Akhras F, Jackson G
Department of Cardiology, Guy's and Lewisham Hospital, London, United Kingdom.
Drugs. 1989;38 Suppl 2:28-34. doi: 10.2165/00003495-198900382-00007.
Epanolol is a new once-daily agent for the treatment of angina pectoris. This study was conducted in 2 parts. Firstly, a dose-finding study was performed using placebo and epanolol 100, 200, 300 and 400mg to assess the efficacy and safety of the drug. Once-daily epanolol 200mg was an effective dose, significantly reducing angina attack rate and increasing exercise duration and work output. At the same time, an improvement was noted in the patients' well-being and their ability to undertake normal daily activities. The 200mg dose regimen was used in a long term (12 months) assessment of the efficacy and safety of epanolol in the second part of this study. The efficacy of epanolol was clearly maintained throughout the full treatment period without adverse events or withdrawals as a result of treatment. The effectiveness and safety of epanolol are attributed to its selective beta 1-partial agonist activity. At rest, the degree of agonist activity (about 20% of that of isoprenaline) may prevent some of the untoward effects occasionally seen with full beta-blockers. During exercise, the antagonist activity becomes apparent and cardiac ischaemia is reduced.
依泮洛尔是一种新型的每日一次用于治疗心绞痛的药物。本研究分两部分进行。首先,进行了一项剂量探索研究,使用安慰剂以及100、200、300和400毫克的依泮洛尔来评估该药物的疗效和安全性。每日一次服用200毫克依泮洛尔是有效剂量,可显著降低心绞痛发作率,并增加运动持续时间和工作量。同时,患者的健康状况以及进行正常日常活动的能力也有所改善。在本研究的第二部分中,采用200毫克剂量方案对依泮洛尔的疗效和安全性进行了长期(12个月)评估。在整个治疗期间,依泮洛尔的疗效得以明确维持,未出现不良事件,也没有因治疗而停药的情况。依泮洛尔的有效性和安全性归因于其选择性β1-部分激动剂活性。在静息状态下,激动剂活性程度(约为异丙肾上腺素的20%)可能会预防一些全β受体阻滞剂偶尔出现的不良影响。在运动期间,拮抗剂活性变得明显,心脏缺血得以减轻。