King Paul
Monash University Department of Medicine, Monash Medical Centre, Australia.
Int J Chron Obstruct Pulmon Dis. 2008;3(3):385-91. doi: 10.2147/copd.s753.
Formoterol is a beta2-agonist that has both short and long acting bronchodilator effects. Beta2-agonists used as bronchodilators have been synthesized as racemates that comprise (R,R) and (S,S)-enantiomers. Compounds that are beta2-selective derive their bronchodilator effect from an interaction between the (R,R)-enantiomer and the beta2-adrenoceptor. Arformoterol is the (R,R)-enantiomer and is distinguished from the more commonly used racemic (RR/S,S)-diasteriomer of formoterol. Overall literature on the use of arformoterol in COPD is very preliminary. There is some in vitro data that demonstrate significant bronchodilation and inhibition of inflammation with arformoterol, and these effects may be more pronounced than those caused by racemic formoterol. There are limited clinical trial data that demonstrate that arformoterol produces significant improvement in lung function in COPD; however, many of the subjects involved had marked baseline airway reversibility. Arformoterol has been very well tolerated in clinical trials and could potentially be used only once every 24 hours (due to its prolonged effect). It can only be given in nebulized form. Arformoterol can potentially be given with other inhaled medications.
福莫特罗是一种具有短效和长效支气管扩张作用的β2受体激动剂。用作支气管扩张剂的β2受体激动剂已被合成外消旋体，其包含（R，R）和（S，S）对映体。具有β2选择性的化合物通过（R，R）对映体与β2肾上腺素能受体之间的相互作用产生支气管扩张作用。阿福特罗是（R，R）对映体，与更常用的福莫特罗外消旋（RR/S，S）非对映体不同。关于阿福特罗在慢性阻塞性肺疾病（COPD）中应用的总体文献非常有限。有一些体外数据表明阿福特罗具有显著的支气管扩张作用并能抑制炎症，且这些作用可能比消旋福莫特罗引起的作用更明显。有限的临床试验数据表明阿福特罗可使COPD患者的肺功能有显著改善；然而，许多参与试验的受试者基线气道可逆性明显。阿福特罗在临床试验中耐受性良好，且因其作用持久，可能每24小时仅需使用一次。它只能以雾化形式给药。阿福特罗有可能与其他吸入药物联合使用。
