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泰利霉素:首个用于治疗社区获得性呼吸道感染的酮内酯类抗菌药物。

Telithromycin: the first ketolide antibacterial for the treatment of community-acquired respiratory tract infections.

作者信息

Lorenz J

机构信息

Medical Department, Lüdenscheid General Hospital, Germany.

出版信息

Int J Clin Pract. 2003 Jul-Aug;57(6):519-29.

Abstract

Telithromycin is the first ketolide antibacterial to be approved for clinical use. The ketolides represent a novel class of antibacterial agents structurally related to the macrolides, which has been developed specifically to offer an optimal spectrum for the treatment of upper and lower respiratory tract infections (RTIs) caused by common and atypical pathogens, including strains that are resistant to currently used antibiotics. The innovative structural changes that distinguish telithromycin from macrolides contribute to its unique microbiological profile. Its well-balanced spectrum of antibacterial activity is highly appropriate for the empirical treatment of upper and lower community-acquired RTIs, offering activity against common, including resistant, and atypical/intracellular pathogens. Furthermore, telithromycin demonstrates a low propensity to select for or induce resistance to macrolide-lincosamide-streptogramin antibacterials. A once-daily dose of telithromycin 800 mg rapidly achieves high concentrations in both plasma and respiratory tissues and fluids and is maintained at effective levels throughout the 24-hour dosing period. In clinical trials, telithromycin has demonstrated high clinical and bacteriological efficacy in the treatment of community-acquired pneumonia, acute exacerbations of chronic bronchitis, acute sinusitis and group A beta-haemolytic streptococcal tonsillitis/pharyngitis. High efficacy was maintained in those patient groups considered to be at high risk of complications and those with infections caused by penicillin and/or macrolide (erythromycin) resistant Streptococcus pneumoniae. Together with its favourable tolerability profile and short course of once-daily therapy, these properties indicate that telithromycin will be a valuable new antibacterial for the empirical treatment of community-acquired RTIs.

摘要

泰利霉素是首个被批准用于临床的酮内酯类抗菌药物。酮内酯类是一类结构上与大环内酯类相关的新型抗菌剂,专门开发用于为治疗由常见和非典型病原体引起的上、下呼吸道感染(RTIs)提供最佳抗菌谱,包括对目前使用的抗生素耐药的菌株。使泰利霉素区别于大环内酯类的创新性结构变化促成了其独特的微生物学特性。其抗菌活性谱平衡良好,非常适合社区获得性上、下呼吸道感染的经验性治疗,对常见病原体(包括耐药病原体)以及非典型/细胞内病原体均有活性。此外,泰利霉素不易选择或诱导对大环内酯-林可酰胺-链阳菌素类抗菌药物产生耐药性。每日一次服用800mg泰利霉素可迅速在血浆以及呼吸道组织和体液中达到高浓度,并在整个24小时给药期间维持在有效水平。在临床试验中,泰利霉素在治疗社区获得性肺炎、慢性支气管炎急性加重、急性鼻窦炎以及A组β溶血性链球菌扁桃体炎/咽炎方面已显示出高临床疗效和细菌学疗效。在那些被认为有高并发症风险的患者群体以及由对青霉素和/或大环内酯类(红霉素)耐药的肺炎链球菌引起感染的患者中,也维持了高疗效。连同其良好的耐受性和每日一次的短疗程治疗,这些特性表明泰利霉素将成为社区获得性呼吸道感染经验性治疗中有价值的新型抗菌药物。

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