Evening dosing is associated with higher plasma concentrations of pranlukast, a leukotriene receptor antagonist, in healthy male volunteers

Br J Clin Pharmacol. 1997 Sep;44(3):289-91. doi: 10.1046/j.1365-2125.1997.00650.x.

Abstract

Aims: To study the magnitude of differences in the pharmacokinetics of pranlukast, after morning and evening administration.

Methods: Pranlukast (300 mg) was administered to 12 healthy male volunteers on two separate occasions, either in the morning or evening. Both doses were given 30 min after a standard high fat content meal. Blood samples were collected up to 18 h postdose. Plasma was assayed by high performance liquid chromatography. Standard pharmacokinetic and statistical analyses were performed.

Results: Statistically significant (P < 0.05) increases were noted in AUC(o,t) (56%) and tmax (2.5 h) after evening administration. Cmax was 14% higher after evening dosing (95% C.I. 0.71-1.84).

Conclusions: Pranlukast bioavailability is apparently increased after evening dosing as compared with morning administration. Higher night-time and early morning plasma concentrations may confer additional therapeutic benefit at a time when asthmatics are at greatest risk of developing bronchospasm.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Anti-Asthmatic Agents / administration & dosage
  • Anti-Asthmatic Agents / pharmacokinetics*
  • Area Under Curve
  • Chromones / administration & dosage
  • Chromones / blood
  • Chromones / pharmacokinetics*
  • Chronotherapy*
  • Half-Life
  • Humans
  • Leukotriene Antagonists*
  • Male
  • Metabolic Clearance Rate

Substances

  • Anti-Asthmatic Agents
  • Chromones
  • Leukotriene Antagonists
  • pranlukast