哮喘是一种梗阻性肺疾病,以支气管收缩、持续性气道炎症和气道重塑为特征。临床上常用吸入皮质激素和β2受体拮抗剂辅佐治疗儿童哮喘,但这些药物疗法的治疗效果不是很理想,而且不适当的大剂量皮质激素会导致骨质疏松,生长迟缓和青光眼等严重副作用。口服抗白三烯剂是一种治疗儿童哮喘的新方法。白三烯是由花生四烯酸通过5 脂肪氧化酶途径由肥大细胞、嗜酸粒细胞和肺泡巨噬细胞合成的脂质。它通过与气道平滑肌上的CysLT1受体结合参与哮喘的炎症反应而引起支气管收缩。最近的研究表明,半胱氨酰白三烯可以介导上皮下胶原沉着和平滑肌肥大增生,从而导致不可逆的气道重塑和气道阻塞。实验研究和初步的临床研究显示,白三烯拮抗剂孟鲁司特辅助治疗儿童哮喘,可以减少皮质激素和β2拮抗剂的用量,预防气道重塑、减轻哮喘症状。然而,抗白三烯药物的疗效还需通过随机、双盲和多中心的临床研究得到进一步证实。

Children have the highest prevalence of asthma, an obstructive lung disease characterized by bronchoconstriction, persistent airway inflammation and airway remodeling. Inhaled corticosteroids and β2-agonists add-on therapies are used to treat these children but these medications are not always effective, and inappropriately high doses of corticosteroid may lead to serious side effects such as osteoporosis, growth retardation, and glaucoma. Oral anti-leukotrienes are new treatments for children suffering from asthma that work by antagonizing leukotrienes and inhibiting their synthesis. Leukotrienes are lipids synthesized from arachidonic acids in the 5-lipoxygenase pathway by mast cells, eosinophils, and alveolar macrophages in the lungs. Leukotrienes are involved in the asthmatic response by binding to the CysLT1 receptor on the airway smooth muscles, causing bronchoconstriction. Recent studies have shown that the cysteinyl-leukotrienes may mediate subepithelial collagen deposition and smooth muscle hypertrophy and hyperplasia, causing irreversible airway remodeling and airway obstruction. Experimental studies and preliminary clinical reports on pediatric patients have shown that the leukotriene antagonist montelukast may prevent airway remodeling and reduce asthmatic symptoms when used as an add-on treatment to reduce the intake of corticosteroids and β2-agonists. However, the efficacy of anti-leukotrienes drugs still needs to be confirmed by randomized, double-blind and multicenter clinical trials.