Skip to main content
Log in

Pharmacokinetics of roxithromycin and influence of H2-blockers and antacids on gastrointestinal absorption

  • New Antimicrobial Agents
  • Published:
European Journal of Clinical Microbiology and Infectious Diseases Aims and scope Submit manuscript

Abstract

The pharmacokinetics of roxithromycin (300 mg orally) and the influence of the antacid aluminum magnesium hydroxide and the H2-blocker ranitidine on bioavailability of roxithromycin in ten healthy volunteers were studied. Pharmacokinetics after a single dose of roxithromycin were characterized by high peak serum levels (9.1 ± 2.1 mg/l) and a long elimination half-life (7.2 ± 2.5 h), resulting in a large area under the curve (116.9 ± 32.7 mg h/l). High inter- and intraindividual variations were found for both the absorption time and the elimination half-life. The bioavailability of roxithromycin was not affected by coadministration with antacids or ranitidine.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Lassman HB, Puri SK, Ho I, Mezzino MJ: Pharmacokinetics of roxithromycin (RU 965). Journal of Clinical Pharmacology 1988, 28: 141–152.

    PubMed  Google Scholar 

  2. Deppermann KM, Lode H, Höffken G, Tschink G, Kalz C, Koeppe P: Influence of ranitidine, pirenzipine, and aluminummagnesium hydroxide on the bioavailability of various antibiotics, includine amoxicillin, cephalexin, doxycycline, and amoxicillin-clavulanic acid. Antimicrobial Agents and Chemotherapy 1989, 33: 1901–1907.

    PubMed  Google Scholar 

  3. Höffken G, Borner K, Glatzel PD, Koeppe P, Lode H: Reduced enteral absorption of ciprofloxacin in the presence of antacids. European Journal of Clinical Microbiology 1985, 4: 345–349.

    Google Scholar 

  4. Birkett DJ, Robson RA, Grgurinovich N, Tonkin A: Single oral dose pharmacokinetics of erythromycin and roxithromycin and the effects of chronic dosing. Therapeutic Drug Monitoring 1990, 12: 65–71.

    PubMed  Google Scholar 

  5. Saint-Salvi B, Tremblay D, Surjus A, Lefebvre MA: A study of the interactions of roxithromycin with theophylline and carbamazepine. Journal of Antimicrobial Chemotherapy 1987, 20, Supplement B: 121–129.

    PubMed  Google Scholar 

  6. Billaud EM, Giullemain R, Fortineau N, Kitzis MD, Dreyfus G, Amrein C, Kreft-Jais C, Husson JM, Chretien P: Interaction between roxithromycin and cyclosporin in heart transplant patients. Clinical Pharmacokinetics 1990, 19: 499–502.

    PubMed  Google Scholar 

  7. Koeppe P, Hammann C: A program for nonlinear regression analysis to be used on a desk-top computer. Computer Programs in Biomedicine 1980, 12: 121–128.

    Article  PubMed  Google Scholar 

  8. Peck CC, Sheiner LB, Nicols AI: The problem of choosing weights in nonlinear analysis of pharmacokinetic data. Drug Metabolism Reviews 1984, 15: 133–148.

    PubMed  Google Scholar 

  9. Lode H, Stahlmann R, Koeppe P: Comparative pharmacokinetics of cephalexin, cefachlor, cefadroxil, and CGP 9000. Antimicrobial Agents and Chemotherapy 1984, 16: 1–6.

    Google Scholar 

  10. Wise R, Kirkpatrick B, Ashby J, Andrews JM: Pharmacokinetics and tissue penetration of roxithromycin after multiple dosing. Antimicrobial Agents and Chemotherapy 1987, 31: 1051–1053.

    PubMed  Google Scholar 

  11. Morávek J, Matoušovic K, Prát V, Šedivy J: Pharmacokinetics of roxithromycin in kidney grafted patients under cyclosporin A or azathioprine immunosuppression and in healthy volunteers. International Journal of Clinical Pharmacology, Therapy, & Toxicology 1990, 28: 262–267.

    Google Scholar 

  12. Tremblay D, Jaeger H, Fourtillan JB, Manuel C: Pharmacokinetics of three single doses (150 mg, 300 mg, 450 mg) of roxithromycin in young volunteers. British Journal of Clinical Practice 1988, 42, Supplement 55: 49–50.

    PubMed  Google Scholar 

  13. Segre G, Bianchi E, Zanolo G, Bartucci F, Sassella D: Influence of food on the bioavailability of roxithromycin versus erythromycin stearate. British Journal of Clinical Practice 1988, 42, Supplement 55: 55–57.

    Google Scholar 

  14. Periti P, Mazzei T, Mini E, Novelli A: Clinical pharmacokinetics of macrolide antibiotics. Clinical Pharmacokinetics 1989, 16: 193–214, 261–282.

    PubMed  Google Scholar 

  15. Lassman HB, Puri SK, Ho I, Sabo R, Barry A: Influence of food on the absorption of RU 28965 (a new macrolide antibiotic) from film-coated tablets in healthy volunteers. In: Butzler JP (ed): Macrolides: a review with an outlook on future developments, Exerpta Medica, Amsterdam, 1986, p. 138–142.

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Boeckh, M., Lode, H., Höffken, G. et al. Pharmacokinetics of roxithromycin and influence of H2-blockers and antacids on gastrointestinal absorption. Eur. J. Clin. Microbiol. Infect. Dis. 11, 465–468 (1992). https://doi.org/10.1007/BF01961866

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF01961866

Keywords

Navigation