Kostis J B, Frishman W, Hosler M H, Thorsen N L, Gonasun L, Weinstein J
Am Heart J. 1982 Aug;104(2 Pt 2):496-504. doi: 10.1016/0002-8703(82)90146-6.
Although all beta blockers have been found to be effective in the symptomatic relief of angina pectoris, the importance of intrinsic sympathomimetic activity (ISA) has not been studied extensively. In a randomized, double-blind study, we administered equipotent doses of propranolol (10, 20, and 40 mg four times a day) and pindolol (2.5, 5, and 10 mg four times a day), a beta blocker with significant ISA, to 52 patients with angina. Both agents were found to be effective in the treatment of angina. At peak dose, propranolol reduced the number of angina attacks per 2 weeks from 29.29 +/- 4.79 to 18.0 +/- 4.4 (p = 0.021) (a 39% reduction) and increased the exercise tolerance on the treadmill from 7.55 +/- 0.67 METS to 9.36 +/- 0.58 (p = 0.002). Pindolol decreased the number of anginal attacks per 2 weeks from 16.48 +/- 2.63 to 8.65 +/- 2.46 (p = 0.0027) (a 48% reduction) and increased exercise tolerance from 7.95 +/- 0.56 METS to 9.40 +/- 0.57 (p = 0.0245). At the end of the maximum tolerated exercise, propranolol decreased the heart rate from 110.00 +/- 3.41 to 99.71 +/- 3.74 (p = 0.0015). Pindolol also decreased the heart rate at the maximum tolerated exercise from 113.59 +/- 3.24 to 108.12 +/- 3.16 (p = 0.0102). At rest, however, propranolol induced a more pronounced (p = 0.0066) decrease in heart rate (from 69.00 +/- 1.85 to 61.50 +/- 1.99; p = 0.0018), whereas pindolol did not significantly affect the resting heart rate (65.37 +/- 1.47 to 65.5 +/- 1.44; p = 0.9392). In addition propranolol decreased echocardiographically determined ejection fraction from 0.57 +/- 0.02 to 0.15 +/- 0.01 (p = 0.04) and increased the left ventricular end-diastolic volume from 71.8 +/- 3.2 to 92.2 +/- 1.9 ml (p = 0.003), whereas pindolol did not affect the ejection fraction and caused a less pronounced (p = 0.03) increase in end-diastolic volume (from 70.8 +/- 1.8 to 80.2 +/- 2.8; p = 0.02). The data indicate that both propranolol and pindolol are effective in the treatment of angina pectoris and that pindolol decreases the resting heart rate and ejection fraction and increases the left ventricular end-diastolic volume to a lesser extent than propranolol.
尽管已发现所有β受体阻滞剂在缓解心绞痛症状方面均有效,但对内在拟交感活性(ISA)的重要性尚未进行广泛研究。在一项随机双盲研究中,我们给52例心绞痛患者服用等效剂量的普萘洛尔(每日4次,每次10、20和40 mg)和吲哚洛尔(每日4次,每次2.5、5和10 mg),后者是一种具有显著ISA的β受体阻滞剂。发现两种药物在治疗心绞痛方面均有效。在峰值剂量时,普萘洛尔使每2周心绞痛发作次数从29.29±4.79次降至18.0±4.4次(p = 0.021)(降低39%),并使跑步机运动耐量从7.55±0.67梅脱增加到9.36±0.58(p = 0.002)。吲哚洛尔使每2周心绞痛发作次数从16.48±2.63次降至8.65±2.46次(p = 0.0027)(降低48%),并使运动耐量从7.95±0.56梅脱增加到9.40±0.57(p = 0.0245)。在最大耐受运动结束时,普萘洛尔使心率从110.00±3.41次/分降至99.71±3.74次/分(p = 0.0015)。吲哚洛尔在最大耐受运动时也使心率从113.59±3.24次/分降至108.12±3.16次/分(p = 0.0102)。然而,在静息状态下,普萘洛尔使心率更显著降低(p = 0.0066)(从69.00±1.85次/分降至61.50±1.99次/分;p = 0.0018),而吲哚洛尔对静息心率无显著影响(从65.37±1.47次/分至65.5±1.44次/分;p = 0.9392)。此外,普萘洛尔使超声心动图测定的射血分数从0.57±0.02降至0.15±0.01(p = 0.04),并使左心室舒张末期容积从71.8±3.2 ml增加到92.2±1.9 ml(p = 0.003),而吲哚洛尔不影响射血分数,且使舒张末期容积增加程度较小(p = 0.03)(从70.8±1.8 ml至80.2±2.8 ml;p = 0.02)。数据表明,普萘洛尔和吲哚洛尔在治疗心绞痛方面均有效,且吲哚洛尔降低静息心率和射血分数以及增加左心室舒张末期容积的程度均小于普萘洛尔。