Hüther K J, Renftle G, Barraud N, Burke J T, Koch-Weser J
Eur J Clin Pharmacol. 1977 Nov 14;12(3):195-9. doi: 10.1007/BF00609860.
The inhibitory effect of orally administered terfenadine on the area of histamine-induced skin wheals was studied by single dose and multiple dose trials in 12 normal male volunteers. Single doses of 20, 60 and 200 mg of terfenadine produced dose-dependent decreases in histamine wheal area that reached a maximum by the fourth hour after dosing. The 60 and 200 mg doses blocked almost 90% of histamine whealing, and significant reduction of the wheal area persisted for 8 h. During the multiple dose trial histamine whealing was markedly inhibited after the fifth and sixth dose of terfenadine 20, 40 or 60 mg every 8 h and of 60 mg every 12 h. On the last three dosage schedules inhibition persisted for at least 12 h after the final dose. Inhibition of histamine-induced skin whealing appears to be a quantitative index of the time course of histamine H1-receptor antagonist action.
通过对12名正常男性志愿者进行单剂量和多剂量试验，研究了口服特非那定对组胺诱导的皮肤风团面积的抑制作用。单剂量20、60和200毫克特非那定可使组胺风团面积呈剂量依赖性减小，给药后第四小时达到最大效应。60毫克和200毫克剂量可阻断近90%的组胺风团反应，风团面积的显著减小持续8小时。在多剂量试验中，每8小时服用20、40或60毫克特非那定以及每12小时服用60毫克特非那定，在第五和第六次给药后，组胺风团反应受到明显抑制。在最后三种给药方案中，最后一剂后抑制作用至少持续12小时。组胺诱导的皮肤风团反应的抑制似乎是组胺H1受体拮抗剂作用时间过程的定量指标。
