Price A H, Clissold S P
ADIS Drug Information Services, Auckland, New Zealand.
Drugs. 1989 Jul;38(1):77-122. doi: 10.2165/00003495-198938010-00004.
Salbutamol (albuterol) is a beta 2-selective adrenoceptor agonist which accounts for its pronounced bronchodilatory, cardiac, uterine and metabolic effects. During the intervening years since salbutamol was first reviewed in the Journal (1971), it has become extensively used in the treatment of reversible obstructive airways disease. Numerous studies in this disease (including severe acute, childhood and exercise-induced asthma) have confirmed the bronchodilatory efficacy of salbutamol, and it has been shown to be at least as effective as most of the currently available bronchodilators, if not more effective. The onset of maximum effect of salbutamol is dependent on the formulation used and the route by which it is administered. In most patients inhaled salbutamol is a first-line therapy, since it offers rapid bronchodilation, usually relieving bronchospasm within minutes. Although oral salbutamol has often proved to be less efficacious than the inhaled formulation, it still affords clinically significant bronchodilation, and it is particularly useful in those patients unable to coordinate the use of inhalers. Parenteral formulations of salbutamol are generally reserved for the treatment of severe attacks of bronchospasm and they are one of the treatments of choice in these life-threatening situations. Studies of the concomitant use of salbutamol and other agents such as anticholinergics, methylxanthines and beclomethasone dipropionate have usually shown a complementary response in the majority of patients, as might be expected from the different mechanisms of action of these groups of drugs. Salbutamol is generally well tolerated and any side effects observed are a predictable extension of its pharmacology. Since the frequency of side effects is dose related, and therefore dependent on the route of administration, it is not surprising that they are much more common following intravenous and oral rather than inhalation therapy. Tremor, tachycardia and hypokalaemia are the most frequently reported adverse effects. After nearly 20 years of use, salbutamol is well established as a 'first-choice' treatment in reversible obstructive airways disease. Indeed, throughout this time many new bronchodilatory agents have been studied but none have proved more effective. Clinical evaluation of salbutamol in the treatment of premature labour, hyperkalaemia and cardiac failure awaits further studies, although to date some encouraging results have been reported.
沙丁胺醇(舒喘灵)是一种β2 选择性肾上腺素能受体激动剂,这使其具有显著的支气管扩张、心脏、子宫及代谢作用。自《柳叶刀》首次对沙丁胺醇进行综述(1971 年)后的这些年里,它已被广泛用于治疗可逆性阻塞性气道疾病。针对这种疾病开展的大量研究(包括重症急性、儿童及运动诱发哮喘)证实了沙丁胺醇的支气管扩张疗效,并且已表明它即便不比大多数现有支气管扩张剂更有效,至少也与它们的效果相当。沙丁胺醇达到最大效应的起效时间取决于所用剂型及其给药途径。在大多数患者中,吸入沙丁胺醇是一线治疗方法,因为它能迅速扩张支气管,通常在数分钟内缓解支气管痉挛。尽管口服沙丁胺醇常常被证明不如吸入剂型有效,但它仍能产生具有临床意义的支气管扩张作用,对于那些无法协调使用吸入器的患者尤其有用。沙丁胺醇的肠胃外剂型一般留作治疗严重支气管痉挛发作之用,在这些危及生命的情况下,它们是首选治疗方法之一。对沙丁胺醇与其他药物(如抗胆碱能药物、甲基黄嘌呤和二丙酸倍氯米松)联合使用的研究通常表明,在大多数患者中会产生协同反应,这正如预期的那样,源于这些药物组不同的作用机制。沙丁胺醇一般耐受性良好,观察到的任何副作用都是其药理学作用可预测的延伸。由于副作用的发生频率与剂量相关,因此取决于给药途径,静脉注射和口服治疗后副作用比吸入治疗更为常见也就不足为奇了。震颤、心动过速和低钾血症是最常报告的不良反应。经过近 20 年的使用,沙丁胺醇已确立为可逆性阻塞性气道疾病的“首选”治疗药物。事实上,在此期间,许多新型支气管扩张剂都经过了研究,但没有一种被证明更有效。沙丁胺醇在治疗早产、高钾血症和心力衰竭方面的临床评估有待进一步研究,不过迄今为止已报告了一些令人鼓舞的结果。