Eggertsen R, Sivertsson R, Andrén L, Hansson L
J Hypertens. 1984 Oct;2(5):529-34. doi: 10.1097/00004872-198410000-00013.
Carvedilol (BM 14190) is a new antihypertensive compound which combines beta-adrenoceptor blocking and precapillary vasodilating properties but is devoid of intrinsic sympathomimetic activity. The acute and long-term effects on blood pressure and regional haemodynamics (forearm plethysmography) were studied with carvedilol 25 mg b.i.d. or 50 mg b.i.d. Comparisons were made with propranolol 80 mg b.i.d. in a randomized double-blind placebo controlled trial comprised of 30 patients with essential hypertension. After a four-week placebo period active therapy was given for four weeks. Carvedilol administered acutely reduced blood pressure at both doses, delta 13/6 mmHg (P less than 0.001/P less than 0.01) and 17/10 mmHg (P less than 0.001/P less than 0.01). Resistance in the forearm fell significantly with the higher dose. This was in contrast to propranolol which only reduced heart rate acutely, and as expected caused a rise in forearm resistance. After four weeks both compounds had reduced blood pressure significantly and to the same extent. Blood flow was still significantly reduced with propranolol in contrast to the findings with carvedilol. We conclude that carvedilol given orally has a useful antihypertensive effect both acutely and during prolonged treatment. It is well tolerated and its haemodynamic profile is attractive.
卡维地洛(BM 14190)是一种新型抗高血压化合物,它兼具β-肾上腺素能受体阻断和毛细血管前血管舒张特性,但无内在拟交感活性。采用每日两次、每次25毫克或每日两次、每次50毫克的卡维地洛,研究其对血压和局部血流动力学(前臂体积描记法)的急性和长期影响。在一项由30例原发性高血压患者组成的随机双盲安慰剂对照试验中,与每日两次、每次80毫克的普萘洛尔进行比较。经过四周的安慰剂期后,给予四周的积极治疗。急性给予卡维地洛两种剂量均能降低血压,分别降低13/6毫米汞柱(P<0.001/P<0.01)和17/10毫米汞柱(P<0.001/P<0.01)。较高剂量时前臂阻力显著下降。这与普萘洛尔相反,普萘洛尔仅能急性降低心率,且如预期的那样导致前臂阻力升高。四周后,两种化合物均能显著降低血压,且降低程度相同。与卡维地洛的结果相反,普萘洛尔仍能显著降低血流。我们得出结论,口服卡维地洛在急性和长期治疗中均具有有效的抗高血压作用。它耐受性良好,其血流动力学特征具有吸引力。