Frishman William H, Henderson Linda S, Lukas Mary Ann
Departments of Medicine and Pharmacology, New York Medical College/Westchester Medical Center, Valhalla, NY 10595, USA.
Vasc Health Risk Manag. 2008;4(6):1387-400. doi: 10.2147/vhrm.s3148.
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.
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。