Pouleur H, Raigoso J, Rousseau M F
Department of Physiology, University of Louvain, Medical School, Brussels, Belgium.
Eur Heart J. 1991 Aug;12 Suppl C:29-34. doi: 10.1093/eurheartj/12.suppl_c.29.
The importance of the dopaminergic system in heart failure is unknown and the therapeutic potential of orally active compounds stimulating dopaminergic receptors has yet to be established. Despite similar acute haemodynamic changes in heart failure and despite a comparable profile of receptor stimulation, oral levodopa (the prodrug of dopamine) and oral ibopamine (the prodrug of epinine) produce opposite effects on plasma norepinephrine and have different pharmacokinetics. Placebo-controlled studies indicate a beneficial effect of ibopamine on exercise tolerance in patients with heart failure, whereas invasive evaluation of left ventricular function indicate that at the doses used in these trials, ibopamine does not act as a positive inotropic drug but rather as a vasodilator. This suggests that DA1 and DA2 receptor stimulation may be beneficial in heart failure. Further studies are, however, needed to specify the exact role of this therapeutic approach in comparison with other agents, such as ACE inhibitors, also able to modulate neuro-humoral activation in heart failure.
多巴胺能系统在心力衰竭中的重要性尚不清楚,口服活性化合物刺激多巴胺能受体的治疗潜力也有待确定。尽管心力衰竭时存在相似的急性血流动力学变化,且受体刺激情况相当,但口服左旋多巴(多巴胺的前体药物)和口服异波帕胺(依匹宁的前体药物)对血浆去甲肾上腺素产生相反的作用,且具有不同的药代动力学。安慰剂对照研究表明,异波帕胺对心力衰竭患者的运动耐量有有益作用,而对左心室功能的有创评估表明,在这些试验中所用剂量下,异波帕胺并非作为正性肌力药物起作用,而是作为血管扩张剂。这表明刺激DA1和DA2受体可能对心力衰竭有益。然而,与其他也能够调节心力衰竭时神经体液激活的药物(如血管紧张素转换酶抑制剂)相比,还需要进一步研究以明确这种治疗方法的确切作用。