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关注β-内酰胺类抗生素

[Focus on beta-lactam antibiotics].

作者信息

Cometta A, Glauser M P

机构信息

Division des maladies infectieuses, Centre hospitalier universitaire vaudois, Lausanne.

出版信息

Schweiz Med Wochenschr. 1988 Dec 10;118(49):1817-22.

PMID:3064289
Abstract

The beta-lactams are mainly active on the bacterial cell wall. Although it was long claimed that their clinical efficacy was due to the bactericidal effect observed in vitro, it is now demonstrated that this effect cannot be the sole explanation for the therapeutic successes noted with these antibiotics in clinical situations. Several effects other than bactericidal are observed at subinhibitory concentrations and allow a better understanding of the activity of the beta-lactams. These are, among others, inhibition of bacterial growth, the post-antibiotic effect, the morphological effect, loss of virulent factors and decrease of adherence. --Following recent developments in the field of the beta-lactams, the new antibiotics exhibit a major broadening of their microbiological spectrum that in some cases allows simplification of antibiotic therapy: in some clinical situations monotherapy can be used instead of a combination. Some antibiotics have very good pharmacokinetic properties, allowing once-a-day dosage and outpatient treatment. --Finally, adverse drug effects such as neutropenia, hitherto considered infrequent, have been recognized more often. Explanation of their physiopathological mechanisms could favour the development of less toxic antibiotics.

摘要

β-内酰胺类药物主要作用于细菌细胞壁。尽管长期以来人们认为它们的临床疗效归因于体外观察到的杀菌作用,但现在已证明这种作用不能完全解释这些抗生素在临床情况下取得的治疗成功。在亚抑菌浓度下还观察到了除杀菌作用之外的其他几种作用,这有助于更好地理解β-内酰胺类药物的活性。其中包括抑制细菌生长、抗生素后效应、形态学效应、毒力因子丧失以及黏附性降低。——随着β-内酰胺类药物领域的最新进展,新型抗生素的微生物谱有了很大拓宽,在某些情况下可简化抗生素治疗:在一些临床情况下可采用单一疗法而非联合疗法。一些抗生素具有非常好的药代动力学特性,允许每日一次给药和门诊治疗。——最后,诸如中性粒细胞减少等不良药物反应,以往认为并不常见,现在却更常被认识到。对其生理病理机制的解释可能有助于开发毒性更小的抗生素。

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