Telithromycin
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Telithromycin is an ketolide used to treat community acquired pneumonia of mild to moderate severity.
Telithromycin is an ketolide used to treat community acquired pneumonia of mild to moderate severity.
Telithromycin acts by binding to domains II and V of 23S rRNA of the 50S ribosomal subunit. By binding at domain II, telithromycin retains activity against gram-positive cocci (e.g. Streptococcus pneumoniae) in the presence of resistance mediated by methylases (erm genes) that alter the binding site at domain V. Telithromycin may also inhibit the assembly of nascent ribosomal units. Compared to erythromycin A, telithromycin binds to the 23S rRNA with 10 times greater affinity in erythromycin-susceptible organisms and 25 times greater affinity in macrolide-resistant strains. This increased binding affinity may be conferred by the C11-12 carbamate side chain of telithromycin. The side chain appears to maintain binding at domain II in the presence of resistance mediated by alterations in domain V.
临床主要用于敏感菌所致的呼吸道感染，包括社区获得性肺炎、慢性支气管炎、急性上颌窦咽炎及扁桃体炎。
