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β受体阻滞剂在高血压治疗中药物学差异的潜在意义。

Possible significance of the pharmacological differentiation of beta-blockers for therapy of hypertension.

作者信息

Leenen F H

出版信息

Br J Clin Pharmacol. 1979;7 Suppl 2(Suppl 2):173S-184S. doi: 10.1111/j.1365-2125.1979.tb04688.x.

Abstract

1 Cardioselective and non-selective beta-blockers affect to a different degree several aspects of the circulatory homeostasis. The evidence available in this regard has been evaluated and the possible clinical importance of these differences has been discussed. 2 Venous return in partly regulated by beta-receptors (possibly of the beta 2 type) in the venous resistance vessels. Differences in blockade of venous return by the two classes of beta-blockers may, therefore, influence the degree of increase in left ventricular size, left ventricular end diastolic BPs and stroke volume during beta-blockade. 3 At the first part of the dose-reponse curve, non-selective beta-blockers seem to block more effectively renin release than cardioselective beta-blockers. 4 The direction and the extent to which beta-blockers 'directly' affect total peripheral resistance (TPR), is determined by the resultant of the degree of decrease in TPR by blockade of renin release and the extent of the increase in TPR by blockade of the beta 2-receptors in the arteriolar wall. 5 The clinical relevance of these differences could be that--especially in the low doses range--non-selective beta-blockers may be more 'safe' in patients with compromised cardiac function and may be more appropriate for the therapy of high renin hypertension than cardioselective blockers, whereas the latter may be more appropriate for the majority of hypertensive patients who have low to normal renin hypertension.

摘要
  1. 心脏选择性和非选择性β受体阻滞剂对循环稳态的多个方面有不同程度的影响。已对这方面的现有证据进行了评估,并讨论了这些差异可能具有的临床重要性。2. 静脉回流部分受静脉阻力血管中的β受体(可能是β2型)调节。因此,两类β受体阻滞剂在阻断静脉回流血量方面的差异可能会影响β受体阻滞剂治疗期间左心室大小、左心室舒张末期血压和心搏量的增加程度。3. 在剂量反应曲线的第一部分,非选择性β受体阻滞剂似乎比心脏选择性β受体阻滞剂更有效地阻断肾素释放。4. β受体阻滞剂“直接”影响总外周阻力(TPR)的方向和程度,取决于因阻断肾素释放导致的TPR降低程度与因阻断小动脉壁上的β2受体导致的TPR增加程度之间的综合结果。5. 这些差异的临床意义可能在于——尤其是在低剂量范围内——对于心功能受损的患者,非选择性β受体阻滞剂可能更“安全”,并且对于高肾素性高血压的治疗可能比心脏选择性阻滞剂更合适,而后者可能更适合大多数肾素水平低至正常的高血压患者。

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