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首页> 外文期刊>Pulmonary pharmacology & therapeutics >Pharmacological characterization of the interaction between tiotropium bromide and olodaterol on human bronchi and small airways
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Pharmacological characterization of the interaction between tiotropium bromide and olodaterol on human bronchi and small airways

机译：噻托溴铵与奥洛丹科在人支气管和小气道之间相互作用的药理表征

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Combining a long-acting beta(2)-agonist (LABA) with a long-acting muscarinic antagonist (LAMA) is the cornerstone to treat patients with chronic obstructive pulmonary disease (COPD). In this study we have characterized the interaction between the LAMA tiotropium bromide, and the LABA olodaterol, on the contractile tone of human medium bronchi and small airways. The response to a combination of tiotropium bromide and olodaterol was assessed at sub-maximal contractile tone induced by carbachol. The duration of action was studied in tissue contracted by transmural stimulation. Relaxation of bronchial tone was expressed as % of maximal response to papaverine. Drug interactions were analyzed by the Bliss Independence method and Unified Theory. Tiotropium bromide/olodaterol combination induced a significant synergistic relaxant response (P < 0.05 vs. expected additive effect) in medium bronchi and small airways pre-contracted by carbachol, by enhancing relaxation + 22.13 +/- 4.42% and +26.31 +/- 12.39%, respectively. The combination of tiotropium bromide and olodaterol also reduced the airway smooth muscle contractility elicited by transmural stimulation by 73.60 +/- 3.10%. The extent of synergy was strong to very strong, and was supported by the release of neuronal acetylcholine, cyclic adenosine monophosphate levels, and activation of iberiotoxin-sensitive KCa++ channels. Conversely, the interaction between tiotropium bromide and olodaterl was independent of the activity at M-2 muscarinic receptors. These results indicate that tiotropium bromide/olodaterol combination leads to a potent and durable synergistic relaxation of human medium bronchi and small airways. Further pharmacological studies are needed to confirm these results in clinical settings.
机译：结合长效的β（2）角度（Laba）与长效的毒蕈碱拮抗剂（喇嘛）是治疗慢性阻塞性肺病（COPD）患者的基石。在这项研究中，我们已经表征了喇嘛噻托溴铵和Laba olodaterol之间的相互作用，对人类培养基支气管和小型气道的收缩口。在由卡巴酚诱导的亚气球收缩性调节对噻托溴铵和奥洛丹科醇组合的反应。通过透射刺激收缩的组织中研究了作用的持续时间。支气管间距的松弛表示为对罂粟碱的最大反应的百分比。通过Bliss独立方法和统一理论分析了药物相互作用。脱硫溴铵/ olodaterol组合诱导培养基支气管和小型气道的显着协同缓解响应（P <0.05 Vs.预期添加效应）通过加强弛豫+ 22.13 +/- 4.42％和+ 26.31 +/- 12.39 ％， 分别。噻托溴铵和奥洛丹科醇的组合还将透气刺激引发的气道平滑肌收缩力减少73.60 +/- 3.10％。协同作用的程度强大强劲，并得到神经元乙酰胆碱，环状腺苷一磷酸含量的释放和伊伯因毒敏感KCA ++通道的激活。相反，溴化噻唑和奥洛丹尔之间的相互作用与M-2毒蕈碱受体的活性无关。这些结果表明，噻托溴铵/ olodaterol组合导致人类培养基支气管和小型气道的有效和耐用的协同松弛。需要进一步的药理学研究来确认这些结果在临床环境中。

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