Szelenyi I, Achterrath-Tuckermann U, Schmidt J, Minker E, Paegelow I, Werner H
Department of Pharmacology, ASTA Pharma AG, Frankfurt/Main, FRG.
Agents Actions Suppl. 1991;34:295-311.
Azelastine (4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-p hthalazinone hydrochloride), a novel long-acting antiasthmatic/antiallergic drug has been demonstrated to be effective in the treatment both of asthma and of allergic rhinitis. In this paper some selected properties of azelastine are presented which might contribute to its antiasthmatic and antiallergic effect. Azelastine causes a marked inhibition of generation of oxygen radicals in alveolar macrophages. A bronchosecretolytic activity of azelastine is observed which is based on the secretion of a more liquid mucus. Furthermore, the mucociliary clearance is enhanced as demonstrated in a rabbit model. Also IL-1 generation is inhibited in vitro and in vivo. Finally, the possible tissue and cellular accumulation of azelastine in lung and alveolar macrophages resp. is discussed.
氮卓斯汀（4-（对氯苄基）-2-（六氢-1-甲基-1H-氮杂卓-4-基）-1（2H）-酞嗪酮盐酸盐），一种新型长效抗哮喘/抗过敏药物，已被证明在治疗哮喘和过敏性鼻炎方面均有效。本文介绍了氮卓斯汀的一些特定性质，这些性质可能有助于其抗哮喘和抗过敏作用。氮卓斯汀可显著抑制肺泡巨噬细胞中氧自由基的产生。观察到氮卓斯汀具有支气管分泌溶解活性，这基于更稀薄黏液的分泌。此外，如在兔模型中所示，黏液纤毛清除功能增强。在体外和体内，白细胞介素-1的产生也受到抑制。最后，讨论了氮卓斯汀在肺和肺泡巨噬细胞中可能的组织和细胞蓄积情况。
