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Penetration of Macrolides into the Respiratory Tract

  • F. Fraschini
  • M. Falchi
  • V. Copponi
Part of the New Perspectives in Clinical Microbiology book series (NPCM, volume 4)

Abstract

Almost all antibiotics are known to appear in saliva and bronchial secretions, at least in trace amounts. However, in these secretions certain antibiotics reach concentrations equivalent to or even higher than the M.I.C. for numerous bacterial strains or genera that are responsible for the most common respiratory disorders. Such pharmacokinetic data are therefore of great interest for the choice of the most suitable antibiotic therapy for a bacterial infection of the respiratory system. The exact mechanism underlying penetration of antibiotics into the lung, of their secretion into saliva, or at least all of the factors involved, are still unknown [1]. Antibiotics reach the bronchopulmonary system and saliva in two completely different ways. Salivary secretion is related to pharmacokinetic processes and to the degree of tropism for tissues, because the salivary glands do not offer any appreciable barrier to antibiotic penetration. On the contrary, the concentration of antibiotics in the respiratory system seems to be completely independent of serum levels, and in healthy subjects bronchopulmonary concentrations are usually much lower (30–40 times) than those in the serum. These pharmacokinetic data led to the conclusion that there must be a blood-lung, or rather a blood-bronchi, barrier that may be even less permeable than the better-known blood-brain barrier [2]. However, certain antibiotics reach surprisingly high (macrolides, lincomycin, rifampin, chloramphenicol) or at least therapeutic (ampicillin, cefalosporins) levels in the bronchi. This phenomenon has led some authors to suggest the existence of a mechanism of active transport able to concentrate some antibiotics selectively in bronchial mucus [3,4].

Keywords

Respiratory System Fusidic Acid Pulmonary Tissue Salivary Level Bronchial Secretion 
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.

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References

  1. 1.
    Matsumoto K, Uzuka Y: Concentrations of antibiotics in bronchiolar secretions of the patients with chronic respiratory infections. In: Chemotherapy (Williams JD, Geddes AM, eds.), Plenum Press, New York, Plenum Press, 1975, 4, p. 73.Google Scholar
  2. 2.
    Fraschini F, Copponi V, Dubini F, Scarpazza G: Concentration of erythromycin and ampicillin in bronchial secretions of patients with chronic respiratory infections. In: Current Chemotherapy (Siegenthaler W, Lüthy R (eds.), American Society for Microbiology Washington DC, 1978, p. 650.Google Scholar
  3. 3.
    May JR, Delves DM: Treatment of chronic bronchitis with ampicillin: some pharmacological observations. Lancet i: 929, 1965.Google Scholar
  4. 4.
    Saggers BA, Lawson D: In vivo penetration of antibiotics into sputum in cystic fibrosis. Arch Dis Childh 43: 404, 1968.PubMedCrossRefGoogle Scholar
  5. 5.
    Saggers BA, Lawson D: Some observations on the penetration of antibiotics through mucus in vitro. J Clin Path 19: 313, 1966.PubMedCrossRefGoogle Scholar
  6. 6.
    Simon C and Clasen I: Sputum concentrations of erythromycin after single and repeated oral administration in adult patients with bronchitis. In: Current Chemotherapy ( Siegenthaler W, Lüthy R. (eds.), American Society for Microbiology. Washington DC, 1978, p. 652.Google Scholar
  7. 7.
    Dubini F, Faraone P, Guastamacchia C, Fraschini F: Riccrca della eritromicina e della spiramicina nella saliva. Dental Cadmos 10: 1, 1976.Google Scholar
  8. 8.
    Sheila M, Stewart Fisher M, Young JE, Lutz W: Ampicillin levels in sputum, serum and saliva. Thorax 25: 304, 1970.CrossRefGoogle Scholar
  9. 9.
    Fraschini F, Braga PC, Copponi V, Scaglione F, Fumagalli G, Gattei G, Scarpazza G: Penetration of erythromycin into the bronchi. Acta Pediatrica Belgica, 1980, in press.Google Scholar
  10. 10.
    Balbirsingh M, Dorn J, Klainer AS, Liss RH, Norman JC, Ward EE: Erythromyrin. In: Current chemotherapy ( Siegenthaler W, Lüthy R, (eds.), American Society for Microbiology. Washington DC, 1978, p. 650.Google Scholar
  11. 11.
    Gould JC: Personal communication.Google Scholar
  12. 12.
    Dette G: Personal communication.Google Scholar
  13. 13.
    Canad Med Asso J.: Concentration of orally administered erythromycin and tetracycline in ischemic tissue. Med News in Brief 85: 504, 1961.Google Scholar
  14. 14.
    Fraschini F, Braga PC, Copponi V, Gattei G, Guerrasio E, Scaglione F, Villa F, Scarpazza G: Tropism of erythromycin for respiratory system. Communication. In: Current Chemotherapy and Infections Disease. ( Nelson JD, Grassi C, eds.), American Society for Microbiology, Washington DC, 1980, p. 659.Google Scholar
  15. 15.
    Fraschini F, Avallon R, Copponi V, Fumagalli G, Mandler F, Scaglione F, Scarpazza G: Bactericidal action of an average dose of erythromycin in the bronchi. Current Med Res Opinion 6: 107, 1979.Google Scholar
  16. 16.
    Stephens VC, Puch CT, Davis NE, Hoehn MM, Ralston S, Sparks MC, Thompkins L.: A study of the behavior of propionyl erythromycin in blood by a new chromatographic method. J Antibiot 22: 551, 1969.PubMedGoogle Scholar
  17. 17.
    Neaverson MA: Intravenous administration of erythromycin: serum, sputum, and urine levels. Curr Med Res Opinion 4: 359, 1976.CrossRefGoogle Scholar
  18. 18.
    MacFarlane, JA, Mitchell AA B, Walsh JM, Robertson J: Spiramycin in the prevention of postoperative staphylococcal infection. Lancet i: 1, 1969.Google Scholar

Copyright information

© Martinus Nijhoff Publishers, The Hague 1981

Authors and Affiliations

  • F. Fraschini
  • M. Falchi
  • V. Copponi

There are no affiliations available

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