Telithromycin (HMR 3647) achieves high and sustained concentrations in tonsils of patients undergoing tonsillectomy.
Telithromycin, the first ketolide antimicrobial to be developed for clinical use, has potent activity against group A beta-haemolytic streptococci (GABHS), including macrolide-resistant strains. The penetration of telithromycin into tonsils was assessed in 22 adults undergoing tonsillectomy at 3, 12 or 24 h after the fourth dose of oral telithromycin 800 mg once daily. Telithromycin rapidly penetrated tonsillar tissues, achieving a mean concentration of 3.95 mg/kg at 3 h post dose, 3.4 times greater than the corresponding plasma concentration (1.22 mg/l. The mean tonsil:plasma concentration ratio increased to 13.1 at 24 h post dose, indicating slower elimination from tonsils than plasma. Tonsillar and plasma concentrations exceeded the MIC(50) for GABHS throughout the 24-h dosing period. These findings suggest that telithromycin may be an effective new alternative treatment for GABHS tonsillopharyngitis.
Hôpital Bichat-Claude Bernard, 46 rue Henri Huchard, Paris, France. pierre.gehanno@bch.ap-hop-paris.fr
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Gehanno
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Sultan
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Passot
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Nabet
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Danon
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Romanet
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Attal
D000284:Administration, Oral; D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D048628:Ketolides; D018942:Macrolides; D008297:Male; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D014066:Palatine Tonsil / Q000378:metabolism* / Q000601:surgery*; D013297:Streptococcus pyogenes / Q000187:drug effects; D014068:Tonsillectomy
D000900:Anti-Bacterial Agents; D048628:Ketolides; D018942:Macrolides; C106791:telithromycin