Moellering R C
New England Deaconess Hospital, Boston, Massachusetts 02215.
J Antimicrob Chemother. 1993 Jan;31 Suppl A:1-8. doi: 10.1093/jac/31.suppl_a.1.
A wide variety of beta-lactamases are found in clinical isolates of bacteria and, when present, these enzymes often result in resistance to one or more beta-lactam antibiotics. The prevalence of organisms with these enzymes has increased as beta-lactams have been increasingly used in clinical practice. This paper defines the nature of these enzymes and details the attempts to overcome the problem of resistance mediated by beta-lactamase, efforts which have culminated in the development of a series of effective beta-lactamase inhibitors which can be combined with beta-lactam antibiotics. The currently available compounds, clavulanic acid, sulbactam, and tazobactam are very effective inhibitors of many types of beta-lactamases, but there are additional enzymes which are resistant even to these inhibitors and which pose continuing challenges for the pharmaceutical chemist and clinician alike.
在临床分离的细菌中发现了各种各样的β-内酰胺酶，一旦存在，这些酶通常会导致对一种或多种β-内酰胺抗生素产生耐药性。随着β-内酰胺类药物在临床实践中的使用日益增加，携带这些酶的生物体的流行率也有所上升。本文阐述了这些酶的性质，并详细介绍了为克服由β-内酰胺酶介导的耐药性问题所做的努力，这些努力最终促成了一系列可与β-内酰胺抗生素联合使用的有效β-内酰胺酶抑制剂的开发。目前可用的化合物，克拉维酸、舒巴坦和他唑巴坦是许多类型β-内酰胺酶的非常有效的抑制剂，但仍有其他酶甚至对这些抑制剂具有抗性，这给药物化学家及临床医生都带来了持续的挑战。
