盐酸司他斯汀对湿疹患者脑组胺受体占有率的影响  

Effect of stastatin hydrochloride on brain histamine receptor occupancy in patients with eczema

作　　者：周自广[1] 宋云焕[1] ZHOU Zi-guang;SONG Yun-huan(The Medical Group of Zhengzhou First People's Hospital,Zhengzhou 450004,China)

机构地区：[1]郑州市第一人民医院

出　　处：《中国新药杂志》2019年第22期2741-2745,共5页Chinese Journal of New Drugs

摘　　要：目的:了解盐酸司他斯汀对湿疹患者脑组胺H1受体(H1R)占有率的影响。方法:收集2018年1月-2018年5月本院经治湿疹患者10例,按照盲法原则给予受试者盐酸司他斯汀(1 mg)、非索非那定(60 mg)或乳酸菌素片(6 mg,安慰剂)。每人给药3次,交叉药物之间洗脱时间≥7 d。在给药前及给药后30,60,120和180 min分别检测相应血药浓度,使用斯坦福嗜睡量表(SSS)测量每例受试者的主观嗜睡情况。口服给药后90 min,向每例受试者静脉注射含有11C多塞平的生理盐水,60 min后进行PET扫描。分析PET影像,得到各大脑皮质区的结合电位比(BPR)及H1R占有率(H1RO)。将获得的各项数据进行对比分析。结果:盐酸司他斯汀的BPR与非索非那定及安慰剂的BPR比较无统计学差异。盐酸司他斯汀、非索非那定及安慰剂在颞皮质(TPL)、额叶皮质(FRL)、枕叶皮质(OCL)、顶叶皮质(PRL)、前扣带回(ACG)、后扣带回(PCG)及整体皮质区域的BPR未见明显整体及组间差异。盐酸司他斯汀在OCL,PRL皮质的H1RO高于非索非那定(P<0.05)。盐酸司他斯汀血药浓度峰值[(0.408±0.007)μmol·L-1]高于非索非那定[(0.112±0.010)μmol·L-1],差异有统计学意义(P<0.05)。H1RO与盐酸司他斯汀及非索非那定血药浓度无统计学相关性。给药30,60,120和180 min后,盐酸司他斯汀和非索非那定的SSS评分均无统计学差异[(0.23±0.01)vs(0.24±0.02)分]。主观嗜睡(SSS评分)与盐酸司他斯汀及非索非那定血药浓度无统计学相关性。结论:盐酸司他斯汀属于非镇静性抗组胺药,在治疗剂量下不会结合脑H1R而引起显著的镇静作用。Objective:To investigate the effect of stastatin hydrochloride on the histamine H1 receptor(H1R)occupancy in patients with eczema.Methods:Ten patients with eczema treated in our hospital from January2018 to May 2018 were enrolled.The subjects were given stastatin hydrochloride(1 mg),fexofenadine(60 mg)or lactic acid bacteria tablets(6 mg,placebo)according to the principle of blinding.Each person was administered for 3 times,and the washout period between the drugs was≥7 days.The corresponding plasma drug concentrations were measured before and at 30,60,120,and 180 min after administration,and the subjective sleepiness of each subject was measured using the Stanford Sleepiness Scale(SSS).Ninety minutes after oral administration,physiological saline containing11 C-doxepin was intravenously administered to each subject,and PET scan was performed 60 min later.Analysis of PET images revealed binding potential ratio(BPR)and H1R occupancy(H1RO)in each cerebral cortex.The data was compared and analyzed.Results:There was no significant difference in BPR between stastatin hydrochloride,fexofenadine and placebo.There were no significant overall and intergroup differences in BPR of TRAS,FRL,OCL,PRL,ACG,PCG,and the overall cortical area of stastatin hydrochloride,fexofenadine,and placebo.The H1RO of stastatin hydrochloride in the OCL and PRL cortex was higher than that of fexofenadine(P<0.05).The peak plasma concentration of stastatin hydrochloride(0.408±0.007μmol·L-1)was higher than that of fexofenadine(0.112±0.010μmol·L-1)(P<0.05).There was no significant correlation between H1RO and stastatin hydrochloride and fexofenadine plasma concentrations.There were no significant differences in the SSS scores of stastatin hydrochloride(0.23±0.01)and fexofenadine(0.24±0.02)at 30,60,120,and 180 min.There was no significant correlation between subjective sleepiness(SSS score)and plasma concentrations of stastatin hydrochloride and fexofenadine.Conclusion:Stastatin hydrochloride is a non-sedating antihistamine drug that does n

关 键 词：盐酸司他斯汀 非索非那定 脑 组胺比受体 占有率 

分 类 号：R976[医药卫生—药品]