Riccioni G, Bucciarelli T, Mancini B, Di Ilio C, D'Orazio N
Department of Biomedical Science, Faculty of Medicine and Surgery, University G. D'Annunzio, Chieti, Italy.
Curr Med Chem. 2007;14(18):1966-77. doi: 10.2174/092986707781368522.
Cysteinyl leukotrienes (Cys-LTs) are potent proinflammatory mediators derived from arachidonic acid through the 5-lypoxigenase (5-LO) pathway. They exert important pharmacological effects by interaction with at least two different receptors: Cys-LT(1) and Cys-LT(2). By competitive binding to the Cys-LT(1) receptor, leukotriene receptor antagonist drugs such as montelukast, zafirlukast, and pranlukast, block the effects of Cys-LTs and alleviate the symptoms of many chronic diseases, especially bronchial asthma and allergic rhinitis. Evidence obtained by randomized clinical trials as also by direct experience derived from patients suffering from asthma and allergic rhinitis justifies a broader role for leukotrienes receptor antagonists (LTRAs). Recently published studies and case reports have demonstrated beneficial effects of LTRAs on other diseases commonly associated with asthma (exercise induced asthma, rhinitis, chronic obstructive pulmonary disease, interstitial lung disease, chronic urticaria, atopic dermatitis, allergic fungal disease, nasal polyposis, and paranasal sinus disease) as well as other diseases not connected to asthma (migraine, respiratory syncytial virus postbronchiolitis, systemic mastocytosis, cystic fibrosis, pancreatitis, vulvovaginal candidiasis, cancer, atherosclerosis, eosinophils cystitis, otitis media, capsular contracture, and eosinophilic gastrointestinal disorders). The aim of this review is to show the most recent applications and effectiveness in clinical practice of the LTRAs.
半胱氨酰白三烯(Cys-LTs)是通过5-脂氧合酶(5-LO)途径从花生四烯酸衍生而来的强效促炎介质。它们通过与至少两种不同的受体相互作用发挥重要的药理作用:Cys-LT(1)和Cys-LT(2)。通过竞争性结合Cys-LT(1)受体,孟鲁司特、扎鲁司特和普仑司特等白三烯受体拮抗剂药物可阻断Cys-LTs的作用,并缓解许多慢性疾病的症状,尤其是支气管哮喘和过敏性鼻炎。随机临床试验以及哮喘和过敏性鼻炎患者的直接经验所获得的证据证明白三烯受体拮抗剂(LTRAs)具有更广泛的作用。最近发表的研究和病例报告表明,LTRAs对其他通常与哮喘相关的疾病(运动性哮喘、鼻炎、慢性阻塞性肺疾病、间质性肺疾病、慢性荨麻疹、特应性皮炎、过敏性真菌病、鼻息肉病和鼻窦疾病)以及其他与哮喘无关的疾病(偏头痛、呼吸道合胞病毒细支气管炎后、系统性肥大细胞增多症、囊性纤维化、胰腺炎、外阴阴道念珠菌病、癌症、动脉粥样硬化、嗜酸性粒细胞膀胱炎、中耳炎、包膜挛缩和嗜酸性粒细胞性胃肠疾病)具有有益作用。本综述的目的是展示LTRAs在临床实践中的最新应用和疗效。