Oral pharmacokinetics and food interaction of the leukotriene D₄ receptor antagonist verlukast

The influence of dose and food on the pharmacokinetic profile of orally administered verlukast, a leukotriene D₄ 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. 1993 The British Pharmacological Society