Phillips M J, Meyrick Thomas R H, Moodley I, Davies R J
Br J Clin Pharmacol. 1983 Mar;15(3):277-86. doi: 10.1111/j.1365-2125.1983.tb01500.x.
The effect of ketotifen was compared with that of clemastine and chlorpheniramine, known antihistamines, and sodium cromoglycate, a drug considered to have mast cell "stabilizing' properties on histamine and allergen wealing reactions in human skin, in random order, double-blind, placebo controlled studies. Ketotifen was significantly more potent in the inhibition of both histamine (P less than 0.001) and allergen (P less than 0.001) skin wealing reactions than either clemastine or chlorpheniramine. Sodium cromoglycate had no significant effect on either histamine or allergen skin wealing reactions in any of the concentrations tested. However ketotifen, like clemastine, had a significantly greater inhibitory effect on histamine than on allergen induced weals (P less than 0.001) and both drugs were shown to act as competitive antagonists of histamine. Ketotifen has been shown to be a potent anti-histamine but there is no evidence from these in vivo studies to suggest that it has any additional inhibitory activity on release of mediators from mast cells in human skin.
在随机、双盲、安慰剂对照研究中,将酮替芬与已知的抗组胺药氯马斯汀、氯苯那敏以及色甘酸钠进行了比较。色甘酸钠被认为对人皮肤中的组胺和变应原风团反应具有肥大细胞“稳定”特性。酮替芬在抑制组胺(P<0.001)和变应原(P<0.001)皮肤风团反应方面比氯马斯汀或氯苯那敏显著更有效。在所测试的任何浓度下,色甘酸钠对组胺或变应原皮肤风团反应均无显著影响。然而,酮替芬与氯马斯汀一样,对组胺的抑制作用比对变应原诱导的风团显著更强(P<0.001),且两种药物均表现为组胺的竞争性拮抗剂。已证明酮替芬是一种强效抗组胺药,但这些体内研究没有证据表明它对人皮肤肥大细胞介质释放有任何额外的抑制活性。