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Major determinant factors of the extent of interaction between grapefruit juice and calcium channel antagonists
Author(s) -
Ohnishi Ayako,
Ohtani Hisakazu,
Sawada Yasufumi
Publication year - 2006
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.2006.02636.x
Subject(s) - bioavailability , grapefruit juice , chemistry , calcium , pharmacology , antagonist , pharmacokinetics , biochemistry , biology , receptor , organic chemistry
Aim To evaluate quantitatively the influence of bioavailability and plasma unbound fraction ( f u ) on the extent of interaction between grapefruit juice (GFJ) and calcium antagonists. Methods The extent of drug–GFJ interaction was evaluated from reported clinical interaction studies of 11 calcium antagonists. The relationship between extent of interaction and bioavailability or f u was analysed. Results The following significant hyperbolic relationships were observed: [Extent] = 12.2/[bioavailability] + 1 and [Extent] = 0.718/[ f u ] + 1. Conclusions Bioavailability and f u are major determinant factors of calcium antagonist–GFJ interaction: a drug with smaller bioavailability or lower f u is likely to exhibit a more potent interaction, and vice versa .