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[心力衰竭中的激素活性亢进。β受体阻滞剂的差异]

[Hormonal hyperactivity in heart failure. Differences in beta blockers].

作者信息

Beuckelmann Dirk J

机构信息

Klinik III für Innere Medizin, Universität zu Köln.

出版信息

Herz. 2002 Aug;27 Suppl 1:9-15.

Abstract

PATHOPHYSIOLOGY

Heart failure is characterized by a disturbed contractility and activation of neurohumoral mechanisms. Activation of the adrenergic system and the beta-adrenergic signal transduction pathway leads to downregulation of beta 1-receptors of the heart muscle cell membrane.

THERAPY

In addition to ACE inhibitors, diuretics and glycosides, beta blockers are an integral part in the combination therapy of patients with heart failure. Carvedilol, bisoprolol and metoprolol have been approved for use in patients with heart failure. Carvedilol is a nonselective beta-adrenoceptor antagonist with additional alpha 1-receptor-blocking properties. Furthermore, it has additional antioxidative and antiproliferative effects. Bisoprolol and metoprolol are beta 1-selective beta blockers without intrinsic sympathomimetic activity. Based on the results of the US carvedilol trials, the CIBIS-II trial, the MERIT-HF study and the COPERNICUS study, it has been shown that beta blocker therapy can improve the prognosis of patients with compensated heart failure (NYHA II and III) and carvedilol can improve prognosis in severe heart failure (stage IV). Induction of therapy must be performed using very low doses, that can be increased in 2- to 3-week intervals. Drug dosages should be increased as much as possible. Besides a better prognosis, clinical symptoms and left ventricular ejection fraction can be expected to improve. The final effect can be expected only after months up to 1 year. Therapy should continue lifelong.

CONCLUSION

In summary, beta blocker therapy of congestive heart failure has been established as an integral part in the combination therapy of patients with all clinical stages of heart failure.

摘要

病理生理学

心力衰竭的特征是收缩功能紊乱和神经体液机制激活。肾上腺素能系统和β-肾上腺素能信号转导通路的激活导致心肌细胞膜β1受体下调。

治疗

除了血管紧张素转换酶抑制剂、利尿剂和强心苷外,β受体阻滞剂是心力衰竭患者联合治疗中不可或缺的一部分。卡维地洛、比索洛尔和美托洛尔已被批准用于心力衰竭患者。卡维地洛是一种非选择性β肾上腺素受体拮抗剂,还具有α1受体阻断特性。此外,它还有额外的抗氧化和抗增殖作用。比索洛尔和美托洛尔是β1选择性β受体阻滞剂,无内在拟交感活性。基于美国卡维地洛试验、比索洛尔心脏衰竭研究II(CIBIS-II)试验、美托洛尔缓释片治疗心力衰竭(MERIT-HF)研究和卡维地洛前瞻性随机累积生存研究(COPERNICUS)研究的结果,已表明β受体阻滞剂治疗可改善代偿性心力衰竭(纽约心脏协会II级和III级)患者的预后,卡维地洛可改善重度心力衰竭(IV期)患者的预后。治疗必须从极低剂量开始,每2至3周增加一次剂量。应尽可能增加药物剂量。除了更好的预后外,临床症状和左心室射血分数有望改善。最终效果可能要数月至1年后才会显现。治疗应持续终身。

结论

总之,β受体阻滞剂治疗充血性心力衰竭已成为心力衰竭所有临床阶段患者联合治疗中不可或缺的一部分。

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