三种选择性β a1受体阻滞剂β a1选择性的比较。

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纳托尔，劳特利奇，肯德尔MJ

三种选择性β a1受体阻滞剂β a1选择性的比较。

中华临床医药杂志2003 Jun;28(3):179-86。

PubMed ID
12795776 (PubMed视图
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摘要

目的:通过评估三种β -受体阻滞剂(奈比伏洛尔、比索洛尔和阿替洛尔)对特布他林输注的β - 2介导的血流动力学和生化反应的影响，确定正常治疗剂量口服的β -受体阻滞剂β - 1的相对选择性，从而降低血清钾，增加血清葡萄糖和胰岛素。方法:24名健康志愿者(14男，10女)，无呼吸道疾病史，参加了5个不同的场合;β -受体阻滞剂(奈比伏洛5mg，比索洛尔10mg，阿替洛尔50mg和100mg)或安慰剂按随机顺序提供。在服用受体阻滞剂后65-85分钟采集3份基线血样。服用受体阻滞剂90分钟后开始60分钟特布他林输注。输液后每隔15分钟至30分钟采集血样，记录血压和心率。分析血液样本的血清钾、葡萄糖和胰岛素浓度。结果:特布他林可增加心率。奈比洛尔预处理对特布他林引起的心动过速有中度和不显著的降低，而比索洛尔产生了更显著的效果。阿替洛尔50mg和100mg剂量均可显著降低特布他林诱导的心动过速。 All active preparations had a comparable impact on the terbutaline-induced increase in systolic blood pressure, but the drugs had no impact on the changes produced in diastolic blood pressure. After pretreatment with placebo, the terbutaline infusion caused a significant decrease in serum potassium and increases in serum glucose and insulin. Pretreatment with nebivolol had no discernible effect on potassium compared with placebo. In contrast, when compared with either placebo or nebivolol, bisoprolol (P < 0.01) and both doses of atenolol (P < 0.001) significantly attenuated the hypokalaemic effect of terbutaline. Treatment with nebivolol and bisoprolol modestly but significantly reduced the terbutaline-induced increases in glucose (P < 0.05). The blocking effects of both doses of atenolol were highly significant (P < 0.001) when compared with placebo and also significant (P < 0.05 and P < 0.01, respectively) when compared with nebivolol and bisoprolol. A similar pattern of responses with the different beta-blocker treatments was observed for the effects on insulin concentrations during the terbutaline infusion. CONCLUSION: The beta1-selectivity of three different beta1-blockers has been demonstrated in healthy volunteers using the blocking of biochemical and haemodynamic responses to a beta2 stimulus. Terbutaline alone caused an increase in heart rate, a rise in systolic blood pressure, a fall in serum potassium and a rise in both serum glucose and insulin. In this study, for both haemodynamic and biochemical responses, atenolol 100 mg had the greatest beta2-blocking effect, nebivolol 5 mg the least. Bisoprolol 10 mg and atenolol 50 mg had intermediate effects; bisoprolol was the more beta1-selective of these two.

引用本文的药物库数据

药物
药物靶点
药物 目标 种类 生物 药理作用 行动
阿替洛尔 -2肾上腺素能受体 蛋白质 人类
未知的
拮抗剂
 细节
Nebivolol -2肾上腺素能受体 蛋白质 人类
未知的
拮抗剂
 细节
Pharmaco-metabolomics
药物 药物组 代谢物 改变 描述
Nebivolol 批准临床实验 葡萄糖
减少		 Nebivolol减少的水平葡萄糖在血液中
特布他林 批准 葡萄糖
增加		 特布他林增加的水平葡萄糖在血液中
特布他林 批准 钾
减少		 特布他林减少的水平钾在血液中
Pharmaco-proteomics
药物 药物组 基因 基因身份证 改变 交互 染色体
特布他林 批准 INS 3630
增加		 特布他林可增加INS蛋白的表达 11 p15.5
特布他林 批准 INS 3630
增加		 特布他林可增加INS蛋白的表达 11 p15.5
特布他林 批准 INS 3630
增加		 特布他林可增加INS蛋白的表达 11 p15.5
特布他林 批准 INS 3630
增加		 特布他林可增加INS蛋白的表达 11 p15.5
特布他林 批准 INS 3630
增加		 特布他林可增加INS蛋白的表达 11 p15.5