Brügmann U, Blasini R, Rudolph W
Herz. 1984 Aug;9(4):244-52.
Nisoldipine (Bay K5552), a newly-developed dehydropyridine derivative with calcium antagonistic properties, was found to have a duration of action twice as long as its parent compound, nifedipine, in laboratory experiments. To evaluate the anti-ischemic potency and duration of action, the effects of 10 mg nisoldipine after acute administration and at the end of three weeks of treatment with 10 mg twice daily were compared with those of 120 mg verapamil three times daily in a double-blind, randomized, crossover, placebo-controlled study. In twelve patients with angiographically-documented coronary artery disease and stable exertional angina pectoris, bicycle ergometry was performed before and at three and seven hours after medication on the first and 21st days of the three respective treatment phases. The control value at 8 a.m. on the 21st day corresponded with the ten-hour value on the 20th day of treatment. Between the three treatment phases, there was a one-week wash-out period during which the patients received placebo three times daily. At the time of the ergometric studies, blood was drawn for determination of verapamil plasma concentrations and, additionally, each patient recorded anginal attacks and nitrate consumption. Analysis was carried out for ST-segment depression in each patient at the highest comparable workload achieved in all treatment phases, the time to onset of 1 mm ST-segment depression as well as the response of the heart rate, systolic arterial blood pressure and the heart rate-blood pressure double-product both at rest and during exercise.(ABSTRACT TRUNCATED AT 250 WORDS)
尼索地平(Bay K5552)是一种新开发的具有钙拮抗特性的二氢吡啶衍生物,在实验室实验中发现其作用持续时间是其母体化合物硝苯地平的两倍。为评估抗缺血效力和作用持续时间,在一项双盲、随机、交叉、安慰剂对照研究中,将急性给药后及每日两次服用10 mg、连续治疗三周结束时10 mg尼索地平的效果,与每日三次服用120 mg维拉帕米的效果进行了比较。在12例经血管造影证实患有冠状动脉疾病且有稳定劳力性心绞痛的患者中,在三个相应治疗阶段的第一天和第21天服药后3小时和7小时以及服药前进行了自行车测力计运动测试。第21天上午8点的对照值与治疗第20天的10小时值相对应。在三个治疗阶段之间,有一个为期一周的洗脱期,在此期间患者每日三次服用安慰剂。在进行测力计运动测试时,采集血样以测定维拉帕米血浆浓度,此外,每位患者记录心绞痛发作情况和硝酸酯类药物的用量。对每位患者在所有治疗阶段达到的最高可比工作量时的ST段压低情况、出现1 mm ST段压低的时间以及静息和运动时心率、收缩期动脉血压和心率-血压乘积的反应进行了分析。(摘要截取自250字)