Meltzer Eli O, Gillman Sherwin A
Allergy and Asthma Medical Group and Research Center, University of California at San Diego, San Diego, California, USA.
Allergy Asthma Proc. 2007 Jan-Feb;28(1):67-73. doi: 10.2500/aap.2007.28.2895.
To date, no published articles exist comparing the H1-receptor antagonist activities of fexofenadine and desloratadine using the histamine-induced skin wheal-and-flare model. The aim of this study was to compare the efficacy of fexofenadine versus desloratadine in suppressing histamine-induced skin flares and wheals in adults and adolescents. This was a two-center, randomized, placebo-controlled, complete-crossover study. Subjects were administered either single-dose fexofenadine HCl, 180 mg; desloratadine, 5 mg; or placebo and their response to skin-prick testing with histamine and diluent was recorded at predetermined time intervals. The primary end point was change in size of histamine-induced summation skin flares. Secondary end points included change in skin wheal summation measurements, onset, duration, maximum percent suppression, and time to maximum suppression of flares and wheals. Fexofenadine suppressed skin flares significantly more than desloratadine from 2 to 6 hours, and wheals from 2 to 4 hours, 6 to 9 hours, and 12 hours posttreatment. In addition, fexofenadine suppressed flares more than placebo at all time points from 2 to 24 hours and wheals more than placebo at all time points from 2 to 12 hours posttreatment. Desloratadine suppressed flares significantly more than placebo from 6 to 10 hours and at 12 and 24 hours but suppressed wheals significantly versus placebo only at 10 hours. Fexofenadine had a faster onset of flare suppression than desloratadine (1 hour versus 5 hours) and an equally rapid onset of wheal suppression. Fexofenadine HCl, 180 mg, was superior to desloratadine, 5 mg, in histamine-induced wheal-and-flare suppression, suggesting increased in vivo H1-receptor antagonist potency of fexofenadine versus desloratadine.
迄今为止，尚无已发表的文章使用组胺诱导的皮肤风团和潮红模型比较非索非那定和地氯雷他定的H1受体拮抗剂活性。本研究的目的是比较非索非那定与地氯雷他定在抑制成人和青少年组胺诱导的皮肤潮红和风团方面的疗效。这是一项双中心、随机、安慰剂对照、完全交叉研究。受试者分别接受单剂量180毫克盐酸非索非那定、5毫克地氯雷他定或安慰剂，并在预定时间间隔记录他们对组胺和稀释剂皮肤点刺试验的反应。主要终点是组胺诱导的总皮肤潮红大小的变化。次要终点包括皮肤风团总和测量的变化、起效时间、持续时间、最大抑制百分比以及潮红和风团达到最大抑制的时间。治疗后2至6小时，非索非那定对皮肤潮红的抑制作用明显强于地氯雷他定；在治疗后2至4小时、6至9小时和12小时，对风团的抑制作用也强于地氯雷他定。此外，在治疗后2至24小时的所有时间点，非索非那定对潮红的抑制作用均强于安慰剂；在治疗后2至12小时的所有时间点，对风团的抑制作用也强于安慰剂。地氯雷他定在6至10小时、12小时和24小时对潮红的抑制作用明显强于安慰剂，但仅在10小时对风团的抑制作用明显强于安慰剂。非索非那定对潮红抑制的起效时间比地氯雷他定快（1小时对5小时），对风团抑制的起效时间同样迅速。180毫克盐酸非索非那定在组胺诱导的风团和潮红抑制方面优于5毫克地氯雷他定，表明非索非那定相对于地氯雷他定的体内H1受体拮抗剂效力增强。
