Pharmacodynamic properties of leukotriene receptor antagonists.

摘要: Abstract Leukotrienes (LTs) are among the most important mediators of asthma; cysteine-containing LTs (cysteinyl-LTs, i.e. LTC4, LTD4 and LTE4) very potent bronchoconstrictors participate in inflammatory component asthma by inducing mucus hypersecretion, plasma extravasation, mucosal oedema eosinophil recruitment. Therefore, compounds able to inhibit either formation or action potential antiasthma drugs and, at present, cysteinyl-LT receptor antagonists (LTRAs) appear be promising. The receptors for cysteinyl-LTs, termed CysLT receptors, heterogeneous; least two different classes have so far been recognized, named CysLT1 (blocked so-called classical antagonists, such as FPL 55712, ICI 198,615, 204,219, SK&F 104353, MK-476 others) CysLT2 (insensitive but sensitive BAY u9773). authors' results indicate that even more subclasses might exist human airways, which discriminate between LTC4 LTD4, both mediators. Among many LTRAs, zafirlukast (Accolate, 204,219), montelukast (Singulair, MK-476) pranlukast (Onon, ONO-1078) available clinical use. All LTRAs LTD4-induced bronchoconstriction humans, albeit with potencies. With respect antigen challenge, all them early phase response, whereas only recently developed ones effective late phase. triggered exercise, cold aspirin. Furthermore, although they not bronchodilators per se, increase basal forced expiratory volume one second patients mild-to-moderate asthma, indicating that, these individuals, constant release contributes maintaining increased bronchial tone. Finally, effect is additive beta-agonists potentiated antihistamine compounds. In conclusion, clearly leukotrienes play an role cysteinyl leukotriene promising drugs.