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亲脂性二氢吡啶的临床优势。

Clinical advantages of lipophilic dihydropyridines.

作者信息

Mancia G, Omboni S, Zanchetti A

机构信息

Cattedra di Medicina Interna, Ospedale San Gerardo Monza, Università di Milano, Italy.

出版信息

Blood Press Suppl. 1998;2:23-6.

PMID:9850439
Abstract

Lipophilic dihydropyridines have many theoretical and practical clinical advantages owing to their long permanence at the cell membrane. They have a greater chance of smoothly and permanently reducing blood pressure over 24 h than other dihydropyridines, a feature that may have positive prognostic implications since 24-h blood pressure is more closely related to the end-organ damage of hypertension. They may avoid the sympathetic activation consequent to an excessive early-dose hypotension, which is responsible for an increase in 24-h blood-pressure variability and reflex tachycardia, two phenomena that may worsen the prognosis of hypertensive patients. A further advantage which has been shown in experimental and clinical settings is the possibility of reducing the extension and progression of atherogenic lesions in blood vessels, which are responsible for cardiovascular complications in hypertension. Some of these features have been shown by the novel lipophilic dihydropyridine lercanidipine. In particular, clinical studies have shown that (i) this drug is effective in homogeneously reducing blood pressure over 24 h, (ii) its antihypertensive effect is similar to that of some common antihypertensive drugs, and (iii) the rate of adverse events experienced with lercanidipine is no greater than that observed with other antihypertensive drugs, with special reference to non-lipophilic calcium antagonists. In particular, studies performed so far have shown that lercanidipine does not exert a dangerous reflex tachycardia.

摘要

由于亲脂性二氢吡啶类药物在细胞膜上的停留时间长,它们具有许多理论和临床实际优势。与其他二氢吡啶类药物相比,它们在24小时内平稳持久降低血压的可能性更大,这一特性可能具有积极的预后意义,因为24小时血压与高血压的终末器官损害更为密切相关。它们可以避免因早期剂量过大导致低血压而引起的交感神经激活,这种激活会导致24小时血压变异性增加和反射性心动过速,这两种现象可能会使高血压患者的预后恶化。在实验和临床研究中已显示出的另一个优势是,有可能减少血管中动脉粥样硬化病变的扩展和进展,而这些病变是高血压心血管并发症的原因。新型亲脂性二氢吡啶类药物乐卡地平已显示出其中一些特性。特别是,临床研究表明:(i)这种药物能在24小时内均匀有效地降低血压;(ii)其降压效果与一些常见降压药物相似;(iii)乐卡地平的不良事件发生率不高于其他降压药物,尤其是非亲脂性钙拮抗剂。特别是,迄今为止进行的研究表明,乐卡地平不会引起危险的反射性心动过速。

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