Sponer G, Strein K, Bartsch W, Müller-Beckmann B
Department of Experimental Cardiovascular Research, Boehringer Mannheim GmbH, Germany.
J Cardiovasc Pharmacol. 1992;19 Suppl 1:S5-11. doi: 10.1097/00005344-199219001-00003.
Carvedilol is a dual-acting drug designed to produce two complementary effects: beta-blockade and vasodilation. These effects are induced in the same dose range, a prerequisite for utilizing both properties in an appropriate manner. The vasodilation is mediated predominantly by specific alpha 1-adrenoceptor blockade. At markedly higher concentrations, additional vasodilating actions besides alpha 1-blockade can be observed. These effects resemble those of Ca(2+)-antagonistic properties. However, they do not contribute to the acute blood pressure-lowering activity of carvedilol but may be responsible for the increased blood flow to specific organs. At beta-blocking doses, carvedilol reduces the regional and systemic vascular resistance in various experimental models, healthy volunteers, and in patients with cardiovascular diseases such as hypertension, coronary artery disease, and heart failure. The profile of carvedilol thus insures beneficial treatment of hemodynamic disorders characterized by increased sympathetic tone and increased vascular resistance.
卡维地洛是一种具有双重作用的药物,旨在产生两种互补效应:β受体阻滞和血管舒张。这些效应在相同剂量范围内诱导产生,这是以适当方式利用这两种特性的前提条件。血管舒张主要由特异性α1肾上腺素能受体阻滞介导。在明显更高的浓度下,除α1阻滞外还可观察到其他血管舒张作用。这些效应类似于钙拮抗特性。然而,它们对卡维地洛的急性降压活性没有贡献,但可能是特定器官血流增加的原因。在β受体阻滞剂量下,卡维地洛在各种实验模型、健康志愿者以及患有心血管疾病(如高血压、冠状动脉疾病和心力衰竭)的患者中降低局部和全身血管阻力。因此,卡维地洛的特性确保了对以交感神经张力增加和血管阻力增加为特征的血流动力学紊乱进行有益治疗。