Quyyumi A A, Wright C, Mockus L, Fox K M
Br Med J (Clin Res Ed). 1984 Oct 13;289(6450):951-3. doi: 10.1136/bmj.289.6450.951.
The use of beta adrenoceptor blockade in the treatment of rest angina is controversial, and the effects on severe angina of partial agonist activity in beta blockers are unknown. Eight patients with effort angina and seven with effort and nocturnal angina and severe coronary artery disease were studied initially when they were not taking any antianginal drugs. Pindolol 5 mg thrice daily (with partial agonist activity) and atenolol 100 mg daily (without partial agonist activity) were given for five days each in a double blind randomised manner. Diaries of angina were kept and treadmill exercise testing and ambulatory ST monitoring performed during the last 48 hours of each period of treatment. Daytime and nocturnal resting heart rates and the frequency of angina were significantly reduced by atenolol compared with pindolol (p less than 0.01). The duration of exercise was significantly increased and the frequency, duration, and magnitude of daytime and nocturnal episodes of ST segment depression on ambulatory monitoring were reduced by atenolol. Reduction in resting heart rate is important in the treatment of both effort and nocturnal angina. Partial agonist activity in beta adrenoceptor antagonists may be deleterious in patients with severe angina pectoris.
β肾上腺素能受体阻滞剂用于治疗静息性心绞痛存在争议，且β受体阻滞剂的部分激动剂活性对严重心绞痛的影响尚不清楚。最初对8例劳力性心绞痛患者和7例劳力性及夜间心绞痛伴严重冠状动脉疾病患者进行研究，当时他们未服用任何抗心绞痛药物。以双盲随机方式分别给予吲哚洛尔5毫克每日三次（具有部分激动剂活性）和阿替洛尔100毫克每日一次（无部分激动剂活性），各给药5天。记录心绞痛日记，并在每个治疗阶段的最后48小时进行平板运动试验和动态ST段监测。与吲哚洛尔相比，阿替洛尔使白天和夜间静息心率及心绞痛发作频率显著降低（p<0.01）。阿替洛尔使运动持续时间显著延长，动态监测时白天和夜间ST段压低发作的频率、持续时间和幅度降低。静息心率降低对劳力性和夜间心绞痛的治疗均很重要。β肾上腺素能受体拮抗剂中的部分激动剂活性可能对严重心绞痛患者有害。
