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地氯雷他定:其在过敏性疾病管理中疗效的最新进展

Desloratadine: an update of its efficacy in the management of allergic disorders.

作者信息

Murdoch David, Goa Karen L, Keam Susan J

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 2003;63(19):2051-77. doi: 10.2165/00003495-200363190-00010.

Abstract

UNLABELLED

Desloratadine (Clarinex, Neoclarityn, Aerius, Azomyr, Opulis, Allex), the principal metabolite of loratadine, is itself an orally active, nonsedating, peripheral histamine H(1)-receptor antagonist. It is indicated in the US and Europe for the treatment of seasonal allergic rhinitis (SAR), perennial allergic rhinitis (PAR) and chronic idiopathic urticaria (CIU). It has a rapid onset of effect, efficacy throughout a 24-hour dosage interval, and sustained efficacy in these allergic conditions, as demonstrated in placebo-controlled trials of up to 6 weeks' duration in adult and adolescent patients. At present, there are no published direct comparisons of desloratadine and other H(1)-antihistamines; however, the principal, potential clinical advantages of desloratadine over late-generation H(1)-antihistamines are the drug's decongestant activity, which has been corroborated in several studies of patients with allergic rhinitis, and its anti-inflammatory effects. Indeed, the decongestant activity of desloratadine did not differ from that of pseudoephedrine in a trial in patients with SAR, and in patients with SAR and coexisting asthma, desloratadine reduced asthma symptoms and beta(2)-agonist use, and improved forced expiratory flow in 1 second. However, these issues warrant further study. Desloratadine is generally well tolerated. The overall incidence of adverse events in adults, adolescents and children was not significantly different to that with placebo, and similar proportions of desloratadine or placebo recipients reported events such as pharyngitis, dry mouth, myalgia, somnolence, dysmenorrhoea or fatigue. Desloratadine does not cause sedation or prolong the corrected QT (QTc) interval, can be administered without regard to concurrent intake of food and grapefruit juice, and appears to have negligible potential for drug interactions mediated by several metabolic systems.

CONCLUSION

Although comparative studies with second-generation and other recently developed H(1)-antihistamines are needed to define the drug's clinical profile more clearly, desloratadine can be expected to claim a prominent place in the management of allergic disorders in general, and in the amelioration of specific symptoms of allergy (e.g. nasal congestion) in patients with such disorders.

摘要

未标注

地氯雷他定(克敏能、新敏灵、艾来锭、阿佐敏、奥普力斯、阿莱克斯)是氯雷他定的主要代谢产物,本身是一种口服活性、非镇静性的外周组胺H(1)受体拮抗剂。在美国和欧洲,它被用于治疗季节性变应性鼻炎(SAR)、常年性变应性鼻炎(PAR)和慢性特发性荨麻疹(CIU)。在成人和青少年患者长达6周的安慰剂对照试验中表明,它起效迅速,在24小时给药间隔内均有疗效,且在这些变应性疾病中疗效持续。目前,尚无已发表的地氯雷他定与其他H(1)抗组胺药的直接比较;然而,地氯雷他定相对于新一代H(1)抗组胺药的主要潜在临床优势在于其减充血活性,这在多项变应性鼻炎患者研究中得到了证实,以及其抗炎作用。事实上,在一项SAR患者试验中,地氯雷他定的减充血活性与伪麻黄碱无异,在患有SAR且并存哮喘的患者中,地氯雷他定减轻了哮喘症状,减少了β(2)激动剂的使用,并改善了1秒用力呼气流量。然而,这些问题值得进一步研究。地氯雷他定一般耐受性良好。成人、青少年和儿童不良事件的总体发生率与安慰剂组无显著差异,服用地氯雷他定或安慰剂的患者报告咽炎、口干、肌痛、嗜睡、痛经或疲劳等事件的比例相似。地氯雷他定不会引起镇静或延长校正QT(QTc)间期,给药时无需考虑食物和葡萄柚汁的同时摄入,并且似乎由几种代谢系统介导的药物相互作用可能性可忽略不计。

结论

尽管需要与第二代和其他最近开发的H(1)抗组胺药进行比较研究以更清楚地界定该药物的临床特征,但总体而言,地氯雷他定有望在变应性疾病的管理中占据突出地位,并在改善此类疾病患者的特定变应症状(如鼻充血)方面发挥作用。

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