Simpson K, Jarvis B
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 2000 Feb;59(2):301-21. doi: 10.2165/00003495-200059020-00020.
Fexofenadine, the active metabolite of terfenadine, is a selective histamine H1 receptor antagonist that does not cross the blood brain barrier and appears to display some anti-inflammatory properties. Fexofenadine is rapidly absorbed (onset of relief < or = 2 hours) and has a long duration of action, making it suitable for once daily administration. Clinical trials (< or = 2 weeks' duration) have shown fexofenadine 60 mg twice daily and 120 mg once daily to be as effective as loratadine 10 mg once daily, and fexofenadine 120 mg once daily to be as effective as cetirizine 10 mg once daily in the overall reduction of symptoms of seasonal allergic rhinitis. When given in combination, fexofenadine and extended release pseudoephedrine had complementary activity. Fexofenadine was effective in relieving the symptoms of sneezing, rhinorrhoea, itchy nose palate or throat, and itchy, watery, red eyes in patients with seasonal allergic rhinitis. There were often small improvements in nasal congestion that were further improved by pseudoephedrine. Fexofenadine produced greater improvements in quality of life than loratadine to an extent considered to be clinically meaningful, and enhanced patients' quality of life when added to pseudoephedrine treatment. Although no comparative data with other H1 antagonists exist, fexofenadine 180 mg once daily was effective in reducing the symptoms of chronic idiopathic urticaria for up to 6 weeks. Fexofenadine was well tolerated in clinical trials in adults and adolescents and the adverse event profile was similar to placebo in all studies. The most frequently reported adverse event during fexofenadine treatment was headache, which occurred with a similar incidence to that seen in placebo recipients. Fexofenadine does not inhibit cardiac K+ channels and is not associated with prolongation of the corrected QT interval. When given alone or in combination with erythromycin or ketoconazole, it was not associated with any adverse cardiac events in clinical trials. As it does not cross the blood brain barrier, fexofenadine is free of the sedative effects associated with first generation antihistamines, even at dosages of up to 240 mg/day.
fexofenadine is clinically effective in the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria for which it is a suitable option for first-line therapy. Comparative data suggest that fexofenadine is as effective as loratadine or cetirizine in the treatment of seasonal allergic rhinitis. In those with excessive nasal congestion the combination of fexofenadine plus pseudoephedrine may be useful. In clinical trials fexofenadine is not associated with adverse cardiac or cognitive/psychomotor effects.
非索非那定是特非那定的活性代谢产物，是一种选择性组胺H1受体拮抗剂，不会穿过血脑屏障，并且似乎具有一些抗炎特性。非索非那定吸收迅速（缓解起效时间≤2小时）且作用持续时间长，使其适合每日一次给药。临床试验（持续时间≤2周）表明，非索非那定60毫克每日两次和120毫克每日一次与氯雷他定10毫克每日一次效果相当，非索非那定120毫克每日一次与西替利嗪10毫克每日一次在总体减轻季节性变应性鼻炎症状方面效果相当。联合使用时，非索非那定和缓释伪麻黄碱具有互补活性。非索非那定可有效缓解季节性变应性鼻炎患者的打喷嚏、流涕、鼻腭或咽喉瘙痒以及眼睛瘙痒、流泪、发红等症状。鼻塞情况通常有小幅改善，伪麻黄碱可使其进一步改善。非索非那定在改善生活质量方面比氯雷他定有更大改善，达到了临床上有意义的程度，并且在加用伪麻黄碱治疗时可提高患者的生活质量。虽然不存在与其他H1拮抗剂的比较数据，但非索非那定180毫克每日一次在长达6周的时间内可有效减轻慢性特发性荨麻疹的症状。非索非那定在成人和青少年的临床试验中耐受性良好，在所有研究中不良事件谱与安慰剂相似。非索非那定治疗期间最常报告的不良事件是头痛，其发生率与安慰剂接受者相似。非索非那定不抑制心脏钾通道，也与校正QT间期延长无关。单独使用或与红霉素或酮康唑联合使用时，在临床试验中它与任何不良心脏事件均无关联。由于它不穿过血脑屏障，非索非那定没有第一代抗组胺药相关的镇静作用，即使剂量高达240毫克/天。
非索非那定在治疗季节性变应性鼻炎和慢性特发性荨麻疹方面临床有效，是一线治疗的合适选择。比较数据表明，非索非那定在治疗季节性变应性鼻炎方面与氯雷他定或西替利嗪效果相当。对于鼻塞严重的患者，非索非那定加伪麻黄碱联合使用可能有用。在临床试验中，非索非那定与不良心脏或认知/精神运动效应无关。
