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羟羧氧酰胺菌素、头孢噻肟、头孢哌酮和头孢曲松在实验性细菌性脑膜炎中的药代动力学及细菌学疗效

Pharmacokinetics and bacteriologic efficacy of moxalactam, cefotaxime, cefoperazone, and rocephin in experimental bacterial meningitis.

作者信息

Schaad U B, McCracken G H, Loock C A, Thomas M L

出版信息

J Infect Dis. 1981 Feb;143(2):156-63. doi: 10.1093/infdis/143.2.156.

Abstract

The pharmacokinetics and bacteriologic efficacy of four beta-lactam antibiotics were studied in the serum and cerebrospinal fluid (CSF) of rabbits using two test strains, Escherichia coli type K1 and group B Streptococcus type III, and 24 gram-positive isolates. Although moxalactam, cefotaxime, cefoperazone, and rocephin are active in vitro against gram-negative bacilli, the gram-positive bacteria Listeria monocytogenes and Streptococcus faecalis were resistant to all four drugs; group B streptococci were resistant to moxalactam. In rabbit CSF, moxalactam had the greatest concentration and penetration, but rocephin had the longest half-life and duration of bactericidal activity. These two drugs were most effective in the CSF of E. coli K1-infected rabbits. Except for moxalatam, the four drugs were comparable to ampicillin in reducing counts of group B Streptococcus type III in CSF. Drug accumulation in CSF and appreciable bacterial killing were observed in E. coli K1-infected animals give moxalactam either periodically or by constant infusion.

摘要

使用两种测试菌株(K1型大肠杆菌和III型B组链球菌)以及24株革兰氏阳性分离株,在兔的血清和脑脊液(CSF)中研究了四种β-内酰胺抗生素的药代动力学和细菌学疗效。尽管羟羧氧酰胺菌素、头孢噻肟、头孢哌酮和头孢曲松在体外对革兰氏阴性杆菌有活性,但革兰氏阳性菌单核细胞增生李斯特菌和粪肠球菌对所有四种药物均耐药;B组链球菌对羟羧氧酰胺菌素耐药。在兔脑脊液中,羟羧氧酰胺菌素浓度和渗透率最高,但头孢曲松半衰期最长,杀菌活性持续时间最长。这两种药物在感染K1型大肠杆菌的兔脑脊液中最有效。除羟羧氧酰胺菌素外,这四种药物在降低脑脊液中III型B组链球菌数量方面与氨苄西林相当。在感染K1型大肠杆菌的动物中,定期或持续输注羟羧氧酰胺菌素后,观察到脑脊液中有药物蓄积和明显的细菌杀灭作用。

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