Concentrations of azithromycin in human tonsillar tissue
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Patients scheduled to undergo tonsillectomy were administered 500 mg oral azithromycin as two 250 mg capsules given 12 h apart. Between 9 h and one week after the second dose, tonsil samples were taken during surgery and assayed for azithromycin. Mean concentrations in tonsillar tissue, 12 and 24 h after the second of the two 250 mg doses given 12 h apart, were 4.5 and 3.9 µg/g, respectively. Concurrent mean serum concentrations were approximately 0.03 and 0.01 µg/ml, respectively. The mean concentration in tonsillar tissue 7.5 days after the last dose was 0.93 µg/g. The apparent half-life of drug in the tissue was 76 h. The ratio of mean concentration in tissue to that in serum was greater than 150-fold for all time intervals. The presence of high azithromycin concentrations in tonsillar tissue suggests that a once-daily regimen over five days or less may be effective in treating tonsillo-pharyngitis.
KeywordsInternal Medicine Serum Concentration Azithromycin Tonsillar Tissue Oral Azithromycin
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- 1.Bright GM, Nagel AA, Bordner J, Desai KA, Dibring JN, Nowakowska J, Vincent L, Watrous RM, Sciavolino FC, English AR, Retsema JA, Anderson MR, Brennan LA, Borovoy RJ, Cimochowski CR, Faiella JA, Girard AE, Girard D, Herbert C, Manousos M, Mason R: Synthesis, in vitro and in vivo activity of novel 9-deoxo-9a-aza-9a homoerythromycin A derivatives; a new class of macrolide antibiotics, the azalides. Journal of Antibiotics 1988, 41: 1029–1047.PubMedGoogle Scholar
- 2.Fiese EF, Steffen SH: Comparison of the acid stability of azithromycin and erythromycin A. Journal of Antimicrobial Chemotherapy 1990, 25, Supplement A: 39–47.Google Scholar
- 3.Girard AE, Girard D, English AE, Gootz TD, Cimochowski CK, Faiella JA, Haskell SL, Retsema JA: Pharmacokinetic and in vivo studies with azithromycin (CP-62,993), a new macrolide with an extended half-life and excellent tissue distribution. Antimicrobial Agents and Chemotherapy 1987, 31: 1948–1954.PubMedGoogle Scholar
- 4.Shepard RM, Falkner FC: Pharmacokinetics of azithromycin in rats and dogs. Journal of Antimicrobial Chemotherapy 1990, 25, Supplement A: 49–60.Google Scholar
- 5.Foulds G, Shepard RM, Johnson RB: The pharmacokinetics of azithromycin in human serum and tissues. Journal of Antimicrobial Chemotherapy 1990, 25, Supplement A: 73–82.Google Scholar
- 6.Retsema J, Girard A, Shelkly W, Manousos M, Anderson M, Bright M, Borovoy R, Brennan L, Mason R: Spectrum and mode of action of azithromycin (CP-62,993), a new 15-membered-ring macrolide with improved potency against gram-negative organisms. Antimicrobial Agents and Chemotherapy 1987, 31: 1939–1947.PubMedGoogle Scholar
- 8.Goldstein FW, Emirian MF, Coutrot A, Acar JF: Bacteriostatic and bactericidal activity of azithromycin againstHaemophilus influenzae. Journal of Antimicrobial Chemotherapy 1990, 25, Supplement A: 25–28.Google Scholar
- 13.Retsema JA, Girard AE, Girard D, Milisen WP: Relationship of high tissue concentrations of azithromycin to bactericidal activity and efficacy in vivo. Journal of Antimicrobial Chemotherapy 1990, 25, Supplement A: 83–89.Google Scholar
- 15.Foulds G, Madsen P, Cox C, Shepard R, Johnson R: Concentration of azithromycin in human prostatic tissue. European Journal of Clinical Microbiology and Infectious Diseases 1991, 10: 868–871.Google Scholar
- 17.Kaplan JM, McCracken GH, Culbertson MC: Penicillin and erythromyein concentrations in tonsils. American Journal of Diseases in Children 1974, 127: 206–211.Google Scholar