ポリミキシンB/硫酸 化学特性,用途語,生産方法
外観
白色〜黄褐色, 粉末
溶解性
水に溶けやすく、エタノールに極めて溶けにくく、エーテルにほとんど溶けない。水に溶ける。
用途
ポリミキシン系抗菌剤です。
細菌細胞質膜の透過性を変化させることによ
り、抗菌作用を示します。緑膿菌、肺炎桿菌
といったグラム陰性桿菌に対して、優れた抗
菌作用を示します。
用途
薬理研究用。
効能
抗生物質, 細胞膜機能阻害薬
商品名
硫酸ポリミキシンB (ファイザー); 硫酸ポリミキシンB (ファイザー); 硫酸ポリミキシンB (ファイザー)
説明
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 B
1 to B
4, with polymyxin B
1 and B
2 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.
化学的特性
White Solid
使用
Polymyxin B sulfate is used as topical antibiotic agent, often used in combination with neomycin; products include ointments, creams, eye, and ear drops.
適応症
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.
一般的な説明
Polymyxin (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.
臨床応用
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.
ポリミキシンB/硫酸 上流と下流の製品情報
原材料
準備製品