福莫特罗全身效应短暂 吸入福莫特罗以后肺部效应和全身效应示意图 a ：吸入型福莫特罗作 用时间长（ 12 小时） 1 b ：典型吸入型短效 β 2 激 动剂一般作用时间为 4-6 小时 2 c 和 d ：两个研究已经证 明，福莫特罗在高剂量 时全身效应时间短，与 传统的吸入型 β 2 激动剂 相似，在治疗剂量时， 其全身效应一般很小以 致无法测量
Ultra-long-acting β 2-adrenergic receptor agonists (ultra-LABA) Vilanterol ( 维兰特罗 ) Vilanterol which was approved in May 2013 in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD).fluticasone furoateBreo ElliptaGlaxoSmithKlinechronic obstructive pulmonary disease Vilanterol is available in following combinations: with inhaled corticosteroid fluticasone furoate — fluticasone furoate/vilanterol (trade names Breo Ellipta (U.S.), Relvar Ellipta (EU, RU) )corticosteroidfluticasone furoatefluticasone furoate/vilanterolU.S.EURU with muscarinic antagonist umeclidinium bromide — umeclidinium bromide/vilanterol (trade name Anoro Ellipta)muscarinic antagonistumeclidinium bromideumeclidinium bromide/vilanterol
§Theophyllines Theophyllines: One type of xanthine derivatives ( 甲基黄嘌呤类衍生物 ) One type of xanthine derivatives ( 甲基黄嘌呤类衍生物 ) Bronchial dilators
2. Clinical uses Bronchial asthma (p.o., i.v.) Bronchial asthma (p.o., i.v.) Others: acute pulmonary edema, etc. Others: acute pulmonary edema, etc. Slow-release theophylline (for control of nocturnal asthma) is the most commonly used methylxanthine. Aminophylline pentoxifylline, is promoted as a remedy for intermittent claudication; Bronchial dilators
Common adverse effects: Gastrointestinal distress, tremor, and insomnia. Severe nausea and vomiting, hypotension, cardiac arrhythmias, Seizures Very large overdoses (eg, in suicide attempts) are potentially lethal because of arrhythmias and seizures. Beta blockers are useful in reversing severe cardiovascular toxicity from theophylline.
Mechanism of Action and Effects When given by aerosol, ipratropium and tiotropium competitively block muscarinic receptors in the airways and effectively prevent bronchoconstriction mediated by vagal discharge （迷走神经放电） When given by aerosol, ipratropium and tiotropium competitively block muscarinic receptors in the airways and effectively prevent bronchoconstriction mediated by vagal discharge （迷走神经放电）. Muscarinic antagonists reverse bronchoconstriction in some asthma patients (especially children) and in many patients with COPD. They have no effect on the chronic inflammatory aspects of asthma.
Clinical Use and Toxicity Ipratropium and tiotropium are useful in one third to two thirds of asthmatic patients; β2 agonists are effective in almost all. For acute bronchospasm, therefore, the β agonists are usually preferred. However, in COPD, which is often associated with acute episodes of bronchospasm, the antimuscarinic agents may be more effective and less toxic than β agonists.
Spacer will aid patients to inhale the aerosolized drugs easier Outcome of different sized particles: > 10μm: mouth and oropharynx < 0.5μm: inhaled to the alveoli and subsequently exhaled without being deposited in the lung 1-5μm: the most effective
Stepwise approach to asthma treatment 2016 GINA pocket Guide
哮喘 -COPD 重叠综合征 (asthma-chronic obstructive pulmonary disease overlap syndromes, ACOS) ACOS 不是一种单独的疾病，包括了各种不同类型的气道呼吸疾病 ( 表型 ) 。关于 哮喘和 COPD 的一系列不同潜在机制很可能将会被 ACOS 一一验证。 Some patients with COPD have predominantly eosinophilic inflammation and might respond to high doses of inhaled corticosteroids and newly developed specific antieosinophil therapies, including blocking antibodies against IL-5, IL-13, IL-33, and thymic stromal lymphopoietin, as well as oral chemoattractant receptor-homologous molecule expressed on TH2 cells antagonists. Barnes PJ.Therapeutic approaches to asthma-chronic obstructive pulmonary disease overlap syndromes. J Allergy Clin Immunol. 2015 Sep;136(3):531-45.
Other patients have severe asthma or are asthmatic patients who smoke with features of COPD-induced inflammation and might benefit from treatments targeting neutrophils, including macrolides, CXCR2 antagonists, phosphodiesterase 4 inhibitors, p38 mitogen- activating protein kinase inhibitors, and antibodies against IL-1 and IL-17. Other patients appear to have largely fixed obstruction with little inflammation and might respond to long-acting bronchodilators, including long-acting muscarinic antagonists, to reduce hyperinflation. Highly selected patients with severe asthma might benefit from bronchial thermoplasty( 支气管热成形术 ). Some patients with overlap syndromes can be conveniently treated with triple fixed-dose combination inhaler therapy with an inhaled corticosteroid, long- acting β2-agonist, and long-acting muscarinic antagonist, several of which are now in development. Corticosteroid resistance is a feature of asthma-COPD overlap syndrome, and understanding the various molecular mechanisms of this resistance has identified novel therapeutic targets and presented the prospect of therapies that can restore corticosteroid responsiveness.
Reference Pharmacology and therapeutics of bronchodilators. Cazzola M, Page CP, Calzetta L, Matera MG. Pharmacol Rev. 2012 Jul;64(3):450-504. doi: 10.1124/pr.111.004580. Review. Hansel TT, Neighbour H, Erin EM, et al. (October 2005). "Glycopyrrolate causes prolonged bronchoprotection and bronchodilatation in patients with asthma". Chest 128 (4): 1974–9. Jump up, Gilman MJ, Meyer L, Carter J, Slovis C (November 1990). "Comparison of aerosolized glycopyrrolate and metaproterenol in acute asthma". Chest 98 (5): 1095–8. Tzelepis G, Komanapolli S, Tyler D, Vega D, Fulambarker A (January 1996). "Comparison of nebulized glycopyrrolate and metaproterenol in chronic obstructive pulmonary disease". Eur. Respir. J. 9 (1): 100–3. Pleasants RA, Wang T, Gao J, Tang H, Donohue JF. Inhaled Umeclidinium in COPD Patients: A Review and Meta-Analysis. Drugs. 2016 Mar;76(3):343-61 Melani AS. Long-acting muscarinic antagonists.Expert Rev Clin Pharmacol. 2015;8(4):479-501. Review. Barnes PJ.Therapeutic approaches to asthma-chronic obstructive pulmonary disease overlap syndromes. J Allergy Clin Immunol. 2015 Sep;136(3):531-45.
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