Clinical safety and tolerability of montelukast, a leukotriene receptor antagonist, in controlled clinical trials in patients aged > or = 6 years

Clin Exp Allergy. 2001 Jan;31(1):77-87. doi: 10.1046/j.1365-2222.2001.00969.x.

Abstract

Objective: Montelukast is a leukotriene receptor antagonist administered orally once daily for treatment of chronic asthma in adults and children. A comprehensive analysis of safety data from double-blind, randomized, placebo-controlled trials with montelukast has not been previously reported.

Patients and methods: A pooled analysis of safety data from 11 multicentre, randomized, controlled montelukast Phase IIb and III trials and five long-term extension studies was performed. A total of 3386 adult patients (aged 15-85 years) and 336 paediatric patients (aged 6-14 years) were enrolled in the trials; 2031 adults received montelukast for up to 4.1 years, and 257 children received montelukast for up to 1.8 years. Summary statistics comparing incidences of adverse events among treatment groups were calculated.

Results: The overall incidence of clinical and laboratory adverse events among montelukast-treated patients, both adult and paediatric, was similar to that among patients receiving placebo. There were no clinically relevant differences in individual adverse events, including infectious upper respiratory conditions and transaminase elevations, between montelukast and placebo groups. Discontinuations due to adverse events occurred with similar frequencies during placebo, montelukast and inhaled beclomethasone therapy. No dose-related adverse effects of montelukast were observed in adults treated with dosages as high as 200 mg per day (20 times the recommended dose) for 5 months. This tolerability profile montelukast observed in clinical trials has been generally reflected in the post-marketing safety experience seen to date.

Conclusions: These data indicate a tolerability profile for montelukast similar to placebo during both short-term and long-term administration, even at doses substantially higher than the recommended clinical dose of 10 mg once daily for adults and 5 mg once daily for children aged 6-14 years.

Publication types

  • Meta-Analysis
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetates / therapeutic use*
  • Adolescent
  • Adult
  • Aged
  • Aged, 80 and over
  • Asthma / drug therapy*
  • Child
  • Chronic Disease
  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • Cyclopropanes
  • Double-Blind Method
  • Female
  • Humans
  • Leukotriene Antagonists / therapeutic use*
  • Male
  • Middle Aged
  • Multicenter Studies as Topic
  • Quinolines / therapeutic use*
  • Randomized Controlled Trials as Topic
  • Sulfides
  • Treatment Outcome

Substances

  • Acetates
  • Cyclopropanes
  • Leukotriene Antagonists
  • Quinolines
  • Sulfides
  • montelukast