Leukotriene receptor antagonists and antiallergy drugs

Tsutomu Tamada, Masakazu Ichinose

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

24 Citations (Scopus)


As one of the candidates of the therapeutic strategy for asthma in addition to inhaled corticosteroids (ICS), leukotriene receptor antagonists (LTRAs) are known to be useful for long-term management of asthma patients complicated by allergic rhinitis (AR) or exercise-induced asthma (EIA). Currently available LTRAs are pranlukast hydrate, zafirlukast, and montelukast. These LTRAs have a bronchodilator action and inhibit airway inflammation, resulting in a signifi- cant improvement of asthma symptoms, respiratory function, inhalation fre- quency of as-needed inhaled β2-agonist, airway inflammation, airway hyperresponsiveness, dosage of ICSs, asthma exacerbations, and patients’ QOL. Although cys-LTs are deeply associated with the pathogenesis of asthma, LTRAs alone are less effective compared with ICS. However, the effects of LTRAs in combination with ICS are the same as those of LABAs in combination with ICS in steroid-naïve asthmatic patients. Concerning antiallergy drugs other than LTRAs, some mediator-release suppressants, H1 histamine receptor antagonists (H1RAs), thromboxane A2 (TXA2) inhibitors/antagonists, and Th2 cytokine inhibitor had been used mainly in Japan until the late 1990s. However, the use of these agents rapidly decreased after ICS/long acting beta agonist (LABA) combination was introduced and recommended for the man- agement of asthma in the early 2000s. The effectiveness of other antiallergic agents on asthma management seems to be quite limited, and the safety of oral antiallergic agents has not been demonstrated in fetuses during pregnancy. Further effectiveness studies are needed to determine the true value of these orally administered agents in combination with ICS as an anti-asthma treatment.

Original languageEnglish
Title of host publicationHandbook of Experimental Pharmacology
PublisherSpringer New York LLC
Number of pages17
Publication statusPublished - 2016

Publication series

NameHandbook of Experimental Pharmacology
ISSN (Print)0171-2004
ISSN (Electronic)1865-0325


  • H1RA
  • LTRA
  • Mediator-release suppressant
  • Th2 cytokine inhibitor
  • TXA2 inhibitor/antagonist


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