Felmingham D
GR Micro Ltd, London, UK.
Clin Microbiol Infect. 2001;7 Suppl 3:2-10.
Telithromycin, the first of the ketolide antimicrobials, has been specifically designed to provide potent activity against common and atypical/intracellular or cell-associated respiratory pathogens, including those that are resistant to beta-lactams and/or macrolide-lincosamide-streptograminB (MLS(B)) antimicrobials. Against gram-positive cocci, telithromycin possesses more potent activity in vitro and in vivo than the macrolides clarithromycin and azithromycin. It retains its activity against erm-(MLS(B)) or mef-mediated macrolide-resistant Streptococcus pneumoniae and Streptococcus pyogenes and against Staphylococcus aureus resistant to macrolides through inducible MLS(B) mechanisms. Telithromycin also possesses high activity against the Gram-negative pathogens Haemophilus influenzae and Moraxella catarrhalis, regardless of beta-lactamase production. In vitro, it shows similar activity to azithromycin against H. influenzae, while in vivo its activity against H. influenzae is higher than that of azithromycin. Telithromycin's spectrum of activity also extends to the atypical, intracellular and cell-associated pathogens Legionella pneumophila, Mycoplasma pneumoniae and Chlamydia pneumoniae. In vitro, telithromycin does not induce MLS(B) resistance and it shows low potential to select for resistance or cross-resistance to other antimicrobials. These characteristics indicate that telithromycin will have an important clinical role in the empirical treatment of community-acquired respiratory tract infections.
泰利霉素是首个酮内酯类抗菌药物，其设计初衷是对常见的以及非典型/细胞内或与细胞相关的呼吸道病原体具有强大活性，包括那些对β-内酰胺类和/或大环内酯-林可酰胺-链阳菌素B（MLS(B)）抗菌药物耐药的病原体。在体外和体内，泰利霉素对革兰氏阳性球菌的活性比克拉霉素和阿奇霉素等大环内酯类药物更强。它对erm-(MLS(B))或mef介导的大环内酯耐药肺炎链球菌和化脓性链球菌以及通过诱导型MLS(B)机制对大环内酯耐药的金黄色葡萄球菌仍保持活性。泰利霉素对革兰氏阴性病原体流感嗜血杆菌和卡他莫拉菌也具有高活性，无论其是否产生β-内酰胺酶。在体外，它对流感嗜血杆菌的活性与阿奇霉素相似，而在体内，它对流感嗜血杆菌的活性高于阿奇霉素。泰利霉素的活性谱还扩展到非典型、细胞内和与细胞相关的病原体嗜肺军团菌、肺炎支原体和肺炎衣原体。在体外，泰利霉素不会诱导MLS(B)耐药，并且它产生对其他抗菌药物耐药或交叉耐药的可能性较低。这些特性表明，泰利霉素在社区获得性呼吸道感染的经验性治疗中将发挥重要的临床作用。
