Kuziemski K, Mincewicz G, Sopel R, Słomiński J M
Katedry i Kliniki Chorób Płuc i Gruźlicy Akademii Medycznej w Gdańsku.
Pol Merkur Lekarski. 1998 Dec;5(30):317-20.
Asthma is a chronic inflammatory disorder of airways. It is characterised by bronchoconstriction, oedema and airways mucus hypersecretion. The main clinical features of asthma are dyspnea, cough, wheezing and heaviness in the chest. The pathology of asthma is characterised by presence of many inflammatory mediators, where the most important are cysteinyl leukotriens. Leukotriens C4, D4 and E4 are 1000 times more potent than histamine in contracting airways smooth muscles. Inhibitors of arachidonic acid metabolism have been used in asthma treatment. They can block the 5-lipoxygenase enzyme and/or 5-lipoxygenase-activating-proteine (FLAP), or can block the cysteinyl leukotriene receptors on the cell surface. Many inhibitors of arachidonic acid metabolism have been found during experimental trials. But only two are used as a drugs: zafirlukast and montelukast (leukotriene receptor inhibitors) montelukast and zileuton (5-lipoxygenase inhibitors) having the best efficacy in asthma treatment. Chronic treatment with these drugs results in a decrease of asthmatic symptoms, improvement of lung function (FEV1, PEF) and decreased usage of other medications--beta-adrenergic agonists and inhaled steroids. It has been proved that zafirlukast and zileuton show the high efficacy in mild-to-moderate asthma, exercise-induced asthma, allergen-induced asthma and aspirin-induced asthma. These oral drugs have been shown to course only mild adverse effects (such as temporary elevation in liver function tests, gastrointestinel disturbances, headache). Clinical usage of zafirlukast, montelukast and zileuton is limited in our country, they are hardly approachable on the market and the cost of treatment is high.
哮喘是一种气道慢性炎症性疾病。其特征为支气管收缩、水肿和气道黏液分泌过多。哮喘的主要临床特征为呼吸困难、咳嗽、喘息和胸部憋闷。哮喘的病理特征是存在多种炎症介质，其中最重要的是半胱氨酰白三烯。白三烯C4、D4和E4在收缩气道平滑肌方面比组胺强1000倍。花生四烯酸代谢抑制剂已用于哮喘治疗。它们可以阻断5-脂氧合酶和/或5-脂氧合酶激活蛋白（FLAP），或者可以阻断细胞表面的半胱氨酰白三烯受体。在实验试验中发现了许多花生四烯酸代谢抑制剂。但只有两种用作药物：扎鲁司特和孟鲁司特（白三烯受体抑制剂）以及孟鲁司特和齐留通（5-脂氧合酶抑制剂），它们在哮喘治疗中疗效最佳。长期使用这些药物可减轻哮喘症状，改善肺功能（第一秒用力呼气容积、呼气峰值流速），并减少其他药物——β-肾上腺素能激动剂和吸入性类固醇的使用。已证明扎鲁司特和齐留通在轻至中度哮喘、运动性哮喘、变应原性哮喘和阿司匹林性哮喘中显示出高疗效。这些口服药物仅显示出轻微的不良反应（如肝功能检查暂时升高、胃肠道不适、头痛）。扎鲁司特、孟鲁司特和齐留通在我国的临床应用有限，在市场上很难买到，而且治疗费用很高。
