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Anti-inflammatory activities of beta2-agonists.

机译:β2-激动剂的抗炎活性。

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Beta2-adrenergic agonists (beta2-agonists) play a pivotal role in the acute and chronic management of asthma. Their major action on the airways is the relaxation of smooth muscle cells. In addition to their bronchodilator properties, beta2-agonists may have other effects through their activation of beta2-receptors expressed on resident airway cells such as epithelial cells and mast cells and circulating inflammatory cells such as eosinophils and neutrophils. These non-bronchodilator activities of beta2-agonists may enhance their efficacy in the management of asthma. In pre-clinical studies, the anti-inflammatory effects of beta2-agonists are demonstrated through their stabilizing effect on mast cells and their inhibition of mediator release from eosinophils, macrophages T-lymphocytes, and neutrophils. In addition, beta2-agonists may inhibit plasma exudation in the airway, the release of neuropeptides from sensory nerves, and mediator release from epithelial cells. These in vitro observations are not asclearly demonstrated in clinical trials, which may be explained by the rapid desensitization of beta2-adrenergic receptors on airway inflammatory cells. The regular use of short-acting beta2-agonists alone has been shown to have deleterious effects on asthma control. Therefore, short-acting agents should only be used when needed for rescue of acute symptoms. Monotherapy with long-acting beta2-agonists has also been associated with poor asthma control. However, when given concomitantly with inhaled corticosteroids, beta2-agonists may potentiate the anti-inflammatory effect of corticosteroids, improve asthma control and prevent exacerbations.
机译:β2-肾上腺素能激动剂(β2-激动剂)在哮喘的急性和慢性控制中起着关键作用。它们对呼吸道的主要作用是平滑肌细胞的松弛。除了具有支气管扩张剂的性质外,β2激动剂还可以通过激活在驻留气道细胞(如上皮细胞和肥大细胞)和循环炎症细胞(如嗜酸性粒细胞和嗜中性粒细胞)中表达的β2受体而发挥其他作用。 β2-激动剂的这些非支气管扩张剂活性可以增强其在哮喘控制中的功效。在临床前研究中,通过β2-激动剂对肥大细胞的稳定作用以及对嗜酸性粒细胞,巨噬细胞T淋巴细胞和嗜中性粒细胞的介质释放的抑制作用,证明了其具有抗炎作用。此外,β2-激动剂可能会抑制气道中的血浆渗出,感觉神经神经肽的释放以及上皮细胞的介质释放。这些体外观察未在临床试验中得到明确证明,这可以通过气道炎性细胞上的β2-肾上腺素能受体快速脱敏来解释。单独使用短效β2-激动剂已显示对哮喘控制具有有害作用。因此,短效剂仅应在需要时才能使用以缓解急性症状。长效β2-激动剂的单药治疗也与哮喘控制不良有关。但是,与吸入的糖皮质激素同时使用时,β2激动剂可能会增强糖皮质激素的抗炎作用,改善哮喘控制并预防病情加重。

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