Keam Susan J, Lyseng-Williamson Katherine A, Goa Karen L
Adis International Limited, Auckland, New Zealand.
Drugs. 2003;63(10):991-1019. doi: 10.2165/00003495-200363100-00005.
Pranlukast (Onon, Azlaire), is an orally administered, selective, competitive antagonist of the cysteinyl leukotrienes (LT) C(4), LTD(4) and LTE(4). It is indicated for the prophylactic treatment of chronic bronchial asthma in paediatric and adult patients. The efficacy of pranlukast 225mg twice daily in adults with mild to moderate asthma was demonstrated in double-blind, placebo- or azelastine-controlled studies of 4 or 8 weeks' duration. The drug at this dosage was superior to both comparators in improving mean attack scores and morning and/or evening peak expiratory flow rates, and decreasing the use of rescue bronchodilators (p < 0.05). In limited clinical studies, pranlukast 225mg twice daily appeared to be as effective as montelukast 10mg once daily and zafirlukast 40mg twice daily in adults with mild to moderate asthma. Tachyphylaxis was absent when the drug was administered for up to 4 years. In patients requiring high-dose inhaled corticosteroid therapy, pranlukast 225 mg twice daily plus a halved dosage of inhaled corticosteroid was as effective as the original dosage of inhaled corticosteroid. Pranlukast was also effective in patients with mild to severe asthma in a clinical practice setting. In a double-blind trial, greater improvements in most outcome measures were observed with pranlukast than with oxatomide in children and adolescents with asthma. In clinical trials, pranlukast was well tolerated in adult and paediatric patients with asthma, with an adverse event profile similar to that of placebo. Gastrointestinal events and hepatic function abnormalities were the most commonly reported adverse events. No clinically significant differences in adverse event profiles between pranlukast, zafirlukast or montelukast were shown in limited comparisons. Although Churg-Strauss syndrome has been noted in pranlukast recipients, a direct causal relationship is unlikely.
Pranlukast is a well tolerated and effective preventative treatment in adult and paediatric patients with persistent asthma of all severities. In some patients, pranlukast may be beneficial when added to low-dose inhaled corticosteroids; it may also be a viable alternative to increasing inhaled corticosteroid dosages. The efficacy of pranlukast relative to placebo has been confirmed; its efficacy relative to other therapy awaits further investigation. Nonetheless, pranlukast is a useful therapeutic option (with as-required short-acting beta(2)-agonists), either as preventative monotherapy for the treatment of mild persistent asthma or in conjunction with inhaled corticosteroids in the management of moderate or severe persistent asthma.
普仑司特（Onon、Azlaire）是一种口服的半胱氨酰白三烯（LT）C4、LTD4和LTE4的选择性竞争性拮抗剂。它适用于儿科和成年患者慢性支气管哮喘的预防性治疗。在为期4周或8周的双盲、安慰剂或氮卓斯汀对照研究中，证实了普仑司特225mg每日两次用于轻度至中度哮喘成年患者的疗效。该剂量的药物在改善平均发作评分、早晚呼气峰值流速以及减少急救支气管扩张剂的使用方面优于两种对照药物（p<0.05）。在有限的临床研究中，普仑司特225mg每日两次在轻度至中度哮喘成年患者中似乎与孟鲁司特10mg每日一次和扎鲁司特40mg每日两次效果相当。该药物给药长达4年时未出现快速减敏现象。在需要高剂量吸入性糖皮质激素治疗的患者中，普仑司特225mg每日两次加一半剂量的吸入性糖皮质激素与原剂量的吸入性糖皮质激素效果相当。在临床实践中，普仑司特对轻度至重度哮喘患者也有效。在一项双盲试验中，哮喘儿童和青少年使用普仑司特比使用奥沙米特在大多数结局指标上有更大改善。在临床试验中，哮喘成年和儿科患者对普仑司特耐受性良好，不良事件谱与安慰剂相似。胃肠道事件和肝功能异常是最常报告的不良事件。在有限的比较中，普仑司特、扎鲁司特或孟鲁司特之间的不良事件谱未显示出临床显著差异。尽管在接受普仑司特治疗的患者中已注意到Churg-Strauss综合征，但不太可能存在直接因果关系。
普仑司特在所有严重程度的持续性哮喘成年和儿科患者中是耐受性良好且有效的预防性治疗药物。在一些患者中，普仑司特加低剂量吸入性糖皮质激素可能有益；它也可能是增加吸入性糖皮质激素剂量的可行替代方案。普仑司特相对于安慰剂的疗效已得到证实；其相对于其他疗法的疗效有待进一步研究。尽管如此，普仑司特是一种有用的治疗选择（联合按需使用的短效β2激动剂），可作为轻度持续性哮喘治疗的预防性单药治疗，或在中度或重度持续性哮喘管理中与吸入性糖皮质激素联合使用。
