新型非镇静性抗组胺药特非那丁

特非那丁是一种安全性高的外周H_1受体拮抗剂,用来治疗变应性鼻炎,过敏性皮肤疾病等症。由于不通过血脑屏障,无中枢抑制作用,因而不产生嗜睡,倦怠等副反应。本文综述了它的药理、毒理、药物动力学和临床等方面的研究进展。     

特非那丁治疗146例过敏性和瘙痒性皮肤病的对照试验

特非那丁治疗急、慢性荨麻疹,湿疹,虫咬皮炎和瘙痒症146例。男73例,女73例,年龄38±17yr。用阿司咪唑105例和赛庚啶91例作对照。特非那丁60mg,bid,po;阿司咪唑10mg,qn,po;赛庚啶2mg-4mg,tid,po。6d为一个疗程。特非那丁疗效高于2个对照组(P<0.05)。特非那丁还具有疗效快,疗程短和副作用小的优点。     

特非那定片的含量测定方法

目的：测定特非那定片中特非那定的含量。方法：一阶导数分光光度法。结果：本法的平均回收率101．5％,RSD为0．51％。结论：本法精密,简单,准确。     

特非那定合成工艺改进

特非那定是哌啶类抗组胺药，具有特异的外周H1受体拮抗作用，有抗5-羟色胺的作用，它是无中枢抑制作用、无镇静作用而高效安全的新型组胺受体H1拮抗剂，为目前临床上常用的抗过敏药物，主用于过敏性鼻炎，急慢性荨麻疹，枯草热的治疗。     

特非那丁在抗哮喘方面的应用

新型非镇静性抗组胺药特非那丁,对组胺和花粉、超声波雾化蒸馏水、高渗盐水、冷空气过度换气刺激等过敏原引起的支气管狭窄,运动引起的哮喘有显著保护作用,可减少FEV_1下降,增加PEFR,改善哮喘症状。     

特非那定的心血管不良反应

特非那定（Ｔｅｒｆｅｎａｄｉｎｅ）为一广谱、高效抗组胺药。现就其对心血管系统的不良反应综述如下。１特非那定对心血管系统的不良反应１．１能抑制肝微粒体酶的药物可干扰特非那定的代谢，造成特非那定原药在体内蓄积中毒，即使严格按照治疗剂量使用，严重的心律失常...     

Inhibitory activity of terfenadine on histamine-induced skin wheals in man

Summary 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.     

Effects of azatadine maleate on subjective appraisal and psychomotor functions relevant to driving performance

Summary

Studies were carried out in normal healthy male subjects to assess the effects on psychomotor functions and subjective ratings of performance after acute administration of azatadine maleate, a potent antihistamine with additional antiserotonin activity. In the first trial, 2?mg azatadine was compared with another new antihistamine Sch 12169 (2?mg) and placebo. In a second trial, higher doses of azatadine (4?mg and 8?mg) were compared with dexchlorpheniramine (4?mg) and placebo. Both trials were of a double-blind, randomized Latin square design and subjects were assessed using a battery of tests, after administration of each trial drug. The time and sequence of tests were standardized, with a 1-week interval between test sessions. The results showed that azatadine did not produce significant impairment of psychomotor function at either the standard 2?mg or the maximum recommended 4?mg per day dosage level. Performance was only significantly impaired, compared with that after placebo, at the 8?mg dose level and was of a similar order to that observed after dexchlorpheniramine at the usual 4?mg dosage. It is suggested, therefore, that at the normal recommended dosage of 2?mg per day, azatadine is not likely to impair driving ability.     

Comparison of the central and peripheral effects of cetirizine and terfenadine

Summary The peripheral and central effects of 10 mg cetirizine 2 HCl and 60 mg terfenadine have been compared with placebo in 9 healthy male volunteers.The peripheral effect, in terms of cutaneous reactivity to 1 µg histamine i.d., was measured by planimetry of the wheal and erythemas. Central effects were assessed with a self-evaluation visual scale and from the results of electroencephalographic spectrum analysis. Peripheral inhibition of histamine reactivity was more intense and quicker for cetirizine than for terfenadine. On the self-evaluation scale, no significant difference between terfenadine, cetirizine and placebo was noted. The quantified EEG did not show any variation in spectral parameters at any time after cetirizine. By contrast, at 6 h terfenadine had increased slow waves and had inhibited the alpha band. Thus, 10 mg cetirizine 2 HCl had less effect on the central nervous system than terfenadine 60 mg, whilst its peripheral action appeared more quickly and was more intense.     

西替利嗪抑制组胺诱导角质形成细胞IL-8表达

目的:考察西替利嗪对组胺诱导角质形成细胞系HaCaT细胞IL-8表达的影响。方法:采用RT-PCR方法研究组胺H1受体mRNA表达,组胺及西替利嗪对IL-8mRNA表达的调节作用,并用ELISA法对分泌的IL-8进行定量。结果:HaCaT细胞有组胺H1受体mRNA表达,(1×10-5)mol/L组胺刺激细胞5h,显著增强IL-8mRNA表达;(1×10-6)-(1×10-4)mol/L组胺作用细胞24h则显著地诱导了IL-8产生;1×10-6、1×10-5mol/L西替利嗪抑制了组胺的诱导作用。结论:西替利嗪可通过抑制组胺诱导HaCaT细胞IL-8表达而具有H1受体依赖的抗炎作用。     

五步蛇毒对大鼠海马组胺受体H_1 mRNA和蛋白质表达的影响

目的研究五步蛇毒对大鼠海马组胺受体H1mRNA及蛋白质表达的影响。方法用半定量RT-PCR和Western blot方法,检测腹腔注射五步蛇毒后不同时相大鼠海马组胺受体H1mRNA及蛋白质表达的变化。结果五步蛇毒处理后,大鼠海马组胺受体H1mRNA及蛋白质的表达在各时相点均发生变化,且其mRNA和蛋白质表达均为先下调后上调。结论五步蛇毒对大鼠脑区海马组胺H1受体mRNA和蛋白质表达都有影响。H1受体mRNA和蛋白质表达的改变对大脑的生理功能有一定的影响,可能是该蛇毒致脑功能障碍的分子基础之一。     

抗组胺药敏感性的细胞色素P450研究进展

HP450具有细胞色素P450特征和抗组胺药敏感的双重性,它在不同的大鼠肝脏疾病模型中有明显的变化规律,与肝脏疾病的发展具有一定的相关性,在肝癌发生过程中HP450基因的转录及表达均发生了变化。HP450有可能作为诊断肝癌的新指标,在预防和治疗肝癌中可能作为一个新靶点。     

西替利嗪干预组胺诱导的真皮成纤维细胞IL-8和MCP-1产生

目的　探讨真皮成纤维细胞组胺H1 受体(histamineH1 receptor,H1R)表达及西替利嗪(cetirizine,CET)对组胺(histamine,HIS)诱导炎症因子的干预作用,寻找CET抗皮肤过敏炎症的作用靶点。方法　采用RT- PCR和免疫组化技术检测真皮成纤维细胞H1RmRNA和蛋白表达;用HIS处理细胞为模型组,ELISA检测HIS诱导IL 8和MCP -1的蛋白分泌及CET的干预作用。结果　真皮成纤维细胞有H1RmRNA和蛋白表达; 10-6 ~10-4 mol·L-1 HIS显著地诱导了真皮成纤维细胞IL -8蛋白分泌(P<0 .05vs对照组),10-5 mol·L-1 HIS明显地诱导了MCP 1分泌(P<0 .01vs对照组),加入10-6、10-5 mol·L-1 CET共同培养24h,抑制了HIS诱导的IL- 8和MCP -1表达(P<0 .05vs模型组)。结论　CET可能通过抑制真皮成纤维细胞趋化因子的表达而发挥抗皮肤过敏炎症作用。     

润燥止痒胶囊联用组胺H1受体拮抗剂治疗老年皮肤瘙痒症的Meta分析

目的 系统评价润燥止痒胶囊联用组胺H1受体拮抗剂治疗老年皮肤瘙痒症的临床疗效和安全性,为临床推广提供理论依据。方法 计算机检索PubMed、Medline、中国生物医学文献数据库（CBM）、中国学术期刊全文数据库（CNKI）、维普中文科技期刊数据库（VIP）、万方数据库,收集润燥止痒胶囊联用组胺H1受体拮抗剂与单用组胺H1受体拮抗剂治疗老年皮肤瘙痒症临床随机对照研究,采用RevMan 5.2软件进行Meta分析。结果 共纳入18项研究,2 003例患者。Meta分析结果显示,与单用组胺H1受体拮抗剂,润燥止痒胶囊联用组胺H1受体拮抗剂能显著提高的临床有效率[RR=1.45,95% CI （1.36,1.54）,P<0.01],降低瘙痒程度评分[MD=-2.83,95% CI （-3.51,-2.15）,P<0.01]、瘙痒持续时间[MD=-2.14,95% CI （-2.49,-1.79）,P<0.01]、瘙痒发作频率[MD=-2.39,95% CI （-2.81,-1.96）,P<0.01]、瘙痒面积[MD=-1.60,95% CI （-1.94,-1.26）,P<0.01]和继发皮损评分[MD=-1.87,95% CI （-2.48,-1.27）,P<0.01]和ADR发生率[RR=0.67,95% CI （0.52,0.88）,P<0.01]。结论 润燥止痒胶囊联用组胺H1受体拮抗剂治疗老年皮肤瘙痒症的临床疗效优于单用组胺H1受体拮抗剂。     

纳多洛尔治疗高血压病20例

本文对原发性高血压患者(男8例,女12例;年龄41±SD7yr)采用纳多洛尔口服40mg/d,2mo为一个疗程。总有效率90％,收缩压平均下降值为3.5±2.4kPa,舒张压平均下降值为2.3±1.2kPa;治疗前、后比较P值均<0.01。副作用轻微,剂量减少或停药后可减轻或消失。