氨力农的治疗学基础探讨

Therapeutic basis of amrinone

充血性心力衰竭（ＣＨＮ）患者６１例应用氨力农静脉滴注治疗。用药第４天ＮＹＨＡ心功能分级改善有效率９０％；第５天降至７７％；第１０天时仅５０％。运动峰耗氧量（ｐＶＯ＿２）的有效率第５天时为３０％，但有１０％出现恶化。治疗后血淋巴细胞β受体密度进一步下调；血浆去甲肾上腺素（ＮＥ）、肾上腺素（Ｅ）有升高倾向；淋巴细胞内ｃＡＭＰ含量增加。我们认为氨力农临床耐药性的产生可能与β受体密度下调有关；ｃＡＭＰ升高导致异源脱敏是可能机制。基于氨力农对ｐＶＯ＿２和β受体－ＡＣ－ｃＡＭＰ系统的不良作用，作者认为它不宜作为治疗心力衰竭的一线药物。

Abstract Sixty-one patients with severe congestive heart failure (CHF) were treated with amrinone,i.v.initial dose of 0. 75mg/kg in 20 min,followed by 6 hours infusion of 0. 75μg · kg-1/min each daily for 5-10 days.The effective rate of improvement in NYHA classification was 90 % at the fourth day,77 % at the fifth day, and only 5 % at the 10th day. The effective rate of VO_2max was 30 %,and 10% patients worsened. After 5days infusion of amrinone,the number of lymphocyte β-adrenoceptor decreased significantly; plasma catecholamine levels slightly increased,and intra-lympocyte cAMP content significantly increased. The clinical tolerance of amrinone may be related to the down regulation of β-adrenoceptor, and heterogeneous desensitization due to the increased intra-lymphocyte cAMP content is the possible mechanism. VO_2max correlated positively with β-adrenoceptor and inversely with plasma norepinephrine level, suggesting that VO_2max can reflect severity of the impaired myocardium to some extent.Based on the deleterious effect of amrinone on the BAR-AC- cAMP system and myocardium, we conclude that amrinone should not be used as the first line drug in the treatment of heart failure.