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Pharmaceutisch Weekblad

, Volume 10, Issue 6, pp 272–276 | Cite as

The influence of ofloxacin and enoxacin on the metabolic pathways of theophylline in healthy volunteers

A pilot study
  • W. J. A. Wijnands
  • T. J. Janssen
  • P. J. M. Guelen
  • T. B. Vree
  • T. M. C. de Witte
Original Articles
  • 17 Downloads

Abstract

The pharmacokinetic parameters of theophylline and its major metabolites were measured in two healthy volunteers, after the administration of theophylline alone and during co-medication with ofloxacin, 200 mg twice daily, or enoxacin, 200 mg twice daily. During enoxacin co-medication, elimination half-lives of theophylline increased from 8.7 h to 17.4 h and from 6.1 h to 12.3 h, respectively. As the renal clearance of theophylline did not change, the decreased elimination of theophylline during enoxacin co-medication must result from a reduced metabolic clearance. Enoxacin co-medication caused a clearly decreased formation of the metabolitesI-methyluric acid and 3-methylxanthine, formed by N-demethylation, whereas the C-8 oxidation of theophylline was less influenced compared to the blank. Enoxacin's interference with the theophylline disposition is predominantly based on the inhibition of the microsomal N-demethylation. Ofloxacin co-medication did not induce a change in the plasma parameters or renal excretion of theophylline and its metabolites.

Keywords

Drug interactions Enoxacin Metabolism Ofloxacin Pharmacokinetics Theophylline 

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Copyright information

© Bohn, Scheltema & Holkema 1988

Authors and Affiliations

  • W. J. A. Wijnands
    • 1
    • 2
  • T. J. Janssen
    • 3
  • P. J. M. Guelen
    • 3
  • T. B. Vree
    • 4
  • T. M. C. de Witte
    • 3
  1. 1.Department of Pulmonary DiseaseFoundation Deventer HospitalsGC Deventerthe Netherlands
  2. 2.Farma Research BVAA Ravensteinthe Netherlands
  3. 3.Department of Pulmonary DiseasesMedical Centre DekkerswaldCA Heilige, Landstichtingthe Netherlands
  4. 4.Departments of Clinical Pharmacy and AnaesthesiologySint Radboud HospitalHB Nijmegenthe Netherlands

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