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Montelukast causes prolonged, potent leukotriene D4-receptor antagonism in the airways of patients with asthma.
Clin Pharmacol Ther. 1997 Jan; 61(1):83-92.CP

Abstract

Montelukast, a new specific oral cysteinyl LT3-receptor antagonist was evaluated for its activity in attenuating inhaled leukotriene D4 (LTD4) bronchoconstriction in patients with asthma. In two double-blind, placebo-controlled, randomized crossover studies, patients with mild asthma (forced expiratory volume in 1 second [FEV1] > or = 70%) were studied. In trial A, LTD4 challenge began 4 hours (peak plasma concentration) after a single dose of placebo or 5, 20, 100, and 250 mg montelukast. In trial B, and LTD4 challenge was started 20 hours after administration of placebo, 40 mg montelukast, or 200 mg montelukast. During each challenge, twofold increasing concentrations of LTD4 were inhaled until specific airways conductance (sGaw) decreased by at least 50% (PC50) or the highest concentration of LTD4 was inhaled. In trial A with all doses and in trial B with the 200 mg dose, bronchoconstriction was attenuated (50% fall in sGaw was not observed) up to the highest dose of LTD4 administered. In trial B, during the 40 mg period, only two of six patients exhibited a 50% fall in sGaw; PC50 ratios (montelukast 40 mg/placebo) were 18 and 45 in these two patients. These results indicate that montelukast is a highly potent and long-lasting antagonist of LTD4-induced bronchoconstriction in patients with asthma.

Authors+Show Affiliations

Merck Research Laboratories, Brussels.No affiliation info availableNo affiliation info availableNo 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

9024176

Citation

De Lepeleire, I, et al. "Montelukast Causes Prolonged, Potent Leukotriene D4-receptor Antagonism in the Airways of Patients With Asthma." Clinical Pharmacology and Therapeutics, vol. 61, no. 1, 1997, pp. 83-92.
De Lepeleire I, Reiss TF, Rochette F, et al. Montelukast causes prolonged, potent leukotriene D4-receptor antagonism in the airways of patients with asthma. Clin Pharmacol Ther. 1997;61(1):83-92.
De Lepeleire, I., Reiss, T. F., Rochette, F., Botto, A., Zhang, J., Kundu, S., & Decramer, M. (1997). Montelukast causes prolonged, potent leukotriene D4-receptor antagonism in the airways of patients with asthma. Clinical Pharmacology and Therapeutics, 61(1), 83-92.
De Lepeleire I, et al. Montelukast Causes Prolonged, Potent Leukotriene D4-receptor Antagonism in the Airways of Patients With Asthma. Clin Pharmacol Ther. 1997;61(1):83-92. PubMed PMID: 9024176.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Montelukast causes prolonged, potent leukotriene D4-receptor antagonism in the airways of patients with asthma. AU - De Lepeleire,I, AU - Reiss,T F, AU - Rochette,F, AU - Botto,A, AU - Zhang,J, AU - Kundu,S, AU - Decramer,M, PY - 1997/1/1/pubmed PY - 1997/1/1/medline PY - 1997/1/1/entrez SP - 83 EP - 92 JF - Clinical pharmacology and therapeutics JO - Clin Pharmacol Ther VL - 61 IS - 1 N2 - Montelukast, a new specific oral cysteinyl LT3-receptor antagonist was evaluated for its activity in attenuating inhaled leukotriene D4 (LTD4) bronchoconstriction in patients with asthma. In two double-blind, placebo-controlled, randomized crossover studies, patients with mild asthma (forced expiratory volume in 1 second [FEV1] > or = 70%) were studied. In trial A, LTD4 challenge began 4 hours (peak plasma concentration) after a single dose of placebo or 5, 20, 100, and 250 mg montelukast. In trial B, and LTD4 challenge was started 20 hours after administration of placebo, 40 mg montelukast, or 200 mg montelukast. During each challenge, twofold increasing concentrations of LTD4 were inhaled until specific airways conductance (sGaw) decreased by at least 50% (PC50) or the highest concentration of LTD4 was inhaled. In trial A with all doses and in trial B with the 200 mg dose, bronchoconstriction was attenuated (50% fall in sGaw was not observed) up to the highest dose of LTD4 administered. In trial B, during the 40 mg period, only two of six patients exhibited a 50% fall in sGaw; PC50 ratios (montelukast 40 mg/placebo) were 18 and 45 in these two patients. These results indicate that montelukast is a highly potent and long-lasting antagonist of LTD4-induced bronchoconstriction in patients with asthma. SN - 0009-9236 UR - https://www.unboundmedicine.com/medline/citation/9024176/Montelukast_causes_prolonged_potent_leukotriene_D4_receptor_antagonism_in_the_airways_of_patients_with_asthma_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0009-9236&date=1997&volume=61&issue=1&spage=83 DB - PRIME DP - Unbound Medicine ER -