Central effects of fexofenadine and cetirizine:: Measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography
Central effects of fexofenadine and cetirizine:: Measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography
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DOI：
10.1177/0091270004267590
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发表时间：
2004-08-01
影响因子：
2.9
通讯作者：
Yanai, K
中科院分区：
文献类型：
--
作者：
Tashiro, M;Sakurada, Y;Yanai, K
组胺H1受体（H1 R）拮抗剂，或抗组胺药，经常诱导镇静副作用时，用于治疗过敏性疾病。本研究使用3种不同标准比较了第二代抗组胺药非索非那定和西替利嗪的镇静作用：通过斯坦福大学嗜睡量表评估的主观嗜睡、客观心理测试（4种不同暴露持续时间的简单和选择反应时间测试和视觉辨别测试）以及脑中组胺H1受体占用率（H1 RO）的测量。在一项双盲、安慰剂对照交叉研究中，在基线和非索非那定120 mg或西替利嗪20 mg给药后90分钟，对20名健康日本志愿者的主观嗜睡和精神状态进行了测量。包括羟嗪30 mg作为阳性对照。使用正电子发射断层扫描（PET）与C-11-多塞平在20名受试者中的12人，并招募了另外11名志愿者作为对照。在精神病学测试中，非索非那定与安慰剂无显著差异，在某些任务上的损害显著低于西替利嗪，在所有任务上的损害显著低于羟嗪。对于主观嗜睡，非索非那定与安慰剂没有显著差异，而西替利嗪与非索非那定和安慰剂相比显示出嗜睡增加的趋势。非索非那定组的H1 RO可忽略不计（-0.1%），但西替利嗪组的H1 RO中等偏高（26.0%）。总之，通过H1 RO和精神病学测试评估，非索非那定120 mg与西替利嗪20 mg可区分。
Histamine H1-receptor (H1R) antagonists, or antihistamines, often induce sedative side effects when used for the treatment of allergic disorders. This study compared the sedative profiles of the second-generation antihistamines, fexofenadine and cetirizine, using 3 different criteria: subjective sleepiness evaluated by the Stanford Sleepiness Scale, objective psychomotor tests (simple and choice reaction time tests and visual discrimination tests at 4 different exposure durations), and measurement of histamine H1-receptor occupancy (H1RO) in the brain. Subjective sleepiness and psychomotor performance were measured in 20 healthy Japanese volunteers at baseline and 90 min after administration of fexofenadine 120 mg or cetirizine 20 mg in a double-blind, placebo-con trolled crossover study. Hydroxyzine 30 mg was included as a positive control. H1RO was measured using positron emission tomography (PET) with C-11-doxepin in 12 of the 20 subjects, and a further 11 volunteers were recruited to act as controls. In psychomotor tests, fexofenadine was not significantly different from placebo and significantly less impairing than cetirizine on some tasks, as well as significantly less impairing than hydroxyzine on all tasks. For subjective sleepiness, fexofenadine was not significantly different from placebo, whereas cetirizine showed a trend toward increased sleepiness compared with fexofenadine and placebo. H1RO was negligible with fexofenadine (-0.1%) but moderately high with cetirizine (26.0%). In conclusion, fexofenadine 120 mg is distinguishable from cetirizine 20 mg, as assessed by H1RO and psychomotor testing.