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卢帕他定在变应性鼻炎中的药理特性、疗效及安全性

Pharmacological profile, efficacy and safety of rupatadine in allergic rhinitis.

作者信息

Katiyar Subodh, Prakash Shivesh

机构信息

Department of Tuberculosis & Respiratory diseases, GSVM Medical College, Kanpur, India.

出版信息

Prim Care Respir J. 2009 Jun;18(2):57-68. doi: 10.3132/pcrj.2008.00043.

Abstract

Allergic rhinitis (AR) is a disease with high prevalence. In AR, exposure to airborne allergens elicits an allergic response which involves epithelial accumulation of effector cells - e.g. mast cells and basophils - and subsequent inflammation. During the early response in AR, histamine has been found to be the most abundant mediator and it is associated with many symptoms of this disease mediated through the histamine H1 receptor. Therefore, anti-histamines have a role to play in the management of AR. However, the available antihistamines have certain well-known side effects like sedation and potential pro-arrythmic effects owing to their interactions with other drugs, as well as having poor or no effect on platelet activating factor (PAF) which also plays an important role in AR. This article is a qualitative systematic literature review on the pharmacological profile of rupatadine in order to evaluate its safety and efficacy in AR as compared to other anti-histamines. Rupatadine is a once-daily non-sedative, selective, long-acting H1 anti-histamine with antagonistic PAF effects through its interaction with specific receptors. Rupatadine significantly improves nasal symptoms in patients with AR. It has a good safety profile and is devoid of arrythmogenic effects. These properties make rupatadine a suitable first line anti-histamine for the treatment of AR.

摘要

过敏性鼻炎(AR)是一种高发性疾病。在AR中,接触空气传播的过敏原会引发过敏反应,其中涉及效应细胞(如肥大细胞和嗜碱性粒细胞)在上皮的积聚以及随后的炎症反应。在AR的早期反应中,组胺被发现是最丰富的介质,并且它与通过组胺H1受体介导的该疾病的许多症状相关。因此,抗组胺药在AR的治疗中发挥作用。然而,现有的抗组胺药有一些众所周知的副作用,如镇静作用以及由于它们与其他药物相互作用而产生的潜在促心律失常作用,并且对在AR中也起重要作用的血小板活化因子(PAF)效果不佳或无效。本文是关于卢帕他定药理学特性的定性系统文献综述,目的是评估其与其他抗组胺药相比在AR中的安全性和疗效。卢帕他定是一种每日一次的非镇静性、选择性、长效H1抗组胺药,通过与特定受体相互作用具有拮抗PAF的作用。卢帕他定能显著改善AR患者的鼻部症状。它具有良好的安全性,且没有致心律失常作用。这些特性使卢帕他定成为治疗AR的合适一线抗组胺药。

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