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Effect of grapefruit juice on cabergoline pharmacokinetics in patients with Parkinson's disease
Author(s) -
Nagai M.,
Nakatsuka A.,
Yabe H.,
Moritoyo T.,
Nomoto M.
Publication year - 2005
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/j.clpt.2004.12.213
Subject(s) - cabergoline , grapefruit juice , parkinson's disease , pharmacokinetics , medicine , pharmacology , disease , hormone , prolactin
Background Cabergoline is one of the synthetic ergoline dopamine agonists, which is widely used for the treatment of Parkinson's disease (PD). Cytochrome P‐450 (CYP) 3A4 contributes to metabolize Cabergoline. It has been well known that grapefruit juice inhibits CYP3A4 enzyme located in the gut wall. To investigate whether grapefruit juice influences the pharmacokinetics of cabergoline, plasma level of cabergoline in patients of PD was evaluated. Methods Five patients with PD treated with cabergoline were enrolled. Plasma concentrations of cabergoline before and after coadministration of grapefruit juice were evaluated. The plasma concentration of cabergoline was determined using a LC/MS/MS. Results The plasma concentration of cabergoline increased approximately 1.7 times, when grapefruit juice was taken together with cabergoline. Adverse events were not observed during this trial. Conclusions Coadministration of grapefruit juice with cabergoline increases bioavailability of cabergoline. A relatively large therapeutic window of cabergoline may allow the concomitant treatment with grapefruit juice, and this combination treatment may augment the antiparkisonian effect of cabergoline. Clinical Pharmacology & Therapeutics (2005) 77 , P84–P84; doi: 10.1016/j.clpt.2004.12.213