Ullman A, Svedmyr N
Department of Clinical Pharmacology, Sahlgrenska University Hospital, Gothenburg, Sweden.
Thorax. 1988 Sep;43(9):674-8. doi: 10.1136/thx.43.9.674.
Salmeterol is a new inhaled beta 2 adrenoceptor agonist, which has been shown in animal experiments to produce a more prolonged bronchodilator effect than currently available beta 2 adrenoceptor agonists. It was studied in eight adult asthmatic patients. Each patient received on separate test days salbutamol 200 micrograms and salmeterol 50, 100, and 200 micrograms according to a randomised, double blind, crossover design. FEV1, peak expiratory flow (PEF), heart rate, blood pressure, and tremor were recorded in the clinic for six hours after drug inhalation; PEF was recorded for a further six hours at home. All three doses of salmeterol produced peak increases in FEV1 (mean 0.5-0.8 l) and PEF (71-100 l/min) similar to those produced by salbutamol 200 micrograms (0.5 l and 74 l/min). After salbutamol FEV1 and PEF had returned to baseline within six hours, but after all three doses of salmeterol more than half of the maximum bronchodilator effect remained after 12 hours. The effects of salbutamol and the two lower doses of salmeterol (50 and 100 micrograms) on cardiovascular measurements and on tremor were similar, whereas after salmeterol 200 micrograms there was a small decrease in diastolic blood pressure and an increase in heart rate and tremor. Thus inhaled salmeterol has a long acting bronchodilator action in asthmatic patients. This effect may be of value in the treatment of asthma, particularly in patients with nocturnal symptoms.
沙美特罗是一种新型吸入型β2肾上腺素能受体激动剂,动物实验表明,其支气管扩张作用比现有的β2肾上腺素能受体激动剂更持久。对8名成年哮喘患者进行了研究。按照随机、双盲、交叉设计,每位患者在不同的测试日分别吸入200微克沙丁胺醇以及50、100和200微克沙美特罗。吸入药物后6小时内在诊所记录第一秒用力呼气容积(FEV1)、呼气峰值流速(PEF)、心率、血压和震颤情况;在家中继续记录6小时的PEF。沙美特罗的所有三个剂量使FEV1(平均增加0.5 - 0.8升)和PEF(增加71 - 100升/分钟)达到峰值,与200微克沙丁胺醇产生的效果(0.5升和74升/分钟)相似。沙丁胺醇作用后,FEV1和PEF在6小时内恢复到基线水平,但沙美特罗的所有三个剂量作用后,12小时仍有超过一半的最大支气管扩张作用。沙丁胺醇以及沙美特罗两个较低剂量(50和100微克)对心血管指标和震颤的影响相似,而200微克沙美特罗作用后舒张压略有下降,心率和震颤增加。因此,吸入沙美特罗对哮喘患者有长效支气管扩张作用。这种作用在哮喘治疗中可能具有重要价值,尤其是对有夜间症状的患者。