Unit of Respiratory Medicine, Department of Experimental Medicine, University of Rome "Tor Vergata", Rome, Italy.
Unit of Respiratory Medicine, Department of Experimental Medicine, University of Rome "Tor Vergata", Rome, Italy.
Respir Med. 2019 Sep;156:47-52. doi: 10.1016/j.rmed.2019.08.005. Epub 2019 Aug 12.
The term ultra-LABA indicates once-daily β2-AR agonists (abediterol, indacaterol, olodaterol and vilanterol) that are single enantiomers of the (R)-configuration. All have a near full-agonist profile at human β2-AR. They can be prescribed in asthmatics only when associated with an with ICS, although further confirmations need to clarify what really these agents add if used in association to ICS and in what asthmatic patients this association may have more value. They are also under development in triple inhalers that include an ultra-LABA, a LAMA and an ICS. The once-daily posology might increase adherence in long-term treatment of asthma but superiority to twice-daily LABAs has not yet been fully demonstrated. In any case, still no ultra-LABA can be recommended as preferred.
术语“超长效β2-受体激动剂（LABA）”是指每日一次的β2-受体激动剂（阿布特罗、茚达特罗、奥达特罗和维兰特罗），它们是（R）-构型的单一对映异构体。所有这些药物在人β2-受体上均具有近乎完全激动剂的特性。只有当与 ICS 联合使用时，才能将它们用于哮喘患者，尽管还需要进一步的确认，以阐明如果与 ICS 联合使用，这些药物实际上能带来什么益处，以及在哪些哮喘患者中这种联合可能更有价值。这些药物也正在三联吸入器中开发，其中包括一种超长效β2-受体激动剂、一种长效抗胆碱能药物和一种 ICS。每日一次的用药方案可能会提高哮喘长期治疗的依从性，但与每日两次的 LABA 相比，其优越性尚未得到充分证实。在任何情况下，目前还没有一种超长效β2-受体激动剂可以被推荐为首选。
