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Dose-related protection of exercise bronchoconstriction by montelukast, a cysteinyl leukotriene-receptor antagonist, at the end of a once-daily dosing interval.
Clin Pharmacol Ther. 1997 Nov; 62(5):556-61.CP

Abstract

The dose-related protective effects of montelukast, a potent and selective cysteinyl leukotriene-receptor antagonist, against exercise-induced bronchoconstriction were investigated in a five-period, randomized, incomplete-block, crossover study with montelukast (0.4, 2, 10, 50 mg) and placebo. The study subjects were 27 nonsmoking, healthy stable patients with asthma (mean forced expiratory volume in 1 second [FEV1], 82.0% predicted) who demonstrated a > or = 20% decrease in FEV1 while beta-agonist was withheld for 6 hours before treadmill exercise. The standard exercise challenge was performed 20 to 24 hours, and again 32 to 36 hours, after the second of two once-daily doses. The effect of oral montelukast on exercise was measured by the area above the postexercise percentage decrease in FEV1 versus time curve from 0 to 60 minutes [AUC(0-60)], the maximal percentage decrease in FEV1 after exercise, and time after maximal decrease to recovery of FEV1 to within 5% of the preexercise baseline. Twenty to 24 hours after administration, montelukast caused dose-related protection, while providing similar protection against exercise-induced bronchoconstriction at the two highest doses. The AUC(0-60) values (mean +/- SD) were 637 +/- 898, 715 +/- 870, 988 +/- 1147, and 927 +/- 968 min. % for 50, 10, 2, and 0.4 mg montelukast, respectively, and 1193 +/- 1097 min. % for placebo (p = 0.003). No important clinical effect was present 36 hours after dosing. Montelukast was generally well tolerated at all dose levels. In conclusion, montelukast caused dose-related protection against exercise-induced bronchoconstriction at the end of a once-daily dosing interval. Protection against exercise-induced bronchoconstriction can be used to determine appropriate dose selection.

Authors+Show Affiliations

AAAA Medical Research Group, Salt Lake City, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

9390112

Citation

Bronsky, E A., et al. "Dose-related Protection of Exercise Bronchoconstriction By Montelukast, a Cysteinyl Leukotriene-receptor Antagonist, at the End of a Once-daily Dosing Interval." Clinical Pharmacology and Therapeutics, vol. 62, no. 5, 1997, pp. 556-61.
Bronsky EA, Kemp JP, Zhang J, et al. Dose-related protection of exercise bronchoconstriction by montelukast, a cysteinyl leukotriene-receptor antagonist, at the end of a once-daily dosing interval. Clin Pharmacol Ther. 1997;62(5):556-61.
Bronsky, E. A., Kemp, J. P., Zhang, J., Guerreiro, D., & Reiss, T. F. (1997). Dose-related protection of exercise bronchoconstriction by montelukast, a cysteinyl leukotriene-receptor antagonist, at the end of a once-daily dosing interval. Clinical Pharmacology and Therapeutics, 62(5), 556-61.
Bronsky EA, et al. Dose-related Protection of Exercise Bronchoconstriction By Montelukast, a Cysteinyl Leukotriene-receptor Antagonist, at the End of a Once-daily Dosing Interval. Clin Pharmacol Ther. 1997;62(5):556-61. PubMed PMID: 9390112.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Dose-related protection of exercise bronchoconstriction by montelukast, a cysteinyl leukotriene-receptor antagonist, at the end of a once-daily dosing interval. AU - Bronsky,E A, AU - Kemp,J P, AU - Zhang,J, AU - Guerreiro,D, AU - Reiss,T F, PY - 1997/12/9/pubmed PY - 1997/12/9/medline PY - 1997/12/9/entrez SP - 556 EP - 61 JF - Clinical pharmacology and therapeutics JO - Clin Pharmacol Ther VL - 62 IS - 5 N2 - The dose-related protective effects of montelukast, a potent and selective cysteinyl leukotriene-receptor antagonist, against exercise-induced bronchoconstriction were investigated in a five-period, randomized, incomplete-block, crossover study with montelukast (0.4, 2, 10, 50 mg) and placebo. The study subjects were 27 nonsmoking, healthy stable patients with asthma (mean forced expiratory volume in 1 second [FEV1], 82.0% predicted) who demonstrated a > or = 20% decrease in FEV1 while beta-agonist was withheld for 6 hours before treadmill exercise. The standard exercise challenge was performed 20 to 24 hours, and again 32 to 36 hours, after the second of two once-daily doses. The effect of oral montelukast on exercise was measured by the area above the postexercise percentage decrease in FEV1 versus time curve from 0 to 60 minutes [AUC(0-60)], the maximal percentage decrease in FEV1 after exercise, and time after maximal decrease to recovery of FEV1 to within 5% of the preexercise baseline. Twenty to 24 hours after administration, montelukast caused dose-related protection, while providing similar protection against exercise-induced bronchoconstriction at the two highest doses. The AUC(0-60) values (mean +/- SD) were 637 +/- 898, 715 +/- 870, 988 +/- 1147, and 927 +/- 968 min. % for 50, 10, 2, and 0.4 mg montelukast, respectively, and 1193 +/- 1097 min. % for placebo (p = 0.003). No important clinical effect was present 36 hours after dosing. Montelukast was generally well tolerated at all dose levels. In conclusion, montelukast caused dose-related protection against exercise-induced bronchoconstriction at the end of a once-daily dosing interval. Protection against exercise-induced bronchoconstriction can be used to determine appropriate dose selection. SN - 0009-9236 UR - https://www.unboundmedicine.com/medline/citation/9390112/Dose_related_protection_of_exercise_bronchoconstriction_by_montelukast_a_cysteinyl_leukotriene_receptor_antagonist_at_the_end_of_a_once_daily_dosing_interval_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0009-9236&date=1997&volume=62&issue=5&spage=556 DB - PRIME DP - Unbound Medicine ER -