Haffner C A, Horton R C, Lewis H M, Hughes B, Kendall M J
Department of Medicine, Queen Elizabeth Hospital, Birmingham, UK.
J Hum Hypertens. 1992 Oct;6(5):397-400.
Twelve healthy volunteers were given single oral doses of bisoprolol 5 mg, 10 mg and 20 mg and atenolol 50 mg and 100 mg in a randomised, placebo-controlled study. The effects of these drugs on beta 2-stimulated hypokalaemia and hyperglycaemia (produced by intravenous terbutaline infusion) were studied. Comparable beta-blockade was achieved with bisoprolol 20 mg, and atenolol 50 mg and 100 mg as measured by attenuation of exercise heart rate. Measurements of areas under or over the curve (AUC and AOC) of hypokalaemic or hyperglycaemic response to terbutaline infusion showed that bisoprolol (10 mg and 20 mg) and atenolol (50 mg and 100 mg) were significantly less beta 1 selective than 5 mg bisoprolol. Furthermore, there was a trend towards decreasing beta 1 selectivity with increasing doses of bisoprolol. Bisoprolol, an effective once daily antihypertensive and antianginal treatment, has comparable beta 1 selectivity to atenolol as measured by metabolic response. At a dose of 5 mg, bisoprolol has a measurable impact on beta 1 receptors but minimal effect on beta 2 receptors.
在一项随机、安慰剂对照研究中，12名健康志愿者分别单次口服5毫克、10毫克和20毫克比索洛尔以及50毫克和100毫克阿替洛尔。研究了这些药物对β2刺激引起的低钾血症和高血糖症（由静脉输注特布他林产生）的影响。通过运动心率的衰减来衡量，20毫克比索洛尔、50毫克和100毫克阿替洛尔可实现相当的β受体阻滞作用。对特布他林输注的低钾血症或高血糖症反应的曲线下或曲线上面积（AUC和AOC）测量显示，10毫克和20毫克比索洛尔以及50毫克和100毫克阿替洛尔的β1选择性明显低于5毫克比索洛尔。此外，随着比索洛尔剂量增加，β1选择性有降低的趋势。比索洛尔是一种有效的每日一次抗高血压和抗心绞痛治疗药物，通过代谢反应衡量，其β1选择性与阿替洛尔相当。在5毫克剂量时，比索洛尔对β1受体有可测量的影响，但对β2受体的影响最小。
