Meyer J M, Wenzel C L, Kradjan W A
College of Pharmacy, University of Illinois at Chicago 60680.
Ann Pharmacother. 1993 Dec;27(12):1478-87. doi: 10.1177/106002809302701214.
The clinical pharmacology, pharmacokinetics, clinical efficacy, and adverse effects of the long-acting beta 2-agonist salmeterol are reviewed.
A MEDLINE search was performed to identify English-language publications pertaining to salmeterol.
Open and controlled trials were reviewed in assessing clinical efficacy. Only the results of controlled, randomized trials were considered in the effectiveness evaluation.
The primary measures of effectiveness in the clinical trials were bronchodilator activity and reduction of hyperresponsiveness that may reflect antiinflammatory activity. Bronchodilator activity was measured as changes in pulmonary function; reduction of hyperresponsiveness was evaluated using respiratory challenge with methacholine, histamine, allergen, or cold air. Secondary measures included symptom scores, need for rescue doses, and patient preference.
Salmeterol is a selective, beta 2-agonist that has been studied in the treatment of exercise-induced, nocturnal, and allergen-induced asthma. Salmeterol interacts with the traditional beta-receptor in a similar manner as other beta-agonists, and it exhibits potent in vitro antiinflammatory effects as an inhibitor of inflammatory mediator release. Less evidence exists for its in vivo antiinflammatory activity. Salmeterol demonstrates prolonged receptor occupancy, which is thought to contribute to its long duration of action. The recommended dose is 50 micrograms via metered-dose inhaler or dry-powdered inhalation. In the published clinical trials, salmeterol was more effective than albuterol in treating asthma, including exercise and allergen-induced asthma. Salmeterol's major advantage over other inhaled beta-agonists is its long duration of action (12 hours), making it an excellent choice for treatment of nocturnal asthma. A potential disadvantage is delayed onset of action. Tachyphylaxis to salmeterol's bronchodilator effects has not been shown, but tolerance to its protective effects against methacholine-induced bronchoconstriction has occurred. Adverse effects reported have been mild and have included headache, tremor, and palpitations.
Salmeterol is an effective beta 2-agonist in the treatment of asthma. However, several issues require further investigation regarding its long-term effects on disease control, significance of antiinflammatory activity, and role as a rescue medication.
综述长效β2受体激动剂沙美特罗的临床药理学、药代动力学、临床疗效及不良反应。
通过医学文献数据库（MEDLINE）检索，查找有关沙美特罗的英文出版物。
评估临床疗效时，对开放试验和对照试验进行了综述。有效性评估仅考虑对照随机试验的结果。
临床试验中有效性的主要指标为支气管扩张活性及高反应性降低，后者可能反映抗炎活性。支气管扩张活性通过肺功能变化来衡量；高反应性降低则采用乙酰甲胆碱、组胺、变应原或冷空气进行呼吸激发试验来评估。次要指标包括症状评分、急救药物需求及患者偏好。
沙美特罗是一种选择性β2受体激动剂，已用于运动诱发性、夜间及变应原诱发哮喘的治疗。沙美特罗与传统β受体的相互作用方式与其他β受体激动剂相似，且作为炎症介质释放抑制剂，在体外具有强大的抗炎作用。其体内抗炎活性的证据较少。沙美特罗显示出较长时间的受体占据，这被认为与其作用持续时间长有关。推荐剂量为通过定量吸入器或干粉吸入器吸入50微克。在已发表的临床试验中，沙美特罗在治疗哮喘（包括运动和变应原诱发的哮喘）方面比沙丁胺醇更有效。沙美特罗相对于其他吸入性β受体激动剂的主要优势在于其作用持续时间长（12小时），使其成为治疗夜间哮喘的理想选择。一个潜在的缺点是起效延迟。尚未显示对沙美特罗支气管扩张作用的快速耐受性，但对其预防乙酰甲胆碱诱发支气管收缩的保护作用已出现耐受性。报告的不良反应较轻，包括头痛、震颤和心悸。
沙美特罗是治疗哮喘的有效β2受体激动剂。然而，关于其对疾病控制的长期影响、抗炎活性的意义以及作为急救药物的作用等几个问题仍需进一步研究。
