Polymyxin B sulfate
Basic information Indications Dosage Drug Interactions Injection polymyxin B sulfate manufacturer Precautions Uses Safety Related Supplier
Polymyxin B sulfate Chemical Properties
- Melting point:217-220°C (dec.)
- storage temp. 2-8°C
- solubility H2O: 50 mg/mL
- form powder
- pkapKa 8.9 (Uncertain)
- color colorless or slightly yellow
- PHpH (10g/L, 25℃) : 4.5～7.0
- optical activity[α]/D 20/D (Rotation: -2.3 +/- 0.2 degrees)
- Water Solubility Soluble in water at 50mg/ml/n
- Merck 14,7573
- CAS DataBase Reference1405-20-5(CAS DataBase Reference)
- EPA Substance Registry SystemPolymixin B sulfate (1405-20-5)
Polymyxin B sulfate Usage And Synthesis
- IndicationsPolymyxin 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.
- Dosage1. 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 InteractionsWe 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 chemicalbook of Dai Xiongfeng.
- Injection polymyxin B sulfate manufacturerShanghai “Xin Xianfeng” Pharmaceutical Co., Ltd. Zhunzi H31022973
Shanghai No. 1 Biochemical Pharmaceutical Co., Ltd. Zhunzi H31022631
- Precautions1. 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.
- UsesBiochemical 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.
- Chemical PropertiesWhite Solid
- UsesAntibiotic 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.
- UsesPolymyxin B sulfate is used as topical antibiotic agent, often used in combination with neomycin; products include ointments, creams, eye, and ear drops.
- IndicationsPolymyxin 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.
- brand name(GlaxoSmithKline); Poly-Rx (X Gen).
- General DescriptionPolymyxin (Aerosporin) was discovered in 1947 almost simultaneouslyin three separate laboratories in the UnitedStates and Great Britain. As often happens whensimilar discoveries are made in widely separated laboratories,differences in nomenclature, referring to both theantibiotic-producing organism and the antibiotic itself, appearedin references to the polymyxins. Because the organismsfirst designated as Bacillus polymyxa and B.aerosporus Greer were found to be identical species, thename B. polymyxa is used to refer to all of the strains thatproduce the closely related polypeptides called polymyxins.Other organisms (e.g., see “Colistin” later) also producepolymyxins. Identified so far are polymyxins A, B1,B2, C, D1, D2, M, colistin A (polymyxin E1), colistin B(polymyxin E2), circulins A and B, and polypeptin. Theknown structures of this group and their properties havebeen reviewed by Vogler and Studer. Of these,polymyxin B as the sulfate usually is used in medicine because,when used systemically, it causes less kidney damagethan the others. Polymyxin B sulfate is a nearly odorless, white to buff powder. It is freely soluble in water and slightly soluble in alcohol.
- Clinical UsePolymyxin 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.
- polymyxin B-sepharose Polymyxin B Sulfate (1.06994),Polymyxin B Sulfate (1.06994) Polymyxin B heptapeptide POLYMYXIN B SULFATE N/H Polymyxin S1 Polymyxin T1 Polymyxin B Sulfate bacitracin zinc,Polymyxin B Sulfate bacitracin zinc Polymyxin E1 Polymyxin B-sulfate solution,Polymyxin B-sulfate solution Benzyl sulfate Benzyl isocyanate Benzyl nicotinate GOLD COAST SOLUTION NO 1 CHONDROITIN SULFATE B SODIUM SALT polymyxin B 2.5sulfate entahydrate,Polymyxin B (base and/or unspecified salts) Polymyxin BENZYL ISOCYANIDE
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