Skip to main content
SpringerLink
Log in

Effects of Iron Supplements on the Oral Bioavailability of Moxifloxacin, a Novel 8-Methoxyfluoroquinolone, in Humans

  • Original Research Article
  • Published:
Clinical Pharmacokinetics Aims and scope Submit manuscript

Abstract

Objective

To investigate the effect of concomitant iron administration on the pharmacokinetics and tolerability of moxifloxacin.

Design

This was a single-centre, nonblinded, randomised, 2-way crossover study in healthy male volunteers.

Participants

12 healthy males (age 19 to 41 years) were enrolled in the study.

Methods

The plasma and urinary pharmacokinetics of moxifloxacin were investigated after single oral doses of moxifloxacin 400mg given either alone or together with ferrous sulfate (Eryfer® 100 equivalent to 100mg of Fe2+) administered concomitantly and again after 24 hours. There was a 1-week washout phase between the treatments. The plasma and urinary pharmacokinetics of moxifloxacin were characterised over the 72 hours after drug administration.

Results

The treatments were well tolerated. The concomitant administration of Eryfer® reduced the bioavailability of moxifloxacin [geometric mean area under the plasma concentration-time curve 20.7 versus 34.0 mg/L · h; relative bioavailability 61%, 90% confidence interval (CI) 54 to 69%] and slowed down the absorption rate (median time to maximum concentration 2.79 versus 1.0 hours), with a reduction in the mean maximum concentration (Cmax) [geometric mean Cmax 1.17 and 2.86 mg/L; estimated true ratio of Cmax41%, 90% CI 34 to 49%].

Conclusions

Concomitant ingestion of iron supplements significantly reduces the bioavailability of moxifloxacin. This is compatible with a reduction in solubilisation due to chelation with polyvalent cations, a common finding for quinolones. Because of the long half-life of moxifloxacin, staggered administration of moxifloxacin and potential cationic interactants should be considered to avoid a loss of therapeutic efficacy caused by subtherapeutic plasma concentrations of the quinolone.

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

Access this article

Log in via an institution

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

Instant access to the full article PDF.

Institutional subscriptions

Table I
Fig. 1

Similar content being viewed by others

References

  1. Dalhoff A, Petersen U, Endermann R. In vitro activity of BAY 12-8039, a new 8-methoxyquinolone. Chemotherapy 1996; 42: 410–25

    Article  CAS  Google Scholar 

  2. Blondeau JM, Felmingham D. In vitro and in vivo activity of moxifloxacin against community respiratory tract pathogens. Clin Drug Invest 1999; 18: 57–78

    Article  CAS  Google Scholar 

  3. Jacobs E, Dalhoff A, Brunner H. Efficacy of BAY 12-8039 in Mycoplasma pneumoniae infected guinea pigs [abstract no. F17]. 36th Interscience Conference on Antimicrobial Agents and Chemotherapy; 1996 Sep 15–18; New Orleans, Louisiana: 102

    Google Scholar 

  4. Lomaestro BM, Bailie GR. Absorption interactions with fluoroquinolones. 1995 update. Drug Saf 1995; 12: 314–33

    Article  CAS  Google Scholar 

  5. Deppermann KM, Lode H. Fluoroquinolones: interaction profile during enterai absorption. Drugs 1993; 45 Suppl. 3: 65–72

    Article  Google Scholar 

  6. Lomaestro BM, Bailie GR. Quinolone-cation interactions: a review. DICP 1991; 25: 1249–58

    Article  CAS  Google Scholar 

  7. Stass H, Kubitza D. Pharmacokinetics and elimination of moxifloxacin after oral and intravenous administration in man. J Antimicrob Chemother 1999; 43 Suppl. B: 83–90

    Article  CAS  Google Scholar 

  8. Ballow C, Lettieri J, Agarwal V, et al. Absolute bioavailability of moxifloxacin. Clin Ther 1999; 21: 513–22

    Article  CAS  Google Scholar 

  9. Stass H, Kubitza D, Unger S. The effect of food on the oral bioavailability of moxifloxacin in healthy male volunteers. Moxifloxacin in Practice 2000; 3: 15–23

    Google Scholar 

  10. Stass H, Kubitza D. Effects of dairy products on the oral bioavailability of moxifloxacin, a novel 8-methoxyfluoroquinolone, in healthy volunteers. Clin Pharmacokinet 2001; 40 Suppl. 1: 33–38

    Article  CAS  Google Scholar 

  11. Stass H, Böttcher M, Ochmann K. Evaluation of the influence of antacids and H2 antagonists on the absorption of moxifloxacin after oral administration of a 400mg dose to healthy volunteers. Clin Pharmacokinet 2001; 40 Suppl. 1: 39–48

    Article  CAS  Google Scholar 

  12. Stass H, Wandel C, Delesen H, et al. The effect of calcium supplements on the oral bioavailability of moxifloxacin in healthy male volunteers [abstract no. 132]. J Antimicrob Chemother 1999; 44 Suppl. A: 416

    Google Scholar 

  13. Stass H, Dalhoff A. Determination of BAY 12-8039, a new 8-methoxyquinolone, in human body fluids by high-performance liquid chromatography with fluorescence detection using on-column focusing. J Chromatogr B Biomed Sci Appl 1997; 702: 163–74

    Article  CAS  Google Scholar 

  14. Gibaldi M, Perrier D. Pharmacokinetics. 2nd ed. New York: Marcel Dekker Inc., 1982

    Google Scholar 

  15. Grasela Jr TH, Schentag JJ, Sedman AJ, et al. Inhibition of enoxacin absorption by antacids or ranitidine. Antimicrob Agents Chemother 1989; 33: 615–7

    Article  CAS  Google Scholar 

  16. Stass H, Ochmann K. Study to evaluate the interaction between BAY 12-8039 and ranitidine [abstract no. 3357]. 20th International Congress on Chemotherapy; 1997 Jun 29–Jul 3; Sydney, Australia: 108

    Google Scholar 

  17. Stass H, Böttcher M, Horstmann R. Study to evaluate the interaction between BAY 12-8039 and antacids [abstract no. 3358]. 20th International Congress on Chemotherapy; 1997 Jun 29–Jul 3; Sydney, Australia: 108

    Google Scholar 

  18. Davies B, Maesen FPV. Drug interactions with quinolones. Rev Infect Dis 1989; 11 Suppl. 5: 1083–90

    Article  Google Scholar 

  19. Janknegt R. Drug interactions with quinolones. J Antimicrob Chemother 1990; 26 Suppl. D: 7–29

    Article  CAS  Google Scholar 

  20. Knupp CA, Barbhaiya RH. A multiple-dose pharmacokinetic interaction study between didanosine (Videx) and Ciprofloxacin (Cipro) in male subjects seropositive for HIV but asymptomatic. Biopharm Drug Dispos 1997; 18: 65–77

    Article  CAS  Google Scholar 

Download references

Acknowledgements

The authors thank Dr Christian de Mey for his valuable scientific and editorial support during the preparation of this manuscript.

Author information

Authors and Affiliations

  1. Pharma Research Centre, Institute of Clinical Pharmacology, Bayer AG, Wuppertal, Germany

    Heino Stass & Dagmar Kubitza

Authors
  1. Heino Stass
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Dagmar Kubitza
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Heino Stass.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Stass, H., Kubitza, D. Effects of Iron Supplements on the Oral Bioavailability of Moxifloxacin, a Novel 8-Methoxyfluoroquinolone, in Humans. Clin Pharmacokinet 40 (Suppl 1), 57–62 (2001). https://doi.org/10.2165/00003088-200140001-00008

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003088-200140001-00008

Keywords

Search

Navigation