国产盐酸氮斯汀抗组胺作用的实验评价

Experimental evaluation of the antihistamine effect of domestic azelastine hydrochloride

目的 :评价国产盐酸氮 艹卓 斯汀的抗组胺作用。方法 :皮内注射组胺增加豚鼠皮肤通透性 ;静脉注射组胺诱导豚鼠休克 ;组胺诱导离体豚鼠回肠平滑肌收缩。结果 :盐酸氮 艹卓 斯汀 (0 .0 5 ,0 .15 ,0 .4 5mg·kg-1,ig)可剂量依赖性地抑制组胺所致皮肤血管通透性增加 ;盐酸氮 艹卓 斯汀 (0 .0 5 ,0 .1,0 .2mg·kg-1,ig)可剂量依赖性地降低休克的反应程度 ,延长休克的潜伏期 ,降低豚鼠的死亡率。盐酸氮艹卓 斯汀 (10 -8,3× 10 -8,10 -7,3× 10 -7mol·L-1)可剂量依赖性拮抗组胺所致离体回肠平滑肌收缩 ,使组胺量效曲线平行右移 (pA2 值为 8.5 5 )。结论 :国产盐酸氮 艹卓

AIM: To evaluate the antihistamine effects of domestic azelastine hydrochloride. METHODS: Histamine increased skin vascular permeability and induced shock model in guinea pigs. In isolated guinea pig ileal rings, the contraction of smooth muscle induced by histamine was determined. RESULTS: Pretreament with azelastine hydrochloride( 0.05, 0.15,and 0.45 mg·kg -1,ig) significantly inhibited the increase in skin vascular permeability induced by histamine in a dose-dependent manner in guinea pigs. Pretreament with azelastine hydrochloride( 0.05, 0.1,and 0.2 mg·kg -1,ig)produced a significant improvement of shock, as shown by a decrease in reactivity degree, mortality and a prolongation of latency. In isolated guinea pig ileal rings, azelastine hydrochloride (10 -8,3×10 -8,10 -7,3× 10 -7 mol·L -1)significantly inhibited contraction of smooth muscle induced by histamine in a concentration-dependent manner and caused a parallel right shift of the dose-effect curve of histamine (pA 2= 8.55). CONCLUSION: Domestic azelastine hydrochloride shows significant the antihistamine effects.