Impairment of mycophenolate mofetil absorption by iron ion

Clin Pharmacol Ther. 2000 Dec;68(6):613-6. doi: 10.1067/mcp.2000.111480.

Abstract

Objective: We sought to evaluate the effect of iron ion on the absorption of mycophenolate mofetil, which is an immunosuppressive agent. The pharmacokinetics of mycophenolic acid were studied.

Methods: A randomized crossover design with two phases was used. A 7-day washout period separated the two treatment conditions. In the first phase, the volunteers received 1.0 g of mycophenolate mofetil alone (study 1); in the second phase, the volunteers received 1.0 g of mycophenolate mofetil and 2 tablets of iron ion preparations concomitantly (study 2). The serum concentration of mycophenolic acid, which is a pharmacologically active metabolite, was measured by reverse-phase HPLC.

Results: The area under the plasma concentration-time curve from 0 to 12 hours and the maximum concentration of mycophenolic acid in study 2 were significantly less than in study 1 (area under the curve, 32.9 +/- 14.7 versus 2.92 +/- 0.883 microg x h/mL, P < .001, maximum concentration, 20.1 +/- 9.21 versus 1.30 +/- 0.367 microg x h/mL, P < .001).

Conclusions: This finding shows that when mycophenolate mofetil and iron ion preparations were administered concomitantly, a remarkable decrease of mycophenolate mofetil absorption was observed. Therefore it seems to be clear that we must avoid the concomitant administration of mycophenolate mofetil and iron ion preparations.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Cations, Divalent
  • Cross-Over Studies
  • Delayed-Action Preparations
  • Drug Interactions
  • Female
  • Ferrous Compounds / administration & dosage
  • Ferrous Compounds / adverse effects*
  • Humans
  • Immunosuppressive Agents / pharmacokinetics*
  • Intestinal Absorption / drug effects*
  • Male
  • Middle Aged
  • Mycophenolic Acid / analogs & derivatives*
  • Mycophenolic Acid / blood
  • Mycophenolic Acid / pharmacokinetics*

Substances

  • Cations, Divalent
  • Delayed-Action Preparations
  • Ferrous Compounds
  • Immunosuppressive Agents
  • ferrous sulfate
  • Mycophenolic Acid