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Oral pharmacokinetics and food interaction of the leukotriene D 4 receptor antagonist verlukast
Author(s) -
SCHWARTZ JULES I.,
MARGOLSKEE DOROTHY J.,
BJORNSSON THORIR D.,
WILLIAMS VANESSA C.,
HSIEH JOHN Y.,
LIN CHARLES C.,
ROGERS J. DOUGLAS
Publication year - 1993
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.1365-2125.1993.tb00397.x
Subject(s) - pharmacokinetics , crossover study , antagonist , meal , pharmacology , leukotriene , oral administration , leukotriene receptor , medicine , chemistry , receptor , asthma , alternative medicine , pathology , placebo
The influence of dose and food on the pharmacokinetic profile of orally administered verlukast, a leukotriene D 4 receptor antagonist, was investigated in 12 healthy male volunteers. This was an open, four‐period, single dose, randomised, crossover design including the following doses: one 75 mg tablet, one 250 mg tablet, 500 mg (2 × 250 mg) and 500 mg immediately following a standard meal. There were dose‐related increases in the AUC, although after 500 mg verlukast this was disproportionately greater than with 75 mg ( P = 0.04). Similarly, there were dose‐related increases in C max . No differences were observed in the t max between treatments. With respect to food, there was a 22% decrease ( P = 0.02) in C max after 500 mg, and the AUC was 13% less ( P = 0.052). The differences in the plasma concentration profiles betweeen fasted and fed states are not considered to be of clinical importance.