Saltissi S, Crowther A, Byrne C, Coltart D J
Br J Clin Pharmacol. 1981 May;11(5):497-503. doi: 10.1111/j.1365-2125.1981.tb01156.x.
1 The demonstration of histamine (H2) receptors in the cardiovascular system in man and the widespread use of the specific H2 receptor antagonist cimetidine for the treatment of peptic ulcer has necessitated assessment of the cardiovascular effects of this drug during oral therapy in man. 2 Consequently, nineteen patients with a history of peptic ulcer but in symptomatic remission underwent a double-blind crossover trial of oral cimetidine v placebo, each treatment period lasting 4 weeks. No significant difference in various cardiac parameters at rest (heart rate, blood pressure, ECG) or following a maximal treadmill exercise test (time-into-protocol, maximum heart rate and blood pressure) was found between the groups. Similarly, cimetidine produced no change in the incidence of ventricular ectopics or in heart rate on 24 h ambulatory monitoring and had no effect on left ventricular volume or contractility as measured by echocardiography. 3 Thus oral administration of cimetidine in a dose of 400 mg four times daily was associated with no demonstrable cardiovascular changes. In addition, since this dose is thought compatible with cardiovascular H2 receptor blockade this study favours the lack of a physiological role for these receptors in man.
1 在人体心血管系统中组胺(H2)受体的证实以及特异性H2受体拮抗剂西咪替丁在消化性溃疡治疗中的广泛应用,使得有必要评估该药物在人体口服治疗期间的心血管效应。2 因此,19例有消化性溃疡病史但症状已缓解的患者接受了口服西咪替丁与安慰剂的双盲交叉试验,每个治疗期持续4周。两组之间在静息时的各种心脏参数(心率、血压、心电图)或最大平板运动试验后(进入试验时间、最大心率和血压)均未发现显著差异。同样,西咪替丁在24小时动态监测中对室性早搏发生率或心率没有影响,并且对通过超声心动图测量的左心室容积或收缩性也没有影响。3 因此,每日4次口服400毫克西咪替丁未出现可证实的心血管变化。此外,由于该剂量被认为与心血管H2受体阻断作用相符,本研究支持这些受体在人体中缺乏生理作用的观点。