Eggertsen R, Andrén L, Sivertsson R, Hansson L
Eur J Clin Pharmacol. 1984;27(1):19-22.
Carvedilol (BM 14190) is a new compound with combined nonselective beta-adrenoceptor blocking activity, devoid of ISA, and a precapillary vasodilating effect. Its acute haemodynamic effects were studied by invasive techniques in 10 patients given 25 mg carvedilol and noninvasively in 10 patients given 25 mg and in 10 given 50 mg orally. All had essential hypertension. In the invasive study intraarterial blood pressure was measured and cardiac output was determined by the dye-dilution method using Cardio-Green as the indicator. Peripheral haemodynamics in all 30 patients were studied in the forearm using strain gauge plethysmography. Measurements were made at rest before and repeatedly for 90 minutes after oral administration of one capsule of 25 mg or 50 mg carvedilol. Significant reductions in the systolic and diastolic blood pressures (p less than 0.05-0.001) were observed in all groups. Cardiac output showed a small, non-significant decrease from 5.81/min to 5.1 l/min. Total peripheral resistance did not change, whereas resistance in the forearm fell by 16% (p less than 0.05). These findings are different from what would have been expected acutely after administration of a pure beta-adrenoceptor blocking agent. They indicate that carvedilol possesses vasodilating activity in addition to its beta-adrenoceptor blocking effect.
卡维地洛(BM 14190)是一种新型化合物,具有非选择性β肾上腺素受体阻断活性,无内在拟交感活性,并具有毛细血管前血管舒张作用。采用侵入性技术对10例口服25 mg卡维地洛的患者进行了急性血流动力学效应研究,对另外10例口服25 mg和10例口服50 mg的患者进行了非侵入性研究。所有患者均患有原发性高血压。在侵入性研究中,测量动脉内血压,并使用心绿作为指示剂通过染料稀释法测定心输出量。使用应变片体积描记法对所有30例患者的前臂外周血流动力学进行了研究。在口服25 mg或50 mg卡维地洛胶囊前静息状态下进行测量,并在给药后90分钟内重复测量。所有组的收缩压和舒张压均显著降低(p<0.05-0.001)。心输出量从5.8升/分钟小幅下降至5.1升/分钟,但无显著差异。总外周阻力未改变,而前臂阻力下降了16%(p<0.05)。这些发现与给予纯β肾上腺素受体阻断剂后急性预期的结果不同。它们表明卡维地洛除了具有β肾上腺素受体阻断作用外,还具有血管舒张活性。