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新型头孢菌素头孢匹胺的实验疗效及药代动力学特性

Experimental efficacy and pharmacokinetic properties of cefpiramide, a new cephalosporin.

作者信息

Fu K P, Vince T, McCloud S, Gregory F J, Chiang S T, Hung P P

出版信息

Drugs Exp Clin Res. 1985;11(11):787-91.

PMID:3939215
Abstract

The in vivo therapeutic efficacy of cefpiramide was investigated and compared with that of cefoperazone. Cefpiramide was more potent than cefoperazone against infections produced by both beta-lactamase-producing and non-beta-lactamase-producing S. aureus. The protective activity of cefpiramide against experimental infections with selected members of Enterobacteriaceae was lower than that of cefoperazone. Against carbenicillin-resistant P. aeruginosa infections, cefpiramide was as active as gentamicin and aztreonam and three times more potent than cefoperazone, cefotaxime and piperacillin. The pharmacokinetic properties of cefpiramide in mice and rats were superior to those of cefotaxime and cefoperazone. The peak serum concentrations of cefpiramide, administered subcutaneously at a dose of 50 mg/kg, were 76 micrograms/ml in mice and 174 micrograms/ml in rats and the corresponding serum half-lives of cefpiramide were 87 min and 49 min in mice and rats respectively.

摘要

对头孢匹胺的体内治疗效果进行了研究,并与头孢哌酮进行了比较。头孢匹胺对产β-内酰胺酶和不产β-内酰胺酶的金黄色葡萄球菌感染的效力均强于头孢哌酮。头孢匹胺对所选肠杆菌科细菌实验性感染的保护活性低于头孢哌酮。对于耐羧苄西林的铜绿假单胞菌感染,头孢匹胺的活性与庆大霉素和氨曲南相当,且效力是头孢哌酮、头孢噻肟和哌拉西林的三倍。头孢匹胺在小鼠和大鼠体内的药代动力学特性优于头孢噻肟和头孢哌酮。以50mg/kg的剂量皮下给药时,头孢匹胺在小鼠体内的血清峰值浓度为76微克/毫升,在大鼠体内为174微克/毫升,头孢匹胺在小鼠和大鼠体内相应的血清半衰期分别为87分钟和49分钟。

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