Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

H1 receptor:10 nM-19 nM

在甩尾试验中,腹腔注射12.5 mg/kg Hydroxyzine降低吗啡在大鼠体内的镇痛作用而腹腔注射50 mg/kg Hydroxyzine加强吗啡的作用.500 μM Hydroxyzine使稳态的依托泊苷浓度明显降低2倍,在Sprague-Dawley大鼠体内的稳态浓度达到0.055 μM/mL.

0.1 mM Hydroxyzine抑制实验性变应性脑脊髓炎Lewis大鼠体内50%的EAE恶化,且抑制70%肥大细胞脱颗粒作用。10 μM Hydroxyzine在预处理的膀胱切片中经过60分钟,抑制34%的10 μM的卡巴胆碱诱导的5-羟色胺释放,1 μM抑制25%,0.1 μM抑制17%。500 μM Hydroxyzine明显增加空肠外翻囊中依托泊苷到浆膜部位的运输。Hydroxyzine明显降低空肠和回肠中大约2.4 μg/mL的依托泊苷流出。