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氮卓斯汀及某些选定药物对黏液纤毛清除功能的影响。

Influence of azelastine and some selected drugs on mucociliary clearance.

作者信息

Achterrath-Tuckermann U, Saano V, Minker E, Stroman F, Arny I, Joki S, Nuutinen J, Szelenyi I

机构信息

Department of Pharmacology, ASTA Pharma AG, Frankfurt/M., FRG.

出版信息

Lung. 1992;170(4):201-9. doi: 10.1007/BF00174117.

Abstract

The effect of azelastine and some selected compounds on ciliary beating frequency (CBF) was investigated in vitro using human mucosal samples and in vivo using anesthetized guinea pigs. Further influence of azelastine on mucus secretion was evaluated in mice and on mucociliary clearance in anesthetized rabbits. Azelastine influenced the ciliary beating frequency neither in vitro nor in vivo. Azelastine, similarly to salbutamol, ambroxol, and bromhexine, increased mucus secretion measured by the tracheal output of phenol red. Azelastine dose-dependently enhanced mucociliary clearance measured by elimination of 99mTc-labeled erythrocytes in rabbits. The activity of azelastine proved to be about 10 times stronger than that of bromhexine. Since the ciliary activity remained unchanged under the influence of azelastine, it is likely that azelastine increases the mucociliary clearance by enhancing bronchial secretion. It is possible that the observed increase in mucociliary clearance may contribute to the beneficial effect of azelastine in the treatment of respiratory diseases.

摘要

使用人体黏膜样本在体外以及使用麻醉的豚鼠在体内研究了氮卓斯汀及一些选定化合物对纤毛摆动频率(CBF)的影响。在小鼠中评估了氮卓斯汀对黏液分泌的进一步影响,并在麻醉的兔子中评估了其对黏液纤毛清除功能的影响。氮卓斯汀在体外和体内均未影响纤毛摆动频率。与沙丁胺醇、氨溴索和溴己新类似,氮卓斯汀通过气管酚红排出量测量增加了黏液分泌。氮卓斯汀剂量依赖性地增强了通过消除兔子体内99mTc标记红细胞所测量的黏液纤毛清除功能。氮卓斯汀的活性被证明比溴己新强约10倍。由于在氮卓斯汀的影响下纤毛活性保持不变,氮卓斯汀很可能通过增强支气管分泌来增加黏液纤毛清除功能。观察到的黏液纤毛清除功能增加可能有助于氮卓斯汀在治疗呼吸道疾病中的有益作用。

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