慢性阻塞性肺疾病的药物治疗:以酒石酸阿福莫特罗为主

P. King
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引用次数: 1

摘要

酒石酸阿福莫特罗是一种新开发的长效ssβ2激动剂,具有急性和延长的支气管扩张作用。它由2个异构体(R,R/R,R)组成,这与更常用的外消旋形式的福莫特罗(R,R/S,S)不同。活性异构体是(R,R),在体外,阿福莫特罗可能比福莫特罗具有更强的抗炎作用。它只能通过喷雾器来提供。已有5项随机、盲法试验评估了阿福莫特罗在慢性阻塞性肺疾病(COPD)中的应用。阿福莫特罗已被证明可以改善肺功能和症状,但测试对象确实有高度的气道反应性。该药物耐受性良好,副作用发生率低,但试验可能没有足够的持续时间来充分评估这一点。阿福莫特罗在有潜在心脏病的患者中应谨慎使用。阿福莫特罗目前主要用于需要长效β2激动剂但不能使用干粉或计量吸入剂制剂的COPD患者。阿福莫特罗可能只需要每天服用一次,并可与其他吸入药物联合使用,特别是噻托溴铵,以获得额外的益处。它可能在急性恶化的管理中发挥作用。
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Pharmacotherapy of Chronic Obstructive Pulmonary Disease: Focus on Arformoterol Tartrate
Arformoterol tartrate is a newly developed long-acting ssβ2-agonist with both acute and prolonged bronchodilator effects. It is formed of 2 isomers (R,R/R,R) which distinguishes it from the more commonly used racemic formoterol (R,R/S,S). The active isomer is the (R,R) and in vitro arformoterol may have more potent anti-inflammatory effects than formoterol. It can only be given by a nebulizer. There have been 5 randomized, blinded trials which have assessed the use of arformoterol in chronic obstructive pulmonary disease (COPD). Arformoterol has been demonstrated to improve lung function and symptoms but the subjects tested did have a high degree of airway reactivity. The medication was well tolerated with a low incidence of side effects but the trials may not have been of sufficient duration to assess this adequately. Arformoterol should be used with caution in subjects with underlying cardiac disease. The current main use of arformoterol is in those subjects with COPD who require a long acting β2-agonist but who cannot use a dry powder or metered dose inhaler preparation. Arformoterol may only need to be given once a day and can be combined with other inhaled medication particularly tiotropium for additional benefit. It potentially has a role in the management of acute exacerbations.
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