Possible Interaction: Arachidonic Acid and Azelastine

“Pretreatment of alveolar macrophages with azelastine prevented the activation induced by PAF-acether and by the chemotactic peptide fMLP as estimated by the reduced liberation of arachidonic acid metabolites formed by the cyclooxygenase and the lipoxygenase pathways.”

“Similarly, a short pretreatment with azelastine (100 microM) prevented arachidonic acid-induced platelet aggregation.”

“The order of potency of the inhibitory effects on the arachidonic acid release were: homochlorcyclizine, clemastine, and azelastine (IC50 less than 20 microM) greater than oxatomide (IC50 less than 60 microM) and diphenylpyraline greater than triprolidine, meclizine, diphenhydramine (IC50 greater than 100 microM).”

“Results obtained in this study were as follows: (i) Formations of leukotriene B4 by neutrophils activated with a calcium ionophore (A23187) … of antiallergic drugs examined here, although the required concentrations were within a range of 20-200 microM. (ii) Releases of arachidonic acid from … azelastine and oxatomide … antiallergic drugs.”

“The arachidonic acid-induced contraction of isolated guinea-pig tracheal rings was also inhibited both by azelastine (IC50=92.6 μmol/l) and NDGA (IC50=20.4 μmol/l).”

“ Azelastine also reduced arachidonic acid-induced bronchoconstriction and LT-like material release from sensitised lungs, regardless of the presence of indomethacin.”

“The inhibition of the formation of the products of the lipoxygenase pathway of arachidonic acid metabolism by azelastine may contribute to its overall antiallergic, antiasthmatic, and pulmonary anti-inflammatory activities.”

“i) Azelastine , an antiallergic drug, inhibited arachidonic acid release as well as superoxide generation.”

“These experimental observations suggested that one of the important roles of the antiallergic agents including azelastine (known as a chemical mediator release inhibitor) and clemastine (known as a histamine H1 receptor antagonist) could be an inhibition of the first step of the arachidonic acid cascade.”