Department of Experimental Medicine, Unit of Pharmacology, Second University of Naples, Naples, Italy.
Trends Pharmacol Sci. 2011 Aug;32(8):495-506. doi: 10.1016/j.tips.2011.04.003. Epub 2011 Jun 16.
Because of the central role of bronchodilators in the treatment of respiratory diseases, there is still considerable interest in finding novel classes of broncholytic drugs. It can be hypothesized that a longer duration of bronchodilation with a once-daily agent might be associated with superior and more consistent efficacy over a range of endpoints than is achieved with a twice-daily agent. Several novel β(2)-adrenoceptor (AR) agonists, antimuscarinic agents, new combination platforms such as dual-acting muscarinic antagonist-β(2)-AR agonist bronchodilators, xanthine drugs and phosphodiesterase inhibitors, and their combination with another bronchodilator class, or an inhaled corticosteroid are currently under development with the aim of achieving once-daily dosing and, therefore, increasing the likelihood of compliance with therapy. This review paper mainly focuses on recent results of preclinical studies that have used human tissue and clinical trials of new bronchodilators in patients with chronic obstructive pulmonary disease.
由于支气管扩张剂在治疗呼吸系统疾病中的核心作用，人们仍然非常关注寻找新型的支气管扩张药物。可以假设，与每日两次的药物相比，每日一次的药物具有更长的支气管扩张持续时间，可能与一系列终点的更优和更一致的疗效相关。目前正在开发几种新型的β(2)-肾上腺素能受体（AR）激动剂、抗毒蕈碱药物、新的联合平台，如双重作用的毒蕈碱拮抗剂-β(2)-AR 激动剂支气管扩张剂、黄嘌呤药物和磷酸二酯酶抑制剂，以及它们与另一种支气管扩张剂类别的联合应用，或与吸入性皮质类固醇联合应用，目的是实现每日一次的给药，从而提高治疗的依从性。这篇综述文章主要关注最近的临床前研究结果，这些研究使用了人类组织，并在慢性阻塞性肺疾病患者中进行了新型支气管扩张剂的临床试验。
