Advenier C, Cerrina J, Duroux P
Sem Hop. 1984 Jan 26;60(3):179-93.
Bronchodilating drugs can be divided into three main groups: beta-adrenergic stimulants including specific beta-2 receptor agonists (salbutamol, terbutaline, fenoterol) which are the agents of this group used in everyday practice, theophylline and its derivatives, and atropine-like drugs (ipratropium bromide). Bronchodilators act chiefly upon the spasm observed at the bronchial level in reversible obstructive phenomena (mainly asthma), their effect upon inflammation and hypersecretion being slight or controversial. Beta-stimulants have a relatively specific mode of action at the bronchial level in the setting of use in pneumology; they exhibit cardiac effects only at high doses and when used by oral or parenteral routes. Relative to isoprenaline, they also have the advantage of being active orally and over a longer period of time. They are given in maintenance treatment of asthma, by parenteral or oral routes or as aerosols. Main side effects of adrenergic beta-stimulants are tremor with oral administration, and tachycardia with very high doses by parenteral or oral routes; when given as aerosols these agents may fail to control severe attacks. The bronchodilating properties of theophylline have been known for a long time; late advances concerning this drug result from better knowledge of its pharmacokinetics. Recent studies have discriminated between serum levels correlated with therapeutic effectiveness and those accompanied with mild or severe side effects; in addition, it has been clearly shown that the half life of this alkaloid varies from one person to another and with various physiopathologic (age, dietary habits, liver failure, heart failure...) or pharmacologic (drug interactions with enzyme inductors or inhibitors...) factors; these recent advances have led to improved individual adjustment of theophylline dosage using serum concentration assays if needed. Theophylline is used in acute attacks and in maintenance therapy of asthma. Main side effects are digestive intolerance and, with toxic doses, neurologic disorders. Atropine-like drugs inhibit the effects of the parasympathetic reflex which results from stimulation of receptors by irritation of the respiratory tract, through the action of mediators. In this group, ipratropium is the only drug given in aerosols; this, together with its pharmacologic specificity, contributes to its tolerance. In some instances, the bronchodilating effect of ipratropium bromide is comparable to that of sympathomimetics.
β-肾上腺素能兴奋剂，包括特定的β2受体激动剂（沙丁胺醇、特布他林、非诺特罗），这些是日常临床中使用的该类药物；茶碱及其衍生物；以及阿托品样药物（异丙托溴铵）。支气管扩张剂主要作用于可逆性阻塞性疾病（主要是哮喘）中在支气管水平观察到的痉挛，它们对炎症和分泌过多的作用轻微或存在争议。在肺病学应用中，β-兴奋剂在支气管水平具有相对特异的作用方式；它们仅在高剂量以及通过口服或胃肠外途径使用时才会出现心脏效应。相对于异丙肾上腺素，它们还具有口服有效且作用时间更长的优势。它们通过胃肠外或口服途径或作为气雾剂用于哮喘的维持治疗。肾上腺素能β-兴奋剂的主要副作用是口服时出现震颤，胃肠外或口服高剂量时出现心动过速；当作为气雾剂使用时，这些药物可能无法控制严重发作。茶碱的支气管扩张特性早已为人所知；关于这种药物的最新进展源于对其药代动力学的更深入了解。最近的研究区分了与治疗效果相关的血清水平和伴有轻度或重度副作用的血清水平；此外，已清楚表明这种生物碱的半衰期因人而异，并受各种生理病理因素（年龄、饮食习惯、肝功能衰竭、心力衰竭等）或药理因素（与酶诱导剂或抑制剂的药物相互作用等）影响；这些最新进展使得在必要时可通过血清浓度测定来改善茶碱剂量的个体化调整。茶碱用于哮喘的急性发作和维持治疗。主要副作用是消化不耐受，中毒剂量时会出现神经紊乱。阿托品样药物通过介质的作用抑制呼吸道刺激引起的受体刺激所产生的副交感反射效应。在这一类药物中，异丙托溴铵是唯一以气雾剂形式给药的药物；这一点连同其药理特异性，使其具有良好的耐受性。在某些情况下，异丙托溴铵的支气管扩张作用与拟交感神经药相当。
