Hägermark O, Wahlgren C F, Giös I
Department of Dermatology, Karolinska sjukhuset, Stockholm, Sweden.
Skin Pharmacol. 1992;5(2):93-8. doi: 10.1159/000211025.
The inhibitory effect of the two H1 antagonists clemastine and loratadine on histamine release in human skin was studied in 15 volunteers. The antihistamines and placebo were administered orally (clemastine 2 mg twice a day, loratadine 10 mg once a day) for 5 days according to a double-blind, crossover design. Clemastine caused a significant sedation in comparison with placebo, whereas there was no difference between loratadine and placebo in this respect. After 5 days' medication, flare reaction was induced by intradermal injection of histamine and the histamine liberator compound 48/80. The antihistamine dosages were approximately equipotent and inhibited the flare response induced by histamine to about the same extent, whereas the flares induced by compound 48/80 were still more inhibited by both drugs. The results indicate that clemastine and loratadine not only inhibit histamine effects at H1 receptor level, but have additional suppressive effects, probably due to inhibition of mast cell degranulation. The simple, virtually noninvasive, in vivo technique described in this paper does not require chemical analysis of the released mediators and could be used to screen 'mast cell stabilizing' effects of various antihistamines.
在15名志愿者中研究了两种H1拮抗剂氯马斯汀和氯雷他定对人皮肤中组胺释放的抑制作用。按照双盲、交叉设计，将抗组胺药和安慰剂口服给药（氯马斯汀2毫克，每日两次；氯雷他定10毫克，每日一次），持续5天。与安慰剂相比，氯马斯汀引起了显著的镇静作用，而在这方面氯雷他定与安慰剂之间没有差异。用药5天后，通过皮内注射组胺和组胺释放剂化合物48/80诱发风团反应。两种抗组胺药的剂量大致等效，并且对组胺诱发的风团反应的抑制程度大致相同，而两种药物对化合物48/80诱发的风团反应的抑制作用仍然更强。结果表明，氯马斯汀和氯雷他定不仅在H1受体水平抑制组胺作用，而且具有额外的抑制作用，可能是由于抑制肥大细胞脱颗粒所致。本文所述的简单、几乎无创的体内技术不需要对释放的介质进行化学分析，可用于筛选各种抗组胺药的“肥大细胞稳定”作用。
