Advertisement

Clinical Pharmacokinetics

, Volume 25, Issue 5, pp 370–374 | Cite as

Azithromycin Clinical Pharmacokinetics

  • Nestor J. Lalak
  • David L. Morris
Review Article Drug Disposition

Summary

Azalide antibiotics, of which azithromycin is the first demonstrated, have different pharmacokinetics from other antibiotics currently used. The bioavailability of the drug is approximately 37%. Extensive and rapid distribution from serum into the intracellular compartments is followed by rapid distribution to the tissues. Tissue concentrations exceed serum concentrations by up to 100-fold following a single azithromycin 500mg dose. Concentration of the drug within phagocytes aids in its ability to combat infections. High concentrations of azithromycin are found in the tonsil, lung, prostate, lymph nodes and liver, with only small concentrations found in fat and muscle. A 500mg dose on day 1, followed by 250mg daily on days 2 to 5, has been demonstrated to maintain azithromycin concentrations at sites of infection and continues to be effective for several days after administration has ceased. The pharmacokinetics of azithromycin make it a drug with diverse therapeutic applications.

Keywords

Erythromycin Azithromycin Clinical Microbiology Roxithromycin Antimicrobial Chemotherapy 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Aronoff SC, Laurent C, Jacobs MR. In vitro activity of erythromycin, roxithromycin and CP-62,993 against common pediatric pathogens. Journal of Antimicrobial Chemotherapy 19: 275–276, 1987PubMedCrossRefGoogle Scholar
  2. Coates P, Daviel R, Houston AC, Antiobus JHI, Taylor T. An open study to compare the pharmacokinetics, safety and tolerability of a multiple dose regimen of azithromycin in young and elderly volunteers. European Journal of Clinical Microbiology and Infectious Diseases 10: 850–852, 1991CrossRefGoogle Scholar
  3. Cooper MA, Nye K, Andrews JM, Wise R. The pharmacokinetics and inflammatory fluid penetration of orally administered azithromycin. Journal of Antimicrobial Chemotherapy 26: 533–538, 1990PubMedCrossRefGoogle Scholar
  4. Dunkin KT, Jones S, Howard AJ. The in vitro activity of CP-62,993 against Haemophilus influenzae, Branhamella catarrhalis, staphylococci and streptococci. Journal of Antimicrobial Chemotherapy 21: 405–411, 1988PubMedCrossRefGoogle Scholar
  5. Earthinf C, Rendel M, Currie B, Seidlin M. Azithromycin for cerebral toxoplasmosis. Lancet 339: 437–438, 1992Google Scholar
  6. Fiese EF, Steffen SH. Comparison of the acid stability of azithromycin and erythromycin. Journal of Antimicrobial Chemotherapy 25 (Suppl. A): 39–47, 1990PubMedGoogle Scholar
  7. Foulds G, Chan KH, Johnson JT, Shepard RM, Johnson RB. Concentration of azithromycin in human tonsillar tissue. European Journal of Clinical Microbiology and Infectious Diseases 10: 853–856, 1991bCrossRefGoogle Scholar
  8. Foulds G, Shepard RM, Johnson RB. The pharmacokinetics of azithromycin in human serum and tissues. Journal of Antimicrobial Chemotherapy 25 (Suppl. A): 73–82, 1990PubMedGoogle Scholar
  9. Foulds G, Madssen P, Cox C, Shepard R, Johnson R. Concentration of azithromycin in human prostatic tissue. European Journal of Clinical Microbiology and Infectious Diseases 10: 868–871, 1991aCrossRefGoogle Scholar
  10. Glaude RP, Bright GM, Isaacson RE, Newborg MF. In vitro and in vivo uptake of azithromycin (CP-62,993) by phagocytic cells: possible mechanisms of delivery and release at sites of infection. Antimicrobial Agents and Chemotherapy 33: 277–282, 1989CrossRefGoogle Scholar
  11. Harrison JD, Jones JA, Morris DL. Azithromycin levels in plasma and gastric tissue, juice and mucus. European Journal of Clinical Microbiology and Infectious Diseases 10: 862–864, 1991CrossRefGoogle Scholar
  12. Karma P, Pukander J, Penttila M. Azithromycin concentrations in sinus fluid and mucosa after oral administration. European Journal of Clinical Microbiology and Infectious Diseases 10: 856–859, 1991CrossRefGoogle Scholar
  13. Kitzis MD, Goldstein FW, Miegi M, Aca JF. In vitro activity of azithromycin against gram negative bacilli and anaerobic bacteria. Journal of Antimicrobial Chemotherapy 25 (Suppl. A): 15–18, 1990PubMedGoogle Scholar
  14. Krohn K. Gynaecological tissue levels of azithromycin. European Journal of Clinical Microbiology and Infectious Diseases 10: 865–868, 1991Google Scholar
  15. Lode H. The pharmacokinetics of azithromycin and their clinical significance. European Journal of Clinical Microbiology and Infectious Diseases 10: 807–812, 1991CrossRefGoogle Scholar
  16. McDonald PJ, Pruul H. Phagocyte uptake and transport of azithromycin. European Journal of Clinical Microbiology and Infectious Diseases 10: 828–833, 1991CrossRefGoogle Scholar
  17. Moellering RC. Introduction: Revolutionary changes in the macrolide and azalide antibiotics. American Journal of Medicine 91 (Suppl. 3A): 1S–4S, 1991PubMedCrossRefGoogle Scholar
  18. Morris DL, De Souza A, Jones JA, Morgan WE. High and prolonged pulmonary tissue concentrations of azithromycin following a single oral dose. European Journal of Clinical Microbiology and Infectious Diseases 10: 859–861, 1991CrossRefGoogle Scholar
  19. Neu HC. Clinical microbiology of azithromycin. American Journal of Medicine 91 (Suppl. 3A): 12S–18S, 1991PubMedCrossRefGoogle Scholar
  20. Norrby SR. Azithromycin: an antibiotic with unusual properties. European Journal of Clinical Microbiology and Infectious Diseases 10: 805–806, 1991CrossRefGoogle Scholar
  21. Schentag JJ, Ballow CH. Tissue directed pharmacokinetics. American Journal of Medicine 91 (Suppl. 3A): 5S–11S, 1991PubMedCrossRefGoogle Scholar
  22. Schonwald S, Gunjaca M, Kolacny-Babic L, Car V, Gasev M. Comparison of azithromycin and erythromycin in the treatment of atypical pneumonias. Journal of Antimicrobial Chemotherapy 25 (Suppl. A): 123–126, 1990PubMedGoogle Scholar
  23. Shepard RM, Falkner FC. Pharmacokinetics of azithromycin in rats and dogs. Journal of Antimicrobial Chemotherapy 25 (Suppl. A): 49–60, 1990PubMedGoogle Scholar
  24. Steingrimsson O, Olafsson O, Thorarinson A, Ryan RW, Johnson RB, et al. Azithromycin in the treatment of sexually transmitted diseases. Journal of Antimicrobial Chemotherapy 25 (Suppl. A): 109–114, 1990PubMedGoogle Scholar
  25. Williams JD. Spectrum of activity of azithromycin. European Journal of Clinical Microbiology and Infectious Diseases 10: 813–820, 1991CrossRefGoogle Scholar

Copyright information

© Adis International Limited 1993

Authors and Affiliations

  • Nestor J. Lalak
    • 1
  • David L. Morris
    • 1
  1. 1.Department of SurgerySt George HospitalSydneyAustralia

Personalised recommendations