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. 1990 Sep;34(9):1744–1748. doi: 10.1128/aac.34.9.1744

Influence of antacid and ranitidine on the pharmacokinetics of oral cefetamet pivoxil.

R A Blouin 1, J Kneer 1, R J Ambros 1, K Stoeckel 1
PMCID: PMC171916  PMID: 1981000

Abstract

The purpose of this investigation was to assess the influence that treatment with antacid and ranitidine had on the pharmacokinetics of oral cefetamet pivoxil in 18 healthy male volunteers. Each subject received, in an open-labeled, randomized, three-way crossover design, a single oral dose of 1,000 mg (two tablets) of cefetamet pivoxil 10 min after a standard breakfast during each of the following treatments: treatment A, control period; treatment B, antacid (80 ml of suspension; Maalox 70) administered on the evening before cefetamet pivoxil dosing (-12.5 h) and again 2 h before and 2 h after a standard breakfast; treatment C, ranitidine (150 mg) administered twice a day for 4 days and again 1 h and 10 min prior to cefetamet pivoxil dosing. Plasma and urine samples were collected over a 24-h period following cefetamet pivoxil administration. Cefetamet was analyzed by high-performance liquid chromatography. Oral bioavailability parameters (area under the concentration-time curve from 0 to 12 h, area under the concentration-time curve from 0 h to infinity, time to maximum concentration of drug in plasma, and maximum concentration of drug in plasma) were obtained by noncompartmental techniques. The results showed that none of these bioavailability parameters was significantly (P greater than 0.05) affected by antacid or rantidine coadministration. A compartmental analysis showed no significant differences. In addition, the terminal elimination half-life and the fraction of cefetamet excreted unchanged in the urine was also not significantly (P greater than 0.05) affected by antacid or ranitidine exposure. Relatively wide intrasubject variability was observed for time to maximum concentration of drug in plasma and terminal elimination half-life in several of the 18 subjects studied. Although these irregularities did not appear to be strongly associated with a particular treatment, they increased in subjects in both the antacid and H2-receptor antagonist treatment groups compared with those in subjects in the control treatment group. We conclude that antacid and ranitidine treatment likely does not alter the bioavailability of oral cefetamet pivoxil.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Blouin R. A., Kneer J., Stoeckel K. Pharmacokinetics of intravenous cefetamet (Ro 15-8074) and oral cefetamet pivoxil (Ro 15-8075) in young and elderly subjects. Antimicrob Agents Chemother. 1989 Mar;33(3):291–296. doi: 10.1128/aac.33.3.291. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Koup J. R., Dubach U. C., Brandt R., Wyss R., Stoeckel K. Pharmacokinetics of cefetamet (Ro 15-8074) and cefetamet pivoxil (Ro 15-8075) after intravenous and oral doses in humans. Antimicrob Agents Chemother. 1988 Apr;32(4):573–579. doi: 10.1128/aac.32.4.573. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Neut C., Lesieur V., Romond C., Beerens H. Analysis of gram-positive anaerobic cocci in oral, fecal and vaginal flora. Eur J Clin Microbiol. 1985 Aug;4(4):435–437. doi: 10.1007/BF02148708. [DOI] [PubMed] [Google Scholar]
  4. Nix D. E., Schentag J. J. The quinolones: an overview and comparative appraisal of their pharmacokinetics and pharmacodynamics. J Clin Pharmacol. 1988 Feb;28(2):169–178. doi: 10.1002/j.1552-4604.1988.tb05740.x. [DOI] [PubMed] [Google Scholar]
  5. Powell J. R., Donn K. H. The pharmacokinetic basis for H2-antagonist drug interactions: concepts and implications. J Clin Gastroenterol. 1983;5 (Suppl 1):95–113. doi: 10.1097/00004836-198312001-00010. [DOI] [PubMed] [Google Scholar]
  6. Sommers D. K., van Wyk M., Moncrieff J., Schoeman H. S. Influence of food and reduced gastric acidity on the bioavailability of bacampicillin and cefuroxime axetil. Br J Clin Pharmacol. 1984 Oct;18(4):535–539. doi: 10.1111/j.1365-2125.1984.tb02501.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Tam Y. K., Kneer J., Dubach U. C., Stoeckel K. Effects of timing of food and fluid volume on cefetamet pivoxil absorption in healthy normal volunteers. Antimicrob Agents Chemother. 1990 Aug;34(8):1556–1559. doi: 10.1128/aac.34.8.1556. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Thomson A. B., Pinchbeck B., Kirdeikis J., Kirdeikis P., Zuk L., Brunet M. K., Jurima-Romet M., Murray P. E. Evaluation of antacid tablets and liquid in fasting and fed men and women. Clin Ther. 1988;10(2):158–168. [PubMed] [Google Scholar]
  9. Wise R., Andrews J. M., Piddock L. J. In vitro activity of Ro 15-8074 and Ro 19-5247, two orally administered cephalosporin metabolites. Antimicrob Agents Chemother. 1986 Jun;29(6):1067–1072. doi: 10.1128/aac.29.6.1067. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Wyss R., Bucheli F. Determination of cefetamet and its orally active ester, cefetamet pivoxyl, in biological fluids by high-performance liquid chromatography. J Chromatogr. 1988 Aug 19;430(1):81–92. doi: 10.1016/s0378-4347(00)83136-9. [DOI] [PubMed] [Google Scholar]

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