Assessment of the duration of action of terfenadine on histamine induced weals.
In this study we aimed to quantify the reduction in area, perimeter and thickness of histamine induced weals 12, 18 and 24 h after a single oral dose of 120 mg terfenadine. Ten healthy volunteers were given 120 mg of terfenadine or placebo in a double-blind randomized two-period cross-over study. Twenty micrograms of histamine were then injected intradermally at 12, 18, and 24 h. The thickness of the resulting weal was measured by an A-scan pulsed ultrasound device. The area and perimeter of the resulting weal and flare were measured by tracing onto acetate sheets and using a digitizing tablet linked to a microcomputer. Just before each dose of histamine was injected, blood was taken to measure the level of the major metabolite of terfenadine. There was a significant difference between terfenadine 120 mg and placebo in the area and perimeter of the weal and the area and perimeter of the weal and flare at 12, 18 and 24 h, but no significant difference in weal thickness. Thus, terfenadine suppresses the wealing response caused by intradermally injected histamine over a 24 h period. It may be possible, therefore, to use a once daily dose of terfenadine.
D000328:Adult; D001559:Benzhydryl Compounds / Q000627:therapeutic use*; D004311:Double-Blind Method; D005260:Female; D006632:Histamine; D006801:Humans; D008297:Male; D008875:Middle Aged; D011897:Random Allocation; D016593:Terfenadine; D014581:Urticaria / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology
D001559:Benzhydryl Compounds; D016593:Terfenadine; D006632:Histamine