Selection of dose regimens of azithromycin .
The unique pharmacokinetics of azithromycin are characterized by high, sustained tissue concentrations. The concentrations of azithromycin were predicted, following various multiple dose regimens, from concentrations in tonsillar, prostatic, and uterine tissues following single oral doses. Following a five-day treatment regimen (500 mg on day 1, followed by 250 mg on days 2-5), or a three-day regimen (500 mg daily for three days), concentrations of azithromycin in tonsillar tissue, representative of respiratory tract tissues, will continuously be greater than the MICs for key target pathogens (Streptococcus pyogenes, Haemophilus influenzae, Staphylococcus aureus) in infections of the respiratory tract for up to 10 days. Since tissue concentrations above the MICs for infecting organisms were correlated with efficacy in animal models of infection, short treatment regimens consisting of once-daily oral administration of azithromycin should be effective in the treatment of a variety of infections. A single 1 g oral dose will provide concentrations in the uterus and prostate, representing urogenital tissues, above the MIC for Chlamydia trachomatis for approximately 10 days. Thus, this regimen should be effective in the treatment of chlamydial infections of the genital tract.
Foulds
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G
Drug Metabolism Department, Pfizer Inc, Groton, CT 06340.
Johnson
R B
RB
D000284:Administration, Oral; D017963:Azithromycin; D004334:Drug Administration Schedule; D004917:Erythromycin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D008297:Male; D008826:Microbial Sensitivity Tests; D008954:Models, Biological; D014066:Palatine Tonsil / Q000737:chemistry / Q000378:metabolism; D011467:Prostate / Q000737:chemistry / Q000378:metabolism; D014599:Uterus / Q000737:chemistry / Q000378:metabolism
D004917:Erythromycin; D017963:Azithromycin