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控释卡维地洛在系统性高血压和心肌功能障碍治疗中的应用

Controlled-release carvedilol in the management of systemic hypertension and myocardial dysfunction.

作者信息

Frishman William H, Henderson Linda S, Lukas Mary Ann

机构信息

Departments of Medicine and Pharmacology, New York Medical College/Westchester Medical Center, Valhalla, NY 10595, USA.

出版信息

Vasc Health Risk Manag. 2008;4(6):1387-400. doi: 10.2147/vhrm.s3148.

Abstract

Cardiovascular disease is the leading cause of death worldwide. Within the treatment armamentarium, beta-blockers have demonstrated efficacy across the spectrum of cardiovascular disease--from modification of a risk factor (ie, hypertension) to treatment after an acute event (ie, myocardial infarction). Recently, the use of beta-blockers as a first-line therapy in hypertension has been called into question. Moreover, beta-blockers as a class are saddled with a misperception of having poor tolerability. However, vasodilatory beta-blockers such as carvedilol have a different hemodynamic action that provides the benefits of beta-blockade with the addition of vasodilation resulting from alpha 1-adrenergic receptor blockade. Vasodilation reduces total peripheral resistance, which may produce an overall positive effect on tolerability. Recently, a new, controlled-release carvedilol formulation has been developed that provides the clinical efficacy of carvedilol but is indicated for once-daily dosing. This review presents an overview of the clinical and pharmacologic carvedilol controlled-release data.

摘要

心血管疾病是全球首要死因。在治疗手段中,β受体阻滞剂已在心血管疾病的各个方面展现出疗效——从危险因素的改善(即高血压)到急性事件后的治疗(即心肌梗死)。最近,β受体阻滞剂作为高血压一线治疗药物的应用受到了质疑。此外,β受体阻滞剂这一类药物还背负着耐受性差的误解。然而,像卡维地洛这样的血管舒张性β受体阻滞剂具有不同的血流动力学作用,它在β受体阻滞的基础上,通过α1肾上腺素能受体阻滞增加了血管舒张作用。血管舒张降低了总外周阻力,这可能对耐受性产生总体上的积极影响。最近,一种新的控释卡维地洛制剂已被研发出来,它具有卡维地洛的临床疗效,但适用于每日一次给药。本综述概述了卡维地洛控释制剂的临床和药理学数据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/19e9/2663448/1577b3fbfaa1/vhrm-4-1387f1.jpg

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