Telithromycin: A Ketolide Antibiotic for Treatment of Respiratory Tract Infections

• Published in: Clinical infectious diseases 2005-06, Vol.40 (11), p.1657-1664
• Main Authors: Lonks, John R., Goldmann, Donald A.
• Format: Article
• Language: English
• Subjects: Anti-Bacterial Agents - pharmacokinetics; Anti-Bacterial Agents - pharmacology; Anti-Bacterial Agents - therapeutic use; Antibacterial agents; Antibiotics; Antibiotics. Antiinfectious agents. Antiparasitic agents; Biological and medical sciences; Chlamydophila pneumoniae; Chronic obstructive pulmonary disease, asthma; Comparators; Dosage; Drug Interactions; Drug Resistance, Bacterial; Drug therapy; FDA approval; Haemophilus influenzae; Humans; Ketolides; Ketolides - pharmacokinetics; Ketolides - pharmacology; Ketolides - therapeutic use; Macrolides; Medical sciences; Moraxella catarrhalis; Mycoplasma pneumoniae; Non tumoral diseases; Otorhinolaryngology (head neck, general aspects and miscellaneous); Otorhinolaryngology. Stomatology; Pathogens; Pharmacology. Drug treatments; Pneumococcal pneumonia; Pneumology; Pneumonia; Respiratory diseases; Respiratory Tract Infections - drug therapy; Respiratory Tract Infections - microbiology; Reviews of Anti-Infective Agents; Sinusitis; Streptococcus pneumoniae; Structure-Activity Relationship
• ISSN: 1058-4838; 1537-6591
• DOI: 10.1086/430067

Telithromycin, a recently approved ketolide antibiotic derived from 14-membered macrolides, is active against erythromycin-resistant pneumococci. Telithromycin has enhanced activity in vitro because it binds not only to domain V of ribosomal RNA (like macrolides do) but also to domain II. However, it is not active against streptococci and staphylococci with constitutive macrolide, lincosamide, and streptogramin B resistance. Telithromycin, available in an oral formulation, is approved by the US Food and Drug Administration for use in adults for treatment of (1) community-acquired pneumonia due to Streptococcus pneumoniae (including multidrug-resistant isolates), Haemophilus influenzae, Moraxella catarrhalis, Chlamydia pneumoniae, or Mycoplasma pneumoniae; (2) acute exacerbation of chronic bronchitis due to S. pneumoniae, H. influenzae, or M. catarrhalis; or (3) acute bacterial sinusitis due to S. pneumoniae, H. influenzae, M. catarrhalis, or methicillin- and erythromycin-susceptible Streptococcus aureus. It is not approved for treatment of tonsillitis, pharyngitis, or severe pneumococcal pneumonia. Unique visual adverse effects occurred in 0.27%–2.1% of patients receiving telithromycin therapy. Its enhanced activity against some common respiratory pathogens makes it a valuable addition to the available macrolides.