地氯雷他定药理作用及机制研究进展

随着工业化的发展,过敏性疾病是一个日益增加的世界性问题,如过敏性鼻炎、慢性特发性荨麻疹等。现已阐明,组胺是各种过敏性疾病的主要介质,因而抗组胺药是目前治疗过敏性疾病的一线用药。     

新型抗组胺药去脂氯雷他定的药理与临床

Ｈ１ 受体拮抗药是一类广泛用于治疗过敏性疾病的药物 ,尤其对过敏性鼻炎和荨麻疹疗效显著。此类药物的作用机制是阻断了平滑肌突触后膜上组胺对Ｈ１ 受体的作用 ,因而可降低血管通透性 ,减少渗出和消除水肿 ;同时也能阻止组胺对Ｃ类痛觉神经纤维上Ｈ１ 受体的作用 ,因而可减轻痒感和打喷嚏症状 ［１］。第一代抗组胺药于２０世纪６０年前问世。然而 ,这些早期的药物可产生明显的中枢反应 (如嗜睡和精神运动性协调障碍 ) ,这主要是由于它们易透过血脑屏障［１］。在新的抗组胺药物研究进程中 ,主要方向是提高药效和减少副作用。人们对无明显…     

地氯雷他定治疗慢性荨麻疹

我科于2003年6月～12月采用地氯雷他定（商品名：芙必叮,海南普利制药有限公司生产）治疗慢性荨麻疹,疗效满意,现将资料完整的66例报告如下。     

地氯雷他定治疗SAR和CIU的研究进展

变应性鼻炎和荨麻疹的发病机制复杂，其中组胺起主要作用，组胺在靶组织能结合H1组胺受体。因而，H1抗组胺药成为治疗这些疾病的主要药物。第一代H1抗组胺药如扑尔敏和苯海拉明能缓解变异性鼻炎和荨麻疹症状，但在治疗剂量下有中枢神经系统(CNS)影响如镇静、精神活动损害和胆碱能副反应。第二代药物如氯雷他定、西替利嗪、阿司咪唑和特非那丁显示较少的镇静和胆碱能副作用。但后2种药物有心血管副作用.     

枸地氯雷他定片与氯雷他定片治疗慢性荨麻疹的疗效比较及安全性分析

目的:分析比较枸地氯雷他定片与氯雷他定片治疗慢性荨麻疹的疗效及安全性.方法:选择120例慢性荨麻疹患者作为研究对象,随机分为对照组和观察组,每组60例;观察组给予枸地氯雷他定片口服治疗,对照组给予氯雷他定片口服治疗,均连续服用28d;比较两组用药前及28d后临床症状评分(TSS)并评价疗效,记录治疗期间药物不良反应的发生情况.结果:两组治疗后TSS评分均较治疗前显著降低,治疗后观察组TSS评分显著低于对照组,差异有统计学意义(P<0.05);观察组治疗有效率为90.00%,显著高于对照组的71.67%,差异具有统计学意义(P<0.05);观察组不良反应发生率为5.00%,对照组不良反应发生率为8.33%,两组比较无显著差异(P>0.05).结论:枸地氯雷他定片较氯雷他定片在缓解慢性荨麻疹临床症状上效果更佳,具有良好的安全性,是治疗慢性荨麻疹的优良选择.     

地氯雷他定治疗慢性荨麻疹临床观察

目的 观察地氯雷他定治疗慢性荨麻疹( chronic urticaria)的临床疗效及安全性.方法 将92例慢性荨麻疹患者随机分为治疗组和对照组,各46例.治疗组口服地氯雷他定片5 mg,1次/d,连续治疗28 d;对照组口服西替利嗪片10 mg,1次/d,连续治疗28 d.采用症状和体征总积分法评估疗效.结果 治疗后第28天,治疗组痊愈率和总有效率分别为82.61％和95.65％,对照组痊愈率和总有效率分别为60.87％和80.43％,两组疗效比较差异有统计学意义(Uc=6.0922,P=0.0136).治疗组1例患者出现嗜睡,对照组16例出现嗜睡,两组不良反应发生率比较差异有统计学意义(x2=14.5607,P＜0.01).结论 地氯雷他定治疗慢性荨麻疹是安全有效的.     

探讨枸地氯雷他定治疗慢性荨麻疹的临床观察

目的探讨对慢性荨麻疹患者采用枸地氯雷他定的临床效果。方法随机选取我院皮肤科于2013年6月至2014年6月收治慢性荨麻疹患者50例,分为研究组(枸地氯雷他定治疗)与对照组(氯雷他定片治疗),各25例;观察与比较两组的临床疗效及不良反应发生情况。结果研究组治疗的总有效率为92.00%,与对照组的72.00%,具有高度统计意义(P<0.05);两组患者的不良反应发生率差异无统计学意义(P>0.05)。结论对慢性荨麻疹患者采用枸地氯雷他定治疗,能有效改善患者的瘙痒症状及促进风团消退,疗效显著,值得推广。     

氯雷他定与西替利嗪治疗慢性荨麻疹的对比观察

为进一步科学地评价氯雷他定（商品名：开瑞坦）和西替利嗪（商品名：西可韦）治疗慢性荨麻疹的疗效和安全性。我科于2003-01—2004—05采用随机双盲、平行对照比较氯霄他定和西替利嗪治疗慢性荨麻疹的疗效和安全性。现总结报告如下：     

复方甘草酸苷联合地氯雷他定治疗慢性荨麻疹及对血浆组胺影响的临床观察

慢性荨麻疹是临床常见病、多发病,病程较长,反复发作,其根本治疗是除去病因.但由于本病病因复杂,单纯使用抗组胺药物往往难以彻底治愈.2010年6月至2011年2月,采用复方甘草酸苷联合地氯雷他定治疗慢性荨麻疹53例,报告如下.     

Review of desloratadine for the treatment of allergic rhinitis,chronic idiopathic urticaria and allergic inflammatory disorders

Desloratadine is a once-daily, non-sedating, non-impairing, selective histamine H₁-receptor antagonist. It relieves the symptoms of seasonal allergic rhinitis (including nasal obstruction and congestion, and morning symptoms), perennial allergic rhinitis and chronic idiopathic urticaria by blocking multiple critical steps in the systemic allergic cascade and downregulating key allergy-induced inflammatory mediators. It also relieves asthma symptoms and decreases rescue medication use in patients with seasonal allergic rhinitis and comorbid asthma. Numerous clinical studies have demonstrated that desloratadine is safe, well tolerated and free of serious cardiac effects. Pharmacokinetic studies have demonstrated a low propensity for drug–drug or drug–food interactions. This review outlines the mechanism of action, efficacy and safety of desloratadine for the treatment of allergic inflammatory disorders.     

非索非那定治疗季节性过敏性鼻炎和慢性特发性荨麻疹的疗效和安全性研究

目的:观察非索非那定治疗季节性过敏性鼻炎和慢性特发性荨麻疹的疗效和安全性。方法:采用双盲、双模拟、随机、对照的方法,对非索非那定60mg,2次/d治疗季节性过敏性鼻炎和慢性特发性荨麻疹进行Ⅱ期临床试验,疗程分别为14d和28d;对照药为西替利嗪10mg,1次/d。结果:季节性过敏性鼻炎共入组144例,非索非那定组和西替利嗪组纳入符合方案集者分别为64和68例,非索非那定组症状积分下降指数(SSRI)为0.719±0.182,总有效率为85.94%,与西替利嗪组比差异均有统计学意义(P<0.05)。慢性特发性荨麻疹共入组144例,2组纳入符合方案集者分别为67和68例,非索非那定组SSRI为0.771±0.269,总有效率为80.60%,与西替利嗪组比差异均无统计学意义(P>0.05)。非索非那定组和西替利嗪组均无严重不良事件,2组分别有25例(17.6%)和24例(16.9%)发生不良反应,差异无统计学意义(P>0.05)。2组不良反应的表现相似,主要为困倦和口干。2组用药后的心电图均未见有临床意义的改变,用药后的QT间期(QTc)与用药前比无统计学差异(P>0.05)。结论:非索非那定为治疗季节性过敏性鼻炎和慢性特发性荨麻疹的安全有效的药物。     

地洛他定片治疗变应性鼻炎随机双盲临床试验

目的 观察地洛他定片（抗变态反应性鼻炎药）治疗变应性鼻炎的疗效及安全性.方法 随机双盲对照临床试验,试验组36人,每日口服地洛他定片1次,每次1片（5 mg）;对照组32人,每日口服氯雷他定片1次,每次1片（10 mg）,疗程均为2周.观察治疗前后2组的疗效和药物不良反应.结果 有效率：试验组为94.44%,对照组90.62%,差异无显著性（P＞0.05）;药物不良反应发生率分别为8.33%和9.37%,也无显著性差异.结论 地洛他定片治疗变应性鼻炎安全、有效.     

Pharmacology and clinical efficacy of desloratadine as an anti-allergic and anti-inflammatory drug

Desloratadine is a biologically active metabolite of the second-generation antihistamine loratadine. Desloratadine is a highly selective peripheral H₁ receptor antagonist that is significantly more potent than loratadine. Results of in vitro and in vivo studies have suggested that desloratadine has anti-allergic effects that are unrelated to its ability to antagonise the effects of histamine. Desloratadine inhibits the expression of cell adhesion molecules, inhibits the generation and release of inflammatory mediators and cytokines, attenuates eosinophil chemotaxis, adhesion and superoxide generation. Studies in animals indicate that desloratadine does not cross the blood-brain barrier and therefore does not cause sedation and does not impair cognition or psychomotor performance. Desloratadine has an excellent overall safety profile. It has no effect on QRS and QT_c intervals and does not cause arrhythmias. Desloratadine is not associated with any significant changes in gastrointestinal function. In clinical studies, oral desloratadine is rapidly absorbed and bioavailability is not affected by ingestion with food or grapefruit juice. The half-life of desloratadine in humans is 27 h; the linear kinetic profile is unaltered by race or gender. Desloratadine is not a substrate for P-glycoprotein or organic anion transport polypeptide and the drug does not appear to be metabolised to a significant extent by the cytochrome P450 CYP3A4 pathway. It therefore may be safely administered with ketoconazole, erythromycin, fluoxetine, or azithromycin. Clinically, desloratadine effectively controls both nasal and non-nasal symptoms of seasonal allergic rhinitis (SAR), including nasal congestion. Desloratadine also provides significant relief of SAR symptoms in patients with co-existing asthma and is effective in the treatment of chronic idiopathic urticaria. Desloratadine improves quality of life and is well-tolerated.     

地洛他定治疗过敏性鼻炎114例的临床疗效和安全性评价

目的 :评价地洛他定治疗过敏性鼻炎的临床疗效和安全性。方法 :采用多中心、随机、双盲、阳性药物平行对照研究。入选过敏性鼻炎病人 2 4 0例 ,完成 2 2 4例 ,其中地洛他定组 114例 ,男性 5 5例 ,女性 5 9例 ,年龄 (4 0±s 7)a ,病程 (6 6± 9)mo ,服用地洛他定 ,5mg,po ,qd ;氯雷他定组 110例 ,男性 4 5例 ,女性 6 5例 ,年龄 (39± 7)a ,病程 (6 3± 8)mo ,予氯雷他定 ,10mg,po ,qd。 2组疗程均为2wk ,观察 2组疗效和不良反应。结果 :地洛他定用于治疗过敏性鼻炎 2wk后的显效例数和有效率分别为 4 6例和 92 .1% ,氯雷他定组的显效例数和有效率分别为 32例和 88.2 %。 2组疗效差异无显著意义 (P >0 .0 5 )。 2组均未出现严重及预料之外的不良反应 ,地洛他定组和氯雷他定组的不良反应发生率分别为 8.3%和 15 .0 % ,P >0 .0 5。结论 :地洛他定治疗过敏性鼻炎具有明显疗效 ,不良反应轻微     

盐酸奥洛他定片治疗慢性特发性荨麻疹疗效和安全性的多中心临床研究

目的：观察盐酸奥洛他定片治疗慢性特发性荨麻疹的临床疗效及安全性。方法：采用随机、双盲双模拟、阳性药物平行对照、多中心的试验方法,试验组和对照组共纳入150例。分别采用盐酸奥洛他定片,每次1片,每日2次;氯雷他定片,每次1片,每日1次,2组分别给予盐酸奥洛他定和氯雷他定模拟片,连续给药4周。疗程结束时以症状体征总积分下降指数、总有效率及疾病总体改善情况等来评估其临床疗效,以不良事件及不良反应、实验室检查来评估其安全性。结果：纳入符合方案分析集（PPS）的病例数为143例,试验组72例,对照组71例。总有效率分别为83.33%和80.28%（P>0.05）。25例患者发生43例次不良事件（试验组14人20例次,对照组11人23例次）,其中37例次不良事件与药物相关,主要表现为口干、头晕、嗜睡、乏力、上腹痛、谷丙转氨酶ALT升高、谷草转氨酶AST升高等。2组间不良事件及不良反应发生率差异无统计学意义（P>0.05）,无严重不良事件发生。结论：盐酸奥洛他定片治疗慢性特发性荨麻疹,疗效显著,安全性好。     

Exploring the real-world profile of refractory and non-refractory chronic idiopathic urticaria in the USA: clinical burden and healthcare resource use

Introduction: Chronic idiopathic/spontaneous urticaria (CIU/CSU) is a debilitating skin condition that is burdensome for patients and healthcare providers. We aimed to describe clinical characteristics, consultation patterns and healthcare resource utilization in real-world US patients with refractory and non-refractory CIU/CSU.

Methods: Data was collected from the Adelphi Real World 2015 Urticaria Disease Specific Programme. Physicians completed patient record forms (PRFs) for the next four patients consulting with non-refractory CIU/CSU and the next six with refractory CIU/CSU; patients were considered refractory if symptomatic and on treatment step ≥2. The same patients were asked to complete patient self-completion (PSC) forms describing how CIU/CSU affected them.

Results: Seventeen physicians (15 allergists; 2 dermatologists) completed 184 PRFs (108 refractory CIU/CSU; 76 non-refractory CIU/CSU); 140 patients completed PSC forms (93 refractory CIU/CSU; 47 non-refractory CIU/CSU). Mean time from first consultation to diagnosis was 13.5 (SD 28.3) weeks; mean time from diagnosis to first treatment was 16.0 (SD 37.9) weeks. Patients with refractory CIU/CSU were more likely to initially consult primary care physicians than those with non-refractory CIU/CSU (51% and 28%, respectively). The most common symptoms were itching, sleep problems and anxiety/distress, affecting 75%, 23% and 18%, respectively. Patient-perceived disease severity was greater than physician-perceived severity (refractory CIU/CSU kappa 0.1512; non-refractory CIU/CSU 0.1590).

Conclusions: Patients with CIU/CSU in this real-world study – particularly those with refractory CIU/CSU – were slow to receive specialist care and had substantial symptom burdens; patient–physician perception of disease severity was discordant. Earlier diagnosis of CIU/CSU may lead to timely use of CIU/CSU therapies.     

Next generation antihistamines: therapeutic rationale,accomplishments and advances

Antihistamines, among the most commonly prescribed drugs in the world, have evolved considerably since the first generation was introduced > 50 years ago. The first generation antihistamines (e.g., chlorpheniramine, diphenhydramine, promethazine and hydroxyzine) are still widely available and in use today. These drugs have considerable sedative effects caused by their ability to cross the blood–brain barrier. The next generation of antihistamines to emerge in the market were devoid of these sedative effects; however, two (terfenadine and astemizole) have shown rare but lethal cardiotoxic side effects. The third generation antihistamines, metabolites of the earlier drugs, have demonstrated no cardiac effects of the parent drugs and are at least as potent. Many have exhibited superior pharmacokinetic and pharmacological profiles, including an improved onset of action and duration of effect. The clinical benefit of these newer oral antihistamines will clearly help improve the quality of life of patients with chronic allergies.     

依巴斯汀治疗慢性特发性荨麻疹的疗效及安全性

目的：观察依巴斯汀治疗慢性特发性荨麻疹患者的疗效及安全性。方法：对68例慢性特发性荨麻疹患者应用依巴斯汀10mg，qd，连续治疗4周，干治疗后2，4和8周时复诊观察记录疗效及不良反应。结果：用药2周时痊愈32例（47．1％），显效41例（显效率60．3％）；4周时痊愈38例（55．9％），显效46例（显效率67．6％）：8周时痊愈41例（60．3％），显效48例（显效率70．1％）。2周时3例出现轻度头晕（4．4％），4周复诊时消失．8周时无明显不良反应。结论：依巴斯汀治疗慢性特发性荨麻疹安全有效。     

Non-clinical pharmacology,pharmacokinetics, and safety findings for the antihistamine bepotastine besilate

Abstract

Scope:

The purpose of this review is to examine published non-clinical literature on the antihistamine bepotastine besilate, including pharmacokinetic and pharmacologic properties.