Sylvén C, Beermann B, Jonzon B, Brandt R
Br Med J (Clin Res Ed). 1986 Jul 26;293(6541):227-30. doi: 10.1136/bmj.293.6541.227.
In a study to characterise the chest pain induced by adenosine this agent was given as a bolus into a peripheral vein to six healthy volunteers (five men) aged 30-44. On the first day the maximum tolerable dose was determined in each case. On the second day three doses of adenosine (one third, two thirds, and the full maximum tolerable dose) and three doses of saline were given single blind in randomised order. Thereafter aminophylline 5 mg/kg was given and the procedure repeated in a different randomised order. On the third day between two thirds and the full maximum tolerable dose was given followed by 10 mg dipyridamole intravenously and a second injection of the same dose of adenosine. Heart rate and atrioventricular blocks were recorded by electrocardiography. One minute after each dose of adenosine the chest pain was scored. The maximum tolerable dose of adenosine ranged from 10.6 to 37.1 mg. All subjects experienced uneasy central chest pain provoking anxiety. The pain radiated to the shoulders, ulnar aspect of the arms, epigastric area, back, and into the throat. The pain began about 20 seconds after the injection and lasted 10-15 seconds. Increasing the dose of adenosine increased the intensity of the pain. Administration of aminophylline reduced the pain significantly. Second degree heart block was recorded in five of the six subjects during the time that the pain was experienced. After aminophylline no block was observed. Dipyridamole increased the intensity of pain. The duration of second degree heart block increased in four of the subjects, and in two of these third degree heart block occurred. These findings suggest that adenosine released from the myocardium during ischaemia induces angina pectoris by stimulating theophylline sensitive receptors.
在一项旨在描述腺苷诱发胸痛特征的研究中,将该药物以大剂量推注的方式经外周静脉给予6名年龄在30 - 44岁的健康志愿者(5名男性)。第一天,确定每种情况下的最大耐受剂量。第二天,以随机顺序单盲给予三剂腺苷(分别为最大耐受剂量的三分之一、三分之二和全量)以及三剂生理盐水。此后给予氨茶碱5mg/kg,并以不同的随机顺序重复该操作。第三天,给予介于最大耐受剂量三分之二和全量之间的腺苷,随后静脉注射10mg双嘧达莫,并再次注射相同剂量的腺苷。通过心电图记录心率和房室传导阻滞情况。每剂腺苷注射1分钟后对胸痛进行评分。腺苷的最大耐受剂量范围为10.6至37.1mg。所有受试者均经历引起焦虑的胸部中央不适疼痛。疼痛放射至肩部、手臂尺侧、上腹部、背部及咽喉部。疼痛在注射后约20秒开始,持续10 - 15秒。增加腺苷剂量会使疼痛强度增加。给予氨茶碱可显著减轻疼痛。6名受试者中有5名在经历疼痛期间记录到二度房室传导阻滞。给予氨茶碱后未观察到传导阻滞。双嘧达莫增加疼痛强度。4名受试者的二度房室传导阻滞持续时间增加,其中2名出现三度房室传导阻滞。这些发现提示,缺血时心肌释放的腺苷通过刺激对茶碱敏感的受体诱发心绞痛。