Andersson K E
Acta Med Scand Suppl. 1986;707:65-73.
In the search for new effective positive inotropic agents for the treatment of congestive heart failure (CHF), interest has focused mainly on two groups of agents namely adrenoceptor agonists and drugs inhibiting phosphodiesterase. Common for drugs belonging to both groups is that their positive inotropic effects seem to involve an increase in the intracellular concentration of cyclic AMP. Drugs acting by stimulation of beta 1- and/or beta 2-adrenoceptors (e.g. dopamine, dobutamine, prenalterol, pirbuterol, salbutamol, terbutaline, fenoterol) have initial beneficial effects, but seem to be ineffective for long-term treatment. This has been suggested to be due to desensitization of the beta-adrenoceptors, and means, if this effect can be definitely established, that beta-adrenoceptor stimulation should be restricted to the acute treatment of CHF. Among drugs inhibiting phosphodiesterase, sulmazole, amrinone, milrinone, and fenoximone all have been shown to improve cardiac performance in patients with CHF during short-term treatment. However, results of long-term treatment with most of these drugs seem less encouraging. It has been suggested that these drugs may not be an effective approach to treatment of patients with CHF, since even if it is possible to achieve short-term gains, the long-term effects on the myocardium may be detrimental. Their ultimate place in the treatment of CHF remains to be established.
在寻找用于治疗充血性心力衰竭(CHF)的新型有效正性肌力药物的过程中,人们的兴趣主要集中在两类药物上,即肾上腺素能受体激动剂和磷酸二酯酶抑制剂。这两类药物的共同之处在于,它们的正性肌力作用似乎都涉及细胞内环磷酸腺苷(cAMP)浓度的升高。通过刺激β1和/或β2肾上腺素能受体起作用的药物(如多巴胺、多巴酚丁胺、普瑞特罗、吡布特罗、沙丁胺醇、特布他林、非诺特罗)具有初始有益作用,但似乎对长期治疗无效。有人认为这是由于β肾上腺素能受体脱敏所致,如果这种效应能够得到确切证实,那就意味着β肾上腺素能受体刺激应仅限于CHF的急性治疗。在磷酸二酯酶抑制剂中,舒马唑、氨力农、米力农和非诺昔酮在短期治疗期间均已显示可改善CHF患者的心脏功能。然而,这些药物大多数的长期治疗结果似乎不太乐观。有人认为这些药物可能不是治疗CHF患者的有效方法,因为即使有可能实现短期获益,对心肌的长期影响可能是有害的。它们在CHF治疗中的最终地位仍有待确定。