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使用具有或不具有内在拟交感活性的β受体阻滞剂治疗高血压。

Treatment of hypertension with beta-blockers with and without intrinsic sympathomimetic activity.

作者信息

Hansson L, Svensson A, Gudbrandsson T, Sivertsson R

出版信息

J Cardiovasc Pharmacol. 1983;5 Suppl 1:S26-9. doi: 10.1097/00005344-198300051-00005.

Abstract

In a randomized double-blind trial 36 patients with essential hypertension were treated with either metoprolol or pindolol for 6 months following a 6-week placebo period. At the end of the placebo period and after 6 weeks and 6 months of active therapy peripheral hemodynamics at rest and during maximal vasodilatation were studied. Exercise heart rate was reduced to the same extent with both metoprolol and pindolol, indicating that the doses used (metoprolol average 179 mg/day; pindolol average 12 mg/day) were equipotent as regards beta-adrenoceptor blocking effect. The antihypertensive effect was identical with both compounds. However, metoprolol caused a significant reduction of heart rate at rest both at 6 weeks and 6 months. With pindolol the reduction in heart rate was not significant at 6 weeks, and it was clearly much less than with metoprolol. On the other hand, no change in calf vascular resistance was seen during metoprolol therapy, whereas a marked and statistically significant reduction was caused by pindolol. Resistance at maximal dilatation in the forearm did not change with metoprolol, but tended to fall with pindolol after 6 weeks and was significantly reduced after 6 months. This indicates that although metoprolol and pindolol have the same antihypertensive potency, the two agents appear to reduce blood pressure through different mechanisms. Thus, cardiac mechanisms seem to play the most important role with metoprolol, whereas pindolol mainly acts by a reduction in vascular resistance. It also seems that treatment with pindolol normalizes the structural arteriolar abnormality present in hypertension as indicated by the reduction in resistance at maximal vasodilation.

摘要

在一项随机双盲试验中,36例原发性高血压患者在经过6周安慰剂期后,用美托洛尔或吲哚洛尔治疗6个月。在安慰剂期末以及积极治疗6周和6个月后,研究了静息和最大血管扩张时的外周血流动力学。美托洛尔和吲哚洛尔使运动心率降低的程度相同,这表明所用剂量(美托洛尔平均179毫克/天;吲哚洛尔平均12毫克/天)在β-肾上腺素能受体阻断作用方面是等效的。两种化合物的降压效果相同。然而,美托洛尔在6周和6个月时均使静息心率显著降低。使用吲哚洛尔时,6周时心率降低不显著,且明显低于美托洛尔。另一方面,美托洛尔治疗期间小腿血管阻力无变化,而吲哚洛尔则导致显著且有统计学意义的降低。美托洛尔治疗后前臂最大扩张时的阻力无变化,但吲哚洛尔在6周后有下降趋势,6个月后显著降低。这表明尽管美托洛尔和吲哚洛尔具有相同的降压效力,但两种药物似乎通过不同机制降低血压。因此,心脏机制在美托洛尔作用中似乎起最重要作用,而吲哚洛尔主要通过降低血管阻力起作用。似乎吲哚洛尔治疗可使高血压患者存在的结构性小动脉异常恢复正常,这表现为最大血管扩张时阻力降低。

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