比较三个beta1-selective beta1-selectivity的β受体阻断剂。
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劳特利奇HC, Nuttall SL肯德尔乔丹
比较三个beta1-selective beta1-selectivity的β受体阻断剂。
中国制药。2003年6月,28 (3):179 - 86。
- PubMed ID
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12795776 (在PubMed]
- 文摘
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目的:确定的相对beta1-selectivity 3β受体阻滞剂(nebivolol、比索洛尔、阿替洛尔),在正常治疗剂量的口服药物,通过评估其影响beta2-mediated,特布他林注入血液动力学的生化反应,降低血清钾和增加血清葡萄糖和胰岛素。方法:24名健康志愿者(14人,10女性),无呼吸道疾病史,参加了五次;阻滞剂(nebivolol 5毫克,比索洛尔10毫克,阿替洛尔50和100毫克)或安慰剂在随机顺序提供。三个基准收集血液样本65 - 85分钟post-beta-blocker。一个点特布他林输液开始后90分钟服用β受体阻滞剂。血液采集标本,记录血压和心率每隔15分钟到30分钟和。血液样本进行分析对血清钾、葡萄糖和胰岛素浓度。结果:特布他林心率增加。预处理nebivolol造成适度的和非重大减少terbutaline-induced心动过速而比索产生更为显著的影响。阿替洛尔在50和100毫克剂量在terbutaline-induced心动过速引起高度显著减少。 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.
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