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头孢西丁,一种半合成头孢霉素类抗生素:体内评价

Cefoxitin, a semisynthetic cephamycin antibiotic: in vivo evaluation.

作者信息

Miller A K, Celozzi E, Kong Y, Pelak B A, Hendlin D, Stapley E O

出版信息

Antimicrob Agents Chemother. 1974 Jan;5(1):33-7. doi: 10.1128/AAC.5.1.33.

Abstract

Cefoxitin, 3-carbamoyloxymethyl-7-alpha-methoxy-7-[2-(2-thienyl)acetamido]-3-cephem-4- carboxylic acid, a semisynthetic cephamycin antibiotic shown to have broad-spectrum activity in vitro, is active also in vivo against a wide variety of bacteria including penicillin-resistant staphylococci. It is, however, particularly effective against gram-negative organisms including strains of indole-positive Proteus against which cephalothin and cephaloridine are ineffective. When cefoxitin is given subcutaneously, concentrations in mouse blood, urine, and other tissues are higher than those seen for cephalothin. Higher concentrations in the blood and greater therapeutic efficacy are achieved with cefoxitin when it is given with probenecid. For this reason it is believed that cefoxitin is excreted mainly by way of the renal tubules. The data indicate that cefoxitin has potential as a therapeutically useful antibiotic.

摘要

头孢西丁,即3-氨甲酰氧甲基-7-α-甲氧基-7-[2-(2-噻吩基)乙酰胺基]-3-头孢烯-4-羧酸,是一种半合成头孢霉素抗生素,体外显示具有广谱活性,体内对多种细菌也有活性,包括耐青霉素葡萄球菌。然而,它对革兰氏阴性菌特别有效,包括吲哚阳性变形杆菌菌株,而头孢噻吩和头孢匹林对这些菌株无效。当皮下注射头孢西丁时,小鼠血液、尿液和其他组织中的浓度高于头孢噻吩。当与丙磺舒合用时,头孢西丁在血液中浓度更高,治疗效果更好。因此,据信头孢西丁主要通过肾小管排泄。数据表明头孢西丁有作为治疗用抗生素的潜力。

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