Abstract：
UNASSIGNED: Fexofenadine is a second-generation inverse agonist of H1-receptor of histamine which is highly selective with proven efficacy in relieving symptoms associated with allergic conditions. It has an additional benefit of not penetrating the blood-brain barrier and therefore do not induce sedation and not impair the cognitive function/psychomotor performance. This review aimed at providing evidence based on available controlled studies to reinforce the non-sedative property of fexofenadine for treating patients with allergic rhinitis and urticaria.
UNASSIGNED: We performed an electronic literature search using keywords such as fexofenadine, drowsiness, somnolence, sedation, fatigue, cognitive, impairment, psychomotor, driving performances, sleep, rapid eye movement, alertness, clinical study, in vitro study, in vivo study, and pharmacodynamics in the Embase search engine. The review included randomized controlled trials, review articles, systematic reviews, and meta-analyses, together with post-marketing analysis conducted in healthy subjects and patients with allergy and were focused on comparing the antihistaminic potential or safety of fexofenadine with other antihistamines or placebo.
UNASSIGNED: Positron emission tomography (PET) and proportional impairment ratio (PIR) data along with other objective tests from various studies confirmed the non-sedative property of fexofenadine. Results of brain H1-receptor occupancy (H1RO) obtained from PET showed no H1RO by fexofenadine, the receptor which is known to cause sedation of H1 antihistamines. Most studies calculating PIR value as 0 showed fexofenadine to be a non-impairing oral antihistamine regardless of dose. Clinical trials in adults and children showed fexofenadine to be well tolerated without sedative effect or impairment of cognitive/psychomotor function even at higher than recommended doses.
UNASSIGNED: Published literature based on various parameters and clinical trials conducted for evaluating the effect of fexofenadine on sedation and central nervous system shows fexofenadine is both clinically effective and non-sedating.
UNASSIGNED: We performed an electronic literature search using keywords such as fexofenadine, drowsiness, somnolence, sedation, fatigue, cognitive, impairment, psychomotor, driving performances, sleep, rapid eye movement, alertness, clinical study, in vitro study, in vivo study, and pharmacodynamics in the Embase search engine. The review included randomized controlled trials, review articles, systematic reviews, and meta-analyses, together with post-marketing analysis conducted in healthy subjects and patients with allergy and were focused on comparing the antihistaminic potential or safety of fexofenadine with other antihistamines or placebo.
UNASSIGNED: Positron emission tomography (PET) and proportional impairment ratio (PIR) data along with other objective tests from various studies confirmed the non-sedative property of fexofenadine. Results of brain H1-receptor occupancy (H1RO) obtained from PET showed no H1RO by fexofenadine, the receptor which is known to cause sedation of H1 antihistamines. Most studies calculating PIR value as 0 showed fexofenadine to be a non-impairing oral antihistamine regardless of dose. Clinical trials in adults and children showed fexofenadine to be well tolerated without sedative effect or impairment of cognitive/psychomotor function even at higher than recommended doses.
UNASSIGNED: Published literature based on various parameters and clinical trials conducted for evaluating the effect of fexofenadine on sedation and central nervous system shows fexofenadine is both clinically effective and non-sedating.
摘要：
■非索非那定是组胺H1受体的第二代反向激动剂，具有高度选择性，在缓解与过敏状况相关的症状方面具有良好的疗效。它具有不穿透血脑屏障的额外益处，因此不会引起镇静作用，也不会损害认知功能/精神运动表现。这篇综述旨在基于现有的对照研究提供证据，以加强非索非那定治疗过敏性鼻炎和荨麻疹患者的非镇静性。
■我们使用非索非那定等关键词进行了电子文献检索，困倦,嗜睡,镇静,疲劳,认知，减值，精神运动，驾驶表演,睡眠,快速的眼球运动，机敏,临床研究,体外研究，体内研究,和Embase搜索引擎中的药效学。该综述包括随机对照试验，评论文章,系统评价,和荟萃分析，以及在健康受试者和过敏患者中进行的上市后分析，重点是比较非索非那定与其他抗组胺药或安慰剂的抗组胺潜力或安全性。
■正电子发射断层扫描（PET）和比例损伤比（PIR）数据以及各种研究的其他客观测试证实了非索非那定的非镇静特性。从PET获得的脑H1受体占据（S1RO）的结果显示，非索非那定没有S1RO，已知能引起H1抗组胺药镇静作用的受体。大多数计算PIR值为0的研究表明，非索非那定是一种无损害的口服抗组胺药，无论剂量如何。成人和儿童的临床试验表明，即使在高于推荐剂量的情况下，非索非那定也具有良好的耐受性，没有镇静作用或认知/精神运动功能受损。
■基于各种参数和为评估非索非那定对镇静和中枢神经系统的影响而进行的临床试验的已发表文献表明，非索非那定在临床上既有效又不镇静。
■我们使用非索非那定等关键词进行了电子文献检索，困倦,嗜睡,镇静,疲劳,认知，减值，精神运动，驾驶表演,睡眠,快速的眼球运动，机敏,临床研究,体外研究，体内研究,和Embase搜索引擎中的药效学。该综述包括随机对照试验，评论文章,系统评价,和荟萃分析，以及在健康受试者和过敏患者中进行的上市后分析，重点是比较非索非那定与其他抗组胺药或安慰剂的抗组胺潜力或安全性。
■正电子发射断层扫描（PET）和比例损伤比（PIR）数据以及各种研究的其他客观测试证实了非索非那定的非镇静特性。从PET获得的脑H1受体占据（S1RO）的结果显示，非索非那定没有S1RO，已知能引起H1抗组胺药镇静作用的受体。大多数计算PIR值为0的研究表明，非索非那定是一种无损害的口服抗组胺药，无论剂量如何。成人和儿童的临床试验表明，即使在高于推荐剂量的情况下，非索非那定也具有良好的耐受性，没有镇静作用或认知/精神运动功能受损。
■基于各种参数和为评估非索非那定对镇静和中枢神经系统的影响而进行的临床试验的已发表文献表明，非索非那定在临床上既有效又不镇静。
