Heel R C, Brogden R N, Speight T M, Avery G S
Drugs. 1978 Jan;15(1):3-32. doi: 10.2165/00003495-197815010-00002.
Fenoterol, the 4-hydroxyphenyl derivative of orciprenaline, is a resorcinol derivative with relatively high selectivity for beta2-adrenoceptors. It is active in man after inhalation or oral administration and is indicated in the treatment of bronchospasm associated with asthma, bronchitis and other obstructive airway diseases. Clinical experience has shown that fenoterol is an effective bronchodilator with negligible effects on the cardiovascular system following aerosol administration of usual therapeutic doses. In children, inhaled fenoterol is effective in preventing exercise-induced asthma and administration of the aerosol in young children has been successfully used to terminate acute asthma attacks. In trials in adults, inhaled fenoterol was superior to placebo. In other controlled studies, it showed a tendency to cause a slightly greater maximum improvement in airway function as assessed spirometrically, and to have a longer duration of action than inhaled orciprenaline, salbutamol or terbutaline, although in these trials statistically significant differences were often not found. The onset of maximum effect is less rapid than with isoprenaline but is longer lasting. About 60% of the eventual maximum response to fenoterol is reached in the first few minutes after inhalation. Oral fenoterol is more effective than placebo, ephedrine or orciprenaline, and probably similar to salbutamol and terbutaline. Following usual aerosol doses, side-effects are minimal. Oral administration is associated with a higher incidence of side-effects than inhalation, including fine muscle tremor and tachycardia.
非诺特罗是间羟异丙肾上腺素的4-羟基苯基衍生物,是一种对β2-肾上腺素受体具有较高选择性的间苯二酚衍生物。吸入或口服后在人体中具有活性,用于治疗与哮喘、支气管炎和其他阻塞性气道疾病相关的支气管痉挛。临床经验表明,非诺特罗是一种有效的支气管扩张剂,在使用常规治疗剂量气雾剂后对心血管系统的影响可忽略不计。在儿童中,吸入非诺特罗可有效预防运动诱发的哮喘,并且在幼儿中使用气雾剂已成功用于终止急性哮喘发作。在成人试验中,吸入非诺特罗优于安慰剂。在其他对照研究中,与吸入间羟异丙肾上腺素、沙丁胺醇或特布他林相比,从肺量测定评估来看,它显示出在气道功能上产生略大的最大改善趋势,并且作用持续时间更长,尽管在这些试验中通常未发现统计学上的显著差异。最大效应的起效比异丙肾上腺素慢,但持续时间更长。吸入后最初几分钟内可达到非诺特罗最终最大反应的约60%。口服非诺特罗比安慰剂、麻黄碱或间羟异丙肾上腺素更有效,可能与沙丁胺醇和特布他林相似。使用常规气雾剂剂量后,副作用最小。口服给药的副作用发生率高于吸入给药,包括细微的肌肉震颤和心动过速。