McNeely W, Wiseman L R
Adis International Limited, Auckland, New Zealand.
Drugs. 1998 Jul;56(1):91-114. doi: 10.2165/00003495-199856010-00011.
Azelastine, a phthalazinone compound, is a second generation histamine H1 receptor antagonist which has shown clinical efficacy in relieving the symptoms of allergic rhinitis when administered as either an oral or intranasal formulation. It is thought to improve both the early and late phase symptoms of rhinitis through a combination of antihistaminic, antiallergic and anti-inflammatory mechanisms. Symptom improvements are evident as early as 30 minutes, after intranasal administration of azelastine [2 puffs per nostril (0.56mg)] and are apparent for up to 12 hours in patients with seasonal allergic rhinitis (SAR). The effect on nasal blockage is variable: in some studies objective and/or subjective assessment showed a reduction in blockage, whereas in other studies there was no improvement. Intranasal azelastine 1 puff per nostril twice daily is generally as effective as standard doses of other antihistamine agents including intranasal levocabastine and oral cetirizine, ebastine, loratadine and terfenadine at reducing the overall symptoms of rhinitis. The relative efficacies of azelastine and intranasal corticosteroids (beclomethasone and budesonide) remain unclear. However, overall, the corticosteroids tended to improve rhinitis symptoms to a greater extent than the antihistamine. Azelastine was well tolerated in clinical trials and postmarketing surveys. The most frequently reported adverse events were bitter taste, application site irritation and rhinitis. The incidence of sedation did not differ significantly between azelastine and placebo recipients and preliminary report showed cardiovascular parameters were not significantly altered in patients with perennial allergic rhinitis (PAR).
Twice-daily intranasal azelastine offers an effective and well tolerated alternative to other antihistamine agents currently recommended for the symptomatic relief of mild to severe SAR and PAR in adults and children (aged > or = 12 years in the US; aged > or = 6 years in some European countries including the UK). The rapid onset, confined topical activity and reduced sedation demonstrated by the intranasal formulation of azelastine may offer an advantage over other antihistamine agents, although this has yet to be confirmed.
氮卓斯汀是一种酞嗪酮化合物，是第二代组胺H1受体拮抗剂，口服或鼻内给药时，在缓解过敏性鼻炎症状方面已显示出临床疗效。它被认为通过抗组胺、抗过敏和抗炎机制的组合来改善鼻炎的早期和晚期症状。鼻内给予氮卓斯汀[每侧鼻孔2喷（0.56毫克）]后，症状改善最早在30分钟时就很明显，在季节性过敏性鼻炎（SAR）患者中可持续长达12小时。对鼻塞的影响不一：在一些研究中，客观和/或主观评估显示鼻塞减轻，而在其他研究中则没有改善。每天两次、每侧鼻孔1喷的鼻内氮卓斯汀在减轻鼻炎总体症状方面通常与其他抗组胺药的标准剂量（包括鼻内左卡巴斯汀以及口服西替利嗪、依巴斯汀、氯雷他定和特非那定）效果相同。氮卓斯汀与鼻内皮质类固醇（倍氯米松和布地奈德）的相对疗效仍不清楚。然而，总体而言，皮质类固醇在改善鼻炎症状方面往往比抗组胺药更有效。氮卓斯汀在临床试验和上市后调查中耐受性良好。最常报告的不良事件是苦味、用药部位刺激和鼻炎。氮卓斯汀接受者和安慰剂接受者之间的镇静发生率没有显著差异，初步报告显示常年性过敏性鼻炎（PAR）患者的心血管参数没有显著改变。
每天两次鼻内给予氮卓斯汀为目前推荐用于缓解成人和儿童（在美国年龄≥12岁；在包括英国在内的一些欧洲国家年龄≥6岁）轻至重度SAR和PAR症状的其他抗组胺药提供了一种有效且耐受性良好的替代方案。氮卓斯汀的鼻内制剂显示出起效迅速、局部作用局限和镇静作用减轻的特点，这可能比其他抗组胺药具有优势，尽管这一点尚未得到证实。
