Tangø M, Carlsen J E, Trap-Jensen J
Eur J Clin Pharmacol. 1985;29(2):155-8. doi: 10.1007/BF00547414.
Dose-response curves for heart rate, arterial blood pressure, cardiac output, total peripheral resistance, systolic time intervals, forearm blood flow and forearm vascular resistance were obtained after i.v. administration of seven logarithmically increasing doses of xamoterol to 8 healthy volunteers. The total cumulative dose was 0.2 mg/kg b.w. At rest after the seventh dose of xamoterol heart rate, systolic blood, pressure, cardiac output and forearm blood flow were increased by 10%, 20%, 23% and 41%, respectively. Diastolic blood pressure was unchanged. Forearm vascular resistance was reduced by 21% and total peripheral resistance by 10%. Systolic time intervals were reduced: total electromechanical systole index (QS2I), left ventricular ejection time index (LVETI), pre ejection period index (PEPI) and PEP/LVET ratio by 4%, 2%, 12% and 14%, respectively. No side-effects were observed. During upright exercise after the seventh dose of xamoterol heart rate was reduced by 11% and systolic BP by 6%. Diastolic blood pressure was unchanged. Thus xamoterol increased the contractility of the heart with only a small increase in heart rate, increased systolic blood pressure and caused vasodilatation in resting skeletal muscle. During exercise the reduction in heart rate and blood pressure suggests beta-adrenoceptor blocking activity of the drug.
对8名健康志愿者静脉注射7个对数递增剂量的昔莫洛尔后,获得了心率、动脉血压、心输出量、总外周阻力、收缩期时间间期、前臂血流量和前臂血管阻力的剂量-反应曲线。总累积剂量为0.2mg/kg体重。在注射第七剂昔莫洛尔后的静息状态下,心率、收缩压、心输出量和前臂血流量分别增加了10%、20%、23%和41%。舒张压未改变。前臂血管阻力降低了21%,总外周阻力降低了10%。收缩期时间间期缩短:总电机械收缩期指数(QS2I)、左心室射血时间指数(LVETI)、射血前期指数(PEPI)和PEP/LVET比值分别降低了4%、2%、12%和14%。未观察到副作用。在注射第七剂昔莫洛尔后的直立运动过程中,心率降低了11%,收缩压降低了6%。舒张压未改变。因此,昔莫洛尔增加了心脏的收缩力,仅使心率略有增加,提高了收缩压,并引起静息骨骼肌血管舒张。在运动过程中,心率和血压的降低表明该药物具有β-肾上腺素能受体阻断活性。