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SCE - 129,抗假单胞菌头孢菌素:体外和体内抗菌活性

SCE-129, antipseudomonal cephalosporin: in vitro and in vivo antibacterial activities.

作者信息

Tsuchiya K, Kondo M, Nagatomo H

出版信息

Antimicrob Agents Chemother. 1978 Feb;13(2):137-45. doi: 10.1128/AAC.13.2.137.

Abstract

SCE-129 [3-(4-carbamoyl-1-pyridiniomethyl)-7beta-(d-alpha-sulfophenylacetamido)-ceph-3-em-4-carboxylate monosodium salt], a new semisynthetic cephalosporin, shows potent in vitro antibacterial activities against Pseudomonas aeruginosa and some gram-positive bacteria, whereas it shows lower activity against many gram-negative rods. Against clinical isolates of P. aeruginosa this cephalosporin exhibited higher activity than did carbenicillin, and against the strains of Staphylococcus aureus, SCE-129 had similar activity to carbenicillin. Variations in pH, addition of horse serum, and type of growth medium had no significant effects on the activity of the cephalosporin; however, the inoculum size had some effect on the activity. SCE-129 is an effective bactericidal agent against P. aeruginosa and S. aureus. The protective effects of SCE-129 in mice infected with P. aeruginosa and S. aureus were more potent than those of carbenicillin. The protective effects of SCE-129 on Pseudomonas infection in mice varied according to the dosage schedule and the challenge dose. In a multiple dose schedule, a smaller amount of SCE-129 was necessary than that in a single dose schedule. The effects of SCE-129 after subcutaneous or intraperitoneal administration were more potent than were those by intravenous administration. No protective effect was observed by oral administration.

摘要

SCE - 129[3 - (4 - 氨甲酰基 - 1 - 吡啶甲基)-7β-(d-α - 磺基苯乙酰氨基)-头孢 - 3 - 烯 - 4 - 羧酸钠盐],一种新型半合成头孢菌素,对铜绿假单胞菌和一些革兰氏阳性菌显示出强大的体外抗菌活性,而对许多革兰氏阴性杆菌活性较低。针对铜绿假单胞菌的临床分离株,这种头孢菌素表现出比羧苄西林更高的活性,而针对金黄色葡萄球菌菌株,SCE - 129与羧苄西林具有相似的活性。pH值的变化、马血清的添加以及生长培养基的类型对头孢菌素的活性没有显著影响;然而,接种量对活性有一定影响。SCE - 129是一种针对铜绿假单胞菌和金黄色葡萄球菌的有效杀菌剂。SCE - 129对感染铜绿假单胞菌和金黄色葡萄球菌的小鼠的保护作用比羧苄西林更强。SCE - 129对小鼠铜绿假单胞菌感染的保护作用根据给药方案和攻击剂量而有所不同。在多剂量方案中,所需的SCE - 129量比单剂量方案中的要少。皮下或腹腔注射SCE - 129后的效果比静脉注射更强。口服给药未观察到保护作用。

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