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双醋洛尔:其临床药理学及高血压治疗应用概述

Dilevalol: an overview of its clinical pharmacology and therapeutic use in hypertension.

作者信息

Lalonde R L, Tenero D M, Kazierad D J

机构信息

Department of Clinical Pharmacy, University of Tennessee, Memphis.

出版信息

Pharmacotherapy. 1990;10(1):15-28.

PMID:2179899
Abstract

Dilevalol is a novel antihypertensive drug that combines nonselective beta blockade with selective beta 2-receptor agonist activity. Its antihypertensive effect is mediated through arterial vasodilation and a decrease in systemic vascular resistance. At rest, dilevalol has little effect on heart rate or cardiac output. The drug is rapidly and completely absorbed but undergoes significant first-pass hepatic extraction. Its elimination half-life of approximately 12 hours allows for once-daily administration. In controlled clinical trials, dilevalol was at least as effective as angiotensin-converting enzyme inhibitors and comparable to beta blockers in antihypertensive efficacy. Preliminary data indicate that dilevalol reverses left ventricular hypertrophy in some patients. It does not adversely affect renal function and may have a favorable effect on plasma lipids, especially high-density lipoprotein cholesterol. The agent is usually well tolerated and may prove to be a useful addition to our antihypertensive drugs.

摘要

地来洛尔是一种新型抗高血压药物,它兼具非选择性β受体阻滞作用和选择性β2受体激动活性。其降压作用是通过动脉血管舒张和全身血管阻力降低来介导的。在静息状态下,地来洛尔对心率或心输出量影响很小。该药吸收迅速且完全,但会经历显著的首过肝提取。其约12小时的消除半衰期允许每日给药一次。在对照临床试验中,地来洛尔的降压效果至少与血管紧张素转换酶抑制剂相当,且在降压疗效上与β受体阻滞剂相当。初步数据表明,地来洛尔可使部分患者的左心室肥厚逆转。它对肾功能无不良影响,可能对血脂,尤其是高密度脂蛋白胆固醇有有益作用。该药物通常耐受性良好,可能会被证明是我们抗高血压药物中的一种有用补充。

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