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美罗培南与亚胺培南-西司他丁在年轻健康男性中的药代动力学比较。

Pharmacokinetics of meropenem compared to imipenem-cilastatin in young, healthy males.

作者信息

Nilsson-Ehle I, Hutchison M, Haworth S J, Norrby S R

机构信息

Department of Infectious Diseases, University Hospital, Lund, Sweden.

出版信息

Eur J Clin Microbiol Infect Dis. 1991 Feb;10(2):85-8. doi: 10.1007/BF01964413.

Abstract

Imipenem combined with cilastatin and meropenem was given as intravenous infusions of 1 g to eight young, healthy males on two separate occasions. Blood and urine samples were collected for up to 12 h. The terminal half-lives in plasma were 0.98 h and 1.11 h for meropenem and imipenem, respectively. The volume of distribution was smaller for meropenem than for imipenem (12.5 l and 14.4 l, respectively). The plasma clearance for meropenem was 188 (SD 31) ml/min and for imipenem 183 (SD 25) ml/min. Renal clearance was on average 139 (SD 24) ml/min and 135 (SD 11) ml/min, respectively. About 75% of the administered dose of both compounds was eliminated unchanged in urine. Non-renal clearance accounted for approximately 25% of the total clearance for both drugs. The kinetics of meropenem are very similar to those of imipenem given with cilastatin, and meropenem is as stable against renal metabolic degradation as imipenem combined with cilastatin.

摘要

亚胺培南与西司他丁联合应用以及美罗培南,分别在两个不同时间以静脉输注1g的剂量给予8名年轻健康男性。采集血样和尿样长达12小时。美罗培南和亚胺培南在血浆中的终末半衰期分别为0.98小时和1.11小时。美罗培南的分布容积比亚胺培南小(分别为12.5升和14.4升)。美罗培南的血浆清除率为188(标准差31)毫升/分钟,亚胺培南为183(标准差25)毫升/分钟。肾脏清除率平均分别为139(标准差24)毫升/分钟和135(标准差11)毫升/分钟。两种化合物给药剂量的约75%以原形经尿液排出。非肾脏清除率约占两种药物总清除率的25%。美罗培南的动力学与亚胺培南联合西司他丁给药时非常相似,并且美罗培南与亚胺培南联合西司他丁一样对肾脏代谢降解稳定。

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