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 x 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.
Schwartz
J I
JI
Merck Research Laboratories, Clinical Pharmacology Department, P.O. Box 2000 (WBD-320), Rahway, NJ 07065-0914, USA.
Margolskee
D J
DJ
Bjornsson
T D
TD
Williams
V C
VC
Hsieh
J Y
JY
Lin
C C
CC
Rogers
J D
JD
D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D004311:Double-Blind Method; D005502:Food; D006801:Humans; D020024:Leukotriene Antagonists; D017998:Leukotriene D4; D008297:Male; D011422:Propionates / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D011804:Quinolines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D020024:Leukotriene Antagonists; D011422:Propionates; D011804:Quinolines; C059141:verlukast; D017998:Leukotriene D4