ORAL PHARMACOKINETICS AND FOOD INTERACTION OF THE LEUKOTRIENE D(4) RECEPTOR ANTAGONIST VERLUKAST

The influence of-dose and food on the pharmacokinetic profile of orall y administered verlukast, a leukotriene D4 receptor antagonist, was in vestigated in 12 healthy male volunteers. This was an open, four-perio d, single dose, randomised, crossover design including the following d oses: one 75 mg tablet, one 250 mg tablet, 500 mg (2 x 250 mg) and 500 mg immediately following a standard meal. There were dose-related inc reases in the AUC, although after 500 mg verlukast this was disproport ionately greater than with 75 mg (P = 0.04). Similarly, there were dos e-related increases in C(max) No differences were observed in the t(ma x) 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 faste d and fed states are not considered to be of clinical importance.