Chand N, Achterrath-Tuckermann U, Szelenyi I, Sofia R D
Wallace Laboratories, Cranbury, New Jersey, USA.
Res Commun Mol Pathol Pharmacol. 1995 Feb;87(2):125-32.
Azelastine prevents down-regulation of beta 2-receptors and adenylate cyclase and upregulation of alpha 1-adrenoceptors induced by repeated allergen challenge in the guinea pig lung. In the present study the protective effects of azelastine and salbutamol and a combination of both drugs was investigated using aeroallergen-induced acute allergic bronchoconstrictor responses in conscious, actively sensitized guinea pig. The drugs were given orally 1 h prior to challenge. The oral PD50 was 230 micrograms/kg for azelastine and 1200 micrograms/kg for salbutamol. Both drugs showed a synergistic protective effect with a PD50 of 60 micrograms/kg of azelastine plus 120 micrograms/kg of salbutamol indicating a reduction in the PD50 of azelastine by a factor of 4 and of salbutamol by a factor of 10. These findings may explain the reduction in the use of salbutamol and theophylline with azelastine by chronic asthmatics.
氮卓斯汀可防止豚鼠肺中因反复变应原激发而引起的β2受体和腺苷酸环化酶下调以及α1肾上腺素能受体上调。在本研究中，采用气传变应原诱发的急性过敏性支气管收缩反应，在清醒、主动致敏的豚鼠中研究了氮卓斯汀和沙丁胺醇以及两种药物联合使用的保护作用。在激发前1小时口服给药。氮卓斯汀的口服半数有效量（PD50）为230微克/千克，沙丁胺醇为1200微克/千克。两种药物显示出协同保护作用，氮卓斯汀60微克/千克加沙丁胺醇120微克/千克时的PD50表明氮卓斯汀的PD50降低了4倍，沙丁胺醇的PD50降低了10倍。这些发现可能解释了慢性哮喘患者使用氮卓斯汀后沙丁胺醇和茶碱用量减少的原因。
