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塞利洛尔的临床展望:心脏保护潜力

Clinical perspective on celiprolol: cardioprotective potential.

作者信息

Frishman W H

机构信息

Department of Medicine, Albert Einstein College of Medicine, Montefiore Medical Center, Bronx, NY 10461.

出版信息

Am Heart J. 1991 Feb;121(2 Pt 2):724-9. doi: 10.1016/0002-8703(91)90453-o.

Abstract

beta-Adrenergic blockers have had widespread use in the treatment of cardiovascular disease. Some agents of this class have been shown to reduce the incidence of total mortality, cardiovascular mortality, sudden death, and nonfatal reinfarction in survivors of acute myocardial infarction. The mechanism for this cardioprotective action is not known. Antiarrhythmic action and hemodynamic alterations have been suggested as possible mechanisms. An anticoagulant mechanism is another possibility, although the antiplatelet effects of beta-blockers are weak. It is now believed that antithrombotic effects may be related to the prevention of coronary artery plaque rupture and the subsequent propagation of an occlusive arterial thrombus rather than a direct anticoagulant action. The therapeutic ability beta-blockers to attenuate the hemodynamic consequences of catecholamine surgers, as they do in aortic dissection, may protect a vulnerable plaque from fracture, reducing the risk of coronary thrombosis, myocardial infarction, and death. Celiprolol, a third-generation beta 1-selective adrenergic blocker with partial beta 2-agonist activity, is comparable to other beta-blockers in antihypertensive and antianginal activity. It has additional actions that may be beneficial to patients: (1) it does not adversely affect lipids and lipoproteins; (2) it does not appear to depress the myocardium in patients with left ventricular dysfunction; (3) it can lower serum fibrinogen levels; and (4) it can cause regression of myocardial mass in patients with left ventricular hypertrophy.

摘要

β-肾上腺素能阻滞剂已广泛应用于心血管疾病的治疗。这类药物中的一些已被证明可降低急性心肌梗死幸存者的总死亡率、心血管死亡率、猝死率以及非致命性再梗死的发生率。这种心脏保护作用的机制尚不清楚。抗心律失常作用和血流动力学改变被认为是可能的机制。抗凝机制是另一种可能性,尽管β-阻滞剂的抗血小板作用较弱。现在认为,抗血栓作用可能与预防冠状动脉斑块破裂及随后闭塞性动脉血栓的形成有关,而非直接的抗凝作用。β-阻滞剂减弱儿茶酚胺激增引起的血流动力学后果的治疗能力,就像它们在主动脉夹层中所起的作用一样,可能会保护易损斑块不发生破裂,降低冠状动脉血栓形成、心肌梗死和死亡的风险。塞利洛尔是一种具有部分β2激动剂活性的第三代β1选择性肾上腺素能阻滞剂,在降压和抗心绞痛活性方面与其他β-阻滞剂相当。它还有一些可能对患者有益的额外作用:(1)它不会对脂质和脂蛋白产生不利影响;(2)它似乎不会使左心室功能不全患者的心肌受到抑制;(3)它可降低血清纤维蛋白原水平;(4)它可使左心室肥厚患者的心肌质量减轻。

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