区分美罗培南和亚胺培南的实验室数据。

J R Edwards, P J Turner
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引用次数: 0

摘要

美罗培南和亚胺培南是碳青霉烯类,通过抗菌谱的宽度和对β -内酰胺酶的稳定性与所有其他现有的β -内酰胺类抗生素区分开来,但可以相互区分。美罗培南对人肾脱氢肽酶i (DHP-I)相对稳定;它不需要与西司他汀共同使用,因此,与亚胺培南不同,它将作为单一药物使用。在体外,美罗培南和亚胺培南对几乎所有临床重要的好氧和厌氧细菌都有活性。药效差异可见,但可能很少有临床意义:亚胺培南对肠球菌更有活性,美罗培南对铜绿假单胞菌、洋葱假单胞菌、流感嗜血杆菌和变形杆菌、摩根菌和普罗维登西亚菌更有活性。亚胺培南在铜绿假单胞菌中的主要靶点是PBP2,而美罗培南对PBP2和pb3均有较高的亲和力;这可能有助于提高对抗这种有机体的效力。实验室评估预测美罗培南不会引起癫痫,结合对可能病原体的活性,确定了其治疗细菌性脑膜炎的潜力。这已经在豚鼠模型中进行了研究,在该模型中,美罗培南对常见的脑膜病原体和由耐青霉素肺炎链球菌或单核细胞增生李斯特菌引起的感染表现出强有力的活性。临床经验将决定这些差异的意义。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Laboratory data which differentiate meropenem and imipenem.

Meropenem and imipenem are carbapenems which are distinguishable from all other currently available beta-lactam antibiotics by breadth of antibacterial spectrum and stability to beta-lactamases, but can be differentiated one from another. Meropenem is relatively stable to human renal dehydropeptidase-I (DHP-I); it does not require to be co-administered with cilastatin and consequently, unlike imipenem, will be administered as a single agent. In vitro both meropenem and imipenem are active against almost all clinically important aerobic and anaerobic bacteria. Differences in potency are seen but few may be of clinical significance: imipenem is more active against enterococci and meropenem is more active against Pseudomonas aeruginosa, Pseudomonas cepacia, Haemophilus influenzae and Proteus, Morganella and Providencia species. The primary target of imipenem is PBP2 in P. aeruginosa whilst meropenem has high affinity for both PBP2 and 3; this may contribute to greater potency against this organism. Laboratory evaluations predict that meropenem will not be seizurogenic, which combined with activity against likely pathogens, identified its potential for the treatment of bacterial meningitis. This has been investigated in a guinea-pig model in which meropenem exhibited potent activity against the common meningeal pathogens and also infections caused by penicillin-resistant Streptococcus pneumoniae or Listeria monocytogenes. Clinical experience will determine the significance of these differences.

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