Stoloff S W
University of Nevada School of Medicine, Reno, USA.
Postgrad Med. 2000 Sep 15;108(4 Suppl):22-31.
Two leukotriene receptor antagonists (LTRAs)--montelukast and zafirlukast--are currently available in the United States. Montelukast is approved for the treatment of asthma in patients as young as 2 years old and zafirlukast, in patients 7 years of age or older. In more than 15 clinical trials of LTRA therapy for mild to moderate persistent asthma, both of these oral agents produced rapid improvement in pulmonary function and daytime asthma symptoms. They also decreased the frequency of nocturnal awakening and the need for rescue therapy with beta2-adrenergic agonists and oral corticosteroids. These effects were maintained throughout the treatment period; tolerance did not develop. When used concomitantly with an inhaled corticosteroid (ICS), each LTRA further improved asthma control, thus permitting the partial or complete tapering off of the ICS dose needed to maintain clinical control. Although rare, previously undiagnosed cases of Churg-Strauss syndrome have been unmasked when ICS use is decreased or discontinued. The improved adherence gained with an oral agent administered as infrequently as once daily maximizes the effectiveness of these newest antiasthma medications.
目前在美国有两种白三烯受体拮抗剂（LTRA）——孟鲁司特和扎鲁司特。孟鲁司特被批准用于治疗2岁及以上的哮喘患者，扎鲁司特则用于治疗7岁及以上的患者。在超过15项针对轻至中度持续性哮喘的LTRA治疗临床试验中，这两种口服药物均能使肺功能和日间哮喘症状迅速改善。它们还减少了夜间觉醒的频率以及使用β2肾上腺素能激动剂和口服糖皮质激素进行急救治疗的需求。这些效果在整个治疗期间都能维持；未出现耐受性。当与吸入性糖皮质激素（ICS）联合使用时，每种LTRA都能进一步改善哮喘控制，从而使维持临床控制所需的ICS剂量得以部分或完全减少。虽然罕见，但当减少或停用ICS时，曾有未被诊断出的Churg-Strauss综合征病例被发现。每日只需服用一次的口服药物提高了依从性，从而使这些最新的抗哮喘药物的疗效最大化。
