Popov T A, Dumitrascu D, Bachvarova A, Bocsan C, Dimitrov V, Church M K
Clinical Centre of Allergology, Medical University, 1, Sv. Georgi Sofiyski St., 1431, Sofia, Bulgaria.
Inflamm Res. 2006 Jun;55(6):241-4. doi: 10.1007/s00011-006-0075-z.
The histamine-induced wheal and flare response was used to compare quantitatively the antihistaminic potency of levocetirizine and desloratadine.
In this double-blind, placebo-controlled crossover study, 24 healthy male non-atopic volunteers received weekly single doses of 1.25, 2.5 or 5 mg levocetirizine, 2.5, 5 or 10 mg desloratadine, or placebo. Four hours after dosing, histamine (100 mg/ml) skin prick tests were performed on the volar surface of both forearms. The diameters of the wheals and flares were measured 10 minutes later. Sedation was evaluated using a visual analogue scale and a motricity test. The effects of individual drug doses were compared using Student's t-test for paired data and the overall effects of the two drugs by ANOVA.
All doses of levocetirizine significantly (P < 0.0001) inhibited both wheals and flares in a dose-related manner. Only the 10 mg dose of desloratadine achieved significant inhibition of response. ANOVA showed levocetirizine to be significantly (P < 0.0001) more active than desloratadine. Neither drug caused significant sedation or loss of motricity.
Levocetirizine is significantly more effective than desloratadine in inhibiting wheal and flare responses to histamine in human skin in vivo, with 1.25 mg levocetirizine being more effective than 10 mg desloratadine.
采用组胺诱发的风团及潮红反应来定量比较左西替利嗪和地氯雷他定的抗组胺效力。
在这项双盲、安慰剂对照的交叉研究中，24名健康非特应性男性志愿者每周接受单剂量的1.25、2.5或5mg左西替利嗪、2.5、5或10mg地氯雷他定或安慰剂。给药4小时后，在双侧前臂掌面进行组胺（100mg/ml）皮肤点刺试验。10分钟后测量风团和潮红的直径。使用视觉模拟评分法和运动功能测试评估镇静作用。采用配对数据的Student t检验比较各药物剂量的效应，并通过方差分析比较两种药物的总体效应。
所有剂量的左西替利嗪均以剂量相关方式显著（P<0.0001）抑制风团和潮红。只有10mg剂量的地氯雷他定对反应有显著抑制作用。方差分析显示左西替利嗪比地氯雷他定活性显著更高（P<0.0001）。两种药物均未引起显著的镇静或运动功能丧失。
在体内抑制人体皮肤对组胺的风团和潮红反应方面，左西替利嗪比地氯雷他定显著更有效，1.25mg左西替利嗪比10mg地氯雷他定更有效。
