Bearden D T, Neuhauser M M, Garey K W
Department of Pharmacy Practice, Albany College of Pharmacy, New York, USA.
Pharmacotherapy. 2001 Oct;21(10):1204-22. doi: 10.1592/phco.21.15.1204.33902.
The ketolides represent a new subclass of antibiotics among the macrolide-lincosamide-streptogramin group. Telithromycin, the first ketolide to be awarded approvable status for clinical use, demonstrates in vitro activity against community-acquired respiratory pathogens including penicillin- and erythromycin-resistant Streptococcus pneumoniae. An extended half-life permits once-daily oral administration. Telithromycin is a substrate for cytochrome P450 (CYP) 3A4 and also inhibits drugs metabolized by CYP3A4. A relatively high frequency of mild-to-moderate gastrointestinal adverse effects has been reported. Similar clinical and microbiologic efficacy has been demonstrated with oral dosing in comparative clinical trials for community-acquired pneumonia, acute sinusitis, acute exacerbations of chronic bronchitis, and pharyngitis. Although limited data on penicillin-resistant S. pneumoniae and erythromycin-resistant Streptococcus pyogenes are available from clinical trials, this drug appears promising for respiratory infections caused by these pathogens.
酮内酯类抗生素是大环内酯-林可酰胺-链阳菌素类抗生素中的一个新亚类。泰利霉素是首个获得临床使用批准地位的酮内酯类抗生素,它在体外对社区获得性呼吸道病原体具有活性,包括对青霉素和红霉素耐药的肺炎链球菌。其较长的半衰期允许每日一次口服给药。泰利霉素是细胞色素P450(CYP)3A4的底物,并且还抑制由CYP3A4代谢的药物。据报道,其轻度至中度胃肠道不良反应的发生率相对较高。在社区获得性肺炎、急性鼻窦炎、慢性支气管炎急性加重和咽炎的比较临床试验中,口服给药已证明具有相似的临床和微生物学疗效。虽然临床试验中关于耐青霉素肺炎链球菌和耐红霉素化脓性链球菌的数据有限,但这种药物对于由这些病原体引起的呼吸道感染似乎很有前景。