Bauer K, Dietersdorfer F, Sertl K, Kaik B, Kaik G
Department of Internal Medicine, University of Vienna Medical School, Austria.
Clin Pharmacol Ther. 1993 Jan;53(1):76-83. doi: 10.1038/clpt.1993.11.
The airway and tremor response and cardiovascular and hypokalemic effects of single doses of inhalative fenoterol dry powder capsules (0.4 mg) were compared with the fenoterol metered dose inhaler (0.4 mg) and colforsin (forskolin) dry powder capsules (10.0 mg), a direct activator of the adenylate cyclase system, in 16 patients with asthma. Subjects (FEV1 < or = 60% predicted) were investigated in a randomized, double-masked, placebo-controlled, four-period, crossover trial for a 120 minute period. All active drugs caused a significant increase in specific airway conductance (p < 0.05); the order of potency (mean +/- SEM maximum increase from baseline) was fenoterol metered dose inhaler (0.51 +/- 0.06 sec-1 x kPa-1), fenoterol dry powder capsules (0.49 +/- 0.07), and colforsin dry powder capsules (0.30 +/- 0.03). A marked increase in finger tremor amplitude resulted after fenoterol metered dose inhaler only (62.93% +/- 10.21%; p < 0.05) in contrast to fenoterol dry powder capsules (15.84% +/- 4.35%; p < 0.05) and colforsin dry powder capsules (12.87% +/- 10.44%; p > 0.05). A decrease in plasma potassium was found after fenoterol (metered dose inhaler > dry powder capsules; p < 0.05). In conclusion, fenoterol dry powder capsules caused less tremor response and hypokalemic effects than the metered dose inhaler, although the bronchodilator capacity was similar. Colforsin dry powder capsules resulted in a measurable bronchodilatation in patients with asthma.
在16例哮喘患者中，比较了单剂量吸入用非诺特罗干粉胶囊（0.4毫克）与非诺特罗定量气雾剂（0.4毫克）以及可福辛（福斯高林）干粉胶囊（10.0毫克，一种腺苷酸环化酶系统直接激活剂）的气道和震颤反应、心血管及低钾血症效应。受试者（第一秒用力呼气量≤预测值的60%）参与了一项随机、双盲、安慰剂对照、四阶段交叉试验，为期120分钟。所有活性药物均使比气道传导率显著增加（p<0.05）；效力顺序（从基线起平均±标准误最大增加量）为非诺特罗定量气雾剂（0.51±0.06秒-1×千帕-1）、非诺特罗干粉胶囊（0.49±0.07）和可福辛干粉胶囊（0.30±0.03）。仅使用非诺特罗定量气雾剂后手指震颤幅度显著增加（62.93%±10.21%；p<0.05），相比之下，非诺特罗干粉胶囊（15.84%±4.35%；p<0.05）和可福辛干粉胶囊（12.87%±10.44%；p>0.05）。使用非诺特罗后发现血钾降低（定量气雾剂>干粉胶囊；p<0.05）。总之，非诺特罗干粉胶囊引起的震颤反应和低钾血症效应比定量气雾剂少，尽管支气管扩张能力相似。可福辛干粉胶囊在哮喘患者中导致了可测量的支气管扩张。
