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.
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Lassman HB, Puri SK, Ho I, Mezzino MJ: Pharmacokinetics of roxithromycin (RU 965). Journal of Clinical Pharmacology 1988, 28: 141–152.
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.
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.
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.
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.
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.
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.
Peck CC, Sheiner LB, Nicols AI: The problem of choosing weights in nonlinear analysis of pharmacokinetic data. Drug Metabolism Reviews 1984, 15: 133–148.
Lode H, Stahlmann R, Koeppe P: Comparative pharmacokinetics of cephalexin, cefachlor, cefadroxil, and CGP 9000. Antimicrobial Agents and Chemotherapy 1984, 16: 1–6.
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.
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.
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.
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.
Periti P, Mazzei T, Mini E, Novelli A: Clinical pharmacokinetics of macrolide antibiotics. Clinical Pharmacokinetics 1989, 16: 193–214, 261–282.
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.
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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
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DOI: https://doi.org/10.1007/BF01961866