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Interaction Between Cyclosporine and Grapefruit Juice Requires Long‐Term Ingestion in Stable Renal Transplant Recipients
Author(s) -
Brunner Lane J.,
Munar Myrna Y.,
Vallian John,
Wolfson Marsha,
Stennett Douglass J.,
Meyer Mary M.,
Bennett William M.
Publication year - 1998
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1002/j.1875-9114.1998.tb03822.x
Subject(s) - grapefruit juice , pharmacokinetics , ingestion , crossover study , pharmacology , oral administration , medicine , drug , orange juice , drug interaction , renal transplant , kidney , chemistry , food science , alternative medicine , pathology , placebo
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.