Suppr超能文献

[大环内酯类、酮内酯类和链阳菌素类]

[Macrolides, ketolides and streptogramins].

作者信息

Mensa José, García-Vázquez Elisa, Vila Jordi

机构信息

Instituto Clínico de Infecciones e Inmunología. Hospital Clínic. Barcelona. España.

出版信息

Enferm Infecc Microbiol Clin. 2003 Apr;21(4):200-7; quiz 208, 219.

Abstract

Macrolides, ketolides and streptogramins are three families of antibiotics with different chemical structures, sharing the same mechanism of action. All three bind to distinct bases of the peptidyl transferase center of ARNr 23S. Their antibacterial spectrum practically overlaps, but dissimilarities in affinity and/or number of binding sites determine differences in the intensity of their antibacterial effects (bacteriostatic or bactericidae) and in their activity against strains with acquired resistance mechanisms. These agents are active against the majority of gram-positive microorganisms and many intracellular microorganisms for growth. Over the last five years in our country, the percentage of macrolide-resistant pneumococci and S. pyogenes strains has increased substantially. Telithromycin (ketolide) and Synercid (streptogramin) have shown maintained activity against these strains. Macrolides, ketolides and streptogramins are metabolized in the liver through CYP 3A4 and they can partially block the activity of the enzyme, interfering with the metabolism of other drugs that use the same metabolic pathway. There is little elimination through the urine, with the exception of clarithromycin. High concentrations are reached in the cellular cytoplasm, but they do not diffuse to the CSF. These agents are included among class B drugs for use during pregnancy. Tolerance to macrolides and telithromycin is good and they have few associated adverse effects. The main clinical indication for these drugs is in empirical treatment of mild to moderate, community-acquired, upper and lower respiratory tract infections. Synercid is indicated in the treatment of infections due to methicillin-resistant staphylococci and glycopeptide-resistant enterococci.

摘要

大环内酯类、酮内酯类和链阳菌素类是三类化学结构不同但作用机制相同的抗生素。这三类抗生素均与23S核糖体RNA肽基转移酶中心的不同碱基结合。它们的抗菌谱几乎重叠,但亲和力和/或结合位点数量的差异决定了它们抗菌作用强度(抑菌或杀菌)以及对具有获得性耐药机制菌株的活性的差异。这些药物对大多数革兰氏阳性微生物和许多细胞内生长的微生物具有活性。在我国过去五年中,对大环内酯类耐药的肺炎球菌和化脓性链球菌菌株的比例大幅上升。泰利霉素(酮内酯类)和达托霉素(链阳菌素类)对这些菌株仍保持活性。大环内酯类、酮内酯类和链阳菌素类在肝脏中通过细胞色素P450 3A4代谢,它们可部分阻断该酶的活性,干扰使用相同代谢途径的其他药物的代谢。除克拉霉素外,经尿液排泄很少。在细胞质中可达到高浓度,但它们不会扩散到脑脊液中。这些药物属于B类妊娠用药。对大环内酯类和泰利霉素的耐受性良好,且相关不良反应较少。这些药物的主要临床适应证是对轻至中度社区获得性上、下呼吸道感染进行经验性治疗。达托霉素适用于治疗耐甲氧西林葡萄球菌和耐糖肽肠球菌引起的感染。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验