Interaction between cyclosporine and grapefruit juice requires long-term ingestion in stable renal transplant recipients

Pharmacotherapy. Jan-Feb 1998;18(1):23-9.

Abstract

Study objective: To examine the effect of the concurrent administration of increasing amounts of grapefruit juice, an inhibitor of drug metabolism, on the steady-state pharmacokinetics of cyclosporine.

Design: Open-label, three-period crossover, food-drug interaction study in stable renal transplant patients.

Setting: A university-affiliated clinical research center.

Patients: Sixteen stable renal transplant recipients.

Intervention: Cyclosporine was administered with 240 ml of water, 240 ml of grapefruit juice, or several 240-ml glasses of grapefruit juice, and serial blood samples were taken to estimate the effect of grapefruit juice on cyclosporine pharmacokinetics.

Measurements and main results: Grapefruit juice caused a significant increase in cyclosporine area under the curve, however, no significant effect was seen in other pharmacokinetic parameters. Grapefruit juice caused an increase in the 24-hour trough cyclosporine concentration, which may be of clinical significance if long-term ingestion of grapefruit juice is recommended.

Conclusion: A drug interaction exists between cyclosporine and grapefruit juice, and it is likely at the level of intestinal drug absorption.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Area Under Curve
  • Beverages*
  • Citrus*
  • Cyclosporine / pharmacokinetics*
  • Cyclosporine / therapeutic use
  • Female
  • Food-Drug Interactions*
  • Humans
  • Immunosuppressive Agents / pharmacokinetics*
  • Immunosuppressive Agents / therapeutic use
  • Kidney Failure, Chronic / metabolism
  • Kidney Failure, Chronic / therapy
  • Kidney Transplantation / physiology*
  • Male
  • Middle Aged

Substances

  • Immunosuppressive Agents
  • Cyclosporine