal toxicity or neuromuscular blocking effects to avoid accidents.
Biochem/physiol Actions
Polymyxin B?is one of the most important antibiotics used to treat gram-negative bacterial infections, including infections caused by carbapenem-resistant non-fermenters and carbapenem-resistant?Enterobacteriaceae.
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.
in vitro
polymyxin b elicited up-regulation of dendritic cells (dcs) maturation markers, including the increase in the in the expression of co-stimulatory molecule cd86 and hla-class i and ii molecules. polymyxin b induced a progressive increase in the adhesion property of human dcs. in addition, polymyxin b triggered the activation of the erk1/2 pathway and iκb-α/nf-κb pathways [1].
in vivo
male bacteraemia ddy mice were subcutaneously treated with polymyxin b at a dose of 5, 10, 15 or 20 mg/kg for 7 days. polymyxin b, in a dose-dependent fashion, improved the survival both of ou-01062- and ou-98039-infected mice. in polymyxin b-treated mice, except for 5 mg/kg polymyxin b, the viable cell counts had a tendency to reduce steadily in each concentration group. it was showed a rapid and marked decline of bacterial cell count between 3 to 6 h after infection [2].
references
[1]. valentinis, b., bianchi, a., zhou, d., cipponi, a., catalanotti, f., russo, v., & traversari, c. direct effects of polymyxin b on human dendritic cells maturation: the role of i b- /nf- b and erk1/2 pathways and adhesion. journal of biological chemistry. 2005; 280(14): 14264-14271. [2]. miyajima, y., hiramatsu, k., mizukami, e., morinaga, r., ishii, h., & shirai, r. et al. in vitro and in vivo potency of polymyxin b against imp-type metallo-β-lactamase-producing pseudomonas aeruginosa. international journal of antimicrobial agents. 2008; 32(5): 437-440.
Check Digit Verification of cas no
The CAS Registry Mumber 1405-20-5 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 1,4,0 and 5 respectively; the second part has 2 digits, 2 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1405-20:
(6*1)+(5*4)+(4*0)+(3*5)+(2*2)+(1*0)=45
45 % 10 = 5
So 1405-20-5 is a valid CAS Registry Number.
InChI:InChI=1/C48H82N16O13.H2O4S/c1-27(2)24-37-47(76)59-32(11-19-52)41(70)56-31(10-18-51)43(72)61-35(14-22-65)39(68)54-21-13-34(45(74)57-33(12-20-53)44(73)64-38(48(77)63-37)25-28-6-4-3-5-7-28)60-42(71)30(9-17-50)58-46(75)36(15-23-66)62-40(69)29(8-16-49)55-26-67;1-5(2,3)4/h3-7,26-27,29-38,65-66H,8-25,49-53H2,1-2H3,(H,54,68)(H,55,67)(H,56,70)(H,57,74)(H,58,75)(H,59,76)(H,60,71)(H,61,72)(H,62,69)(H,63,77)(H,64,73);(H2,1,2,3,4)
