Yamakido M, Inamizu T, Ikuta T, Onari K, Tanabe M, Nishimoto Y
Int J Clin Pharmacol Ther Toxicol. 1985 Sep;23(9):461-8.
The authors administered orally 40, 60 and 80 micrograms of Formoterol which was developed as a new bronchodilator and 4 mg of Salbutamol which is considered to be a beta 2-selective drug, to healthy adults. Pulse rate, blood pressure and blood levels of cyclic GMP, free fatty acid, cyclic AMP, glucose and lactic acid were measured in order to evaluate efficacy and dosage of Formoterol and to compare efficacy of this drug with that of Salbutamol. As a result, it is considered that Formoterol has a strong dose dependent beta 2-effect with 40 micrograms of Formoterol almost as high as 4 mg of Salbutamol in beta 2-effect. In addition, Formoterol has almost no alpha-effect and its beta 1-effect can be considered negligible in the doses of 60 micrograms and 80 micrograms.
作者给健康成年人口服40、60和80微克作为新型支气管扩张剂研发的福莫特罗以及4毫克被认为是β2选择性药物的沙丁胺醇。为了评估福莫特罗的疗效和剂量，并将该药的疗效与沙丁胺醇进行比较，测量了心率、血压以及环磷酸鸟苷、游离脂肪酸、环磷酸腺苷、葡萄糖和乳酸的血药浓度。结果显示，福莫特罗具有很强的剂量依赖性β2效应，40微克福莫特罗的β2效应几乎与4毫克沙丁胺醇一样高。此外，福莫特罗几乎没有α效应，在60微克和80微克剂量下，其β1效应可忽略不计。
