Unit of Respiratory Clinical Pharmacology, Department of Internal Medicine, University of Rome 'Tor Vergata', Italy.
Br J Pharmacol. 2011 May;163(1):4-17. doi: 10.1111/j.1476-5381.2011.01216.x.
Despite the passionate debate over the use of β(2) -adrenoceptor agonists in the treatment of airway disorders, these agents are still central in the symptomatic management of asthma and COPD. A variety of β(2) -adrenoceptor agonists with long half-lives, also called ultra long-acting β(2) -adrenoceptor agonists (ultra-LABAs; indacaterol, olodaterol, vilanterol, carmoterol, LAS100977 and PF-610355) are currently under development with the hopes of achieving once-daily dosing. It is likely that the once-daily dosing of a bronchodilator would be a significant convenience and probably a compliance-enhancing advantage, leading to improved overall clinical outcomes. As combination therapy with an inhaled corticosteroid (ICS) and a LABA is important for treating patients suffering from asthma, and a combination with an inhaled long-acting antimuscarinic agent (LAMA) is important for treating COPD patients whose conditions are not sufficiently controlled by monotherapy with a β(2) -adrenoceptor agonist, some novel once-daily combinations of LABAs and ICSs or LAMAs are under development.
尽管关于β(2) -肾上腺素受体激动剂在气道疾病治疗中的应用存在激烈争论，但这些药物仍在哮喘和 COPD 的症状管理中处于核心地位。目前正在开发各种半衰期较长的β(2) -肾上腺素受体激动剂，也称为超长效β(2) -肾上腺素受体激动剂（ultra-LABAs；茚达特罗、奥达特罗、维兰特罗、卡莫特罗、LAS100977 和 PF-610355），以期实现每日一次给药。每日一次给予支气管扩张剂可能会带来显著的便利，并且可能具有提高顺应性的优势，从而改善整体临床结局。由于联合吸入皮质类固醇（ICS）和 LABA 治疗哮喘患者非常重要，而联合吸入长效抗毒蕈碱药物（LAMA）治疗仅用β(2) -肾上腺素受体激动剂治疗不能充分控制病情的 COPD 患者也非常重要，因此正在开发一些新型的每日一次的 LABA 和 ICS 或 LAMA 联合制剂。
