国产盐酸氮?斯汀抗组胺作用的实验评价

目的 评价国产盐酸氮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 盐酸氮卓斯汀(0.05, 0.15,0.45 mg·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;盐酸氮卓斯汀(0.05, 0.1,0.2 mg·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。盐酸氮卓斯汀(10^-8, 3 ×10^-8, 10^-7, 3 ×10^-7 mol·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8.55)。 结论 国产盐酸氮卓斯汀具有较好的抗组胺作用。

Experimental evaluation of the antihistamine effect of domestic azelastine hydrochloride

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^-7mol·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 (pA₂=8.55). CONCLUSION: Domestic azelastine hydrochloride shows significant the antihistamine effects.