title: Antituberculosis activity of clarithromycin.
abstract: Antituberculosis activity of clarithromycin (CLA), a macrolide antibiotic, was investigated in vitro, in macrophages, and in C57BL/6 mice, CLA showed high in vitro MICs (4 to > 16 micrograms/ml) for several strains of Mycobacterium tuberculosis and caused slight enhancement of activity of rifampin (RIF) against H37Rv but failed to increase the activity of either RIF or isoniazid (INH) against other strains. However, inside J774A.1 macrophages, CLA showed high activity and was synergistic with RIF against some strains of tubercle bacilli susceptible or resistant to INH and RIF. In the in vivo studies with a drug-susceptible strain (H37Rv), CLA protected mice from mortality due to tuberculosis for up to 8 weeks of observation. The CFU data for lungs and spleens revealed that the antituberculosis activity of CLA is inferior to those of INH and streptomycin. However, the activity of CLA when used alone or in combination was comparable to that of thiacetazone, indicating its potential usefulness as a secondary drug for the treatment of tuberculosis.
authors.affiliation: Department of Medicine, University of Illinois at Chicago 60612, USA.
authors.forename: J
authors.initials: J
authors.lastname: Luna-Herrera
authors.forename: V M
authors.initials: VM
authors.lastname: Reddy
authors.forename: D
authors.initials: D
authors.lastname: Daneluzzi
authors.forename: P R
authors.initials: PR
authors.lastname: Gangadharam
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology* / Q000627:therapeutic use; D000904:Antibiotics, Antitubercular / Q000494:pharmacology* / Q000627:therapeutic use; D000995:Antitubercular Agents / Q000494:pharmacology; D017291:Clarithromycin / Q000494:pharmacology* / Q000627:therapeutic use; D015169:Colony Count, Microbial; D004352:Drug Resistance, Microbial; D018432:Drug Resistance, Multiple; D004357:Drug Synergism; D005260:Female; D007538:Isoniazid / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000382:microbiology; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D012293:Rifampin / Q000494:pharmacology; D014376:Tuberculosis / Q000188:drug therapy / Q000382:microbiology / Q000401:mortality
chemical_list: D000900:Anti-Bacterial Agents; D000904:Antibiotics, Antitubercular; D000995:Antitubercular Agents; D017291:Clarithromycin; D007538:Isoniazid; D012293:Rifampin