Stephan K, Meesmann W, Bischoff K O, Hübner H, Geigenmüller L, Diesch J
Arzneimittelforschung. 1975 Nov;25(11):1770-6.
In animals without myocardial infarction the new beta-sympathicolytic agent atenolol (4-[2'-hydroxy-3'-iso-propylaminopropoxy]-phenyl acetamide, ICI 66 082) dose-dependently decreased heart rate, systolic aortic pressure and cardiac output. Coronary mean flow, coronary resistance, stroke volume, left ventricular enddiastolic pressure and total peripheral vascular resistance did not change significantly. Atenolol significantly reduced myocardial contractility, expressed by (dp/dtmax), Vpm, t-(dp/dtmax) and pre-ejection period. Furthermore, the comparative studies in animals with myocardial infarction and concomitant reduced cardial efficiency revealed, that atenolol has neither a positive intrinsic activity as has practolol nor a negative intrinsic activity as has propranolol. The dose-contractility relation of atenolol resembles that of practolol: in low dosages a strong decrease is achieved, in higher dosages no further reduction of the contractility parameters is observed. Because of the strong negative inotropic and blood pressure lowering effect it is suggested to use atenolol only with great caution in patients with reduced cardiac efficiency.
在没有心肌梗死的动物中,新型β-交感神经阻滞剂阿替洛尔(4-[2'-羟基-3'-异丙氨基丙氧基]-苯乙酰胺,ICI 66 082)剂量依赖性地降低心率、主动脉收缩压和心输出量。冠状动脉平均血流量、冠状动脉阻力、每搏量、左心室舒张末期压力和总外周血管阻力无显著变化。阿替洛尔显著降低心肌收缩力,表现为(dp/dtmax)、Vpm、t-(dp/dtmax)和射血前期。此外,在伴有心肌梗死且心脏效率降低的动物中的比较研究表明,阿替洛尔既不像心得宁那样具有正性内在活性,也不像普萘洛尔那样具有负性内在活性。阿替洛尔的剂量-收缩力关系与心得宁相似:在低剂量时收缩力大幅下降,在高剂量时未观察到收缩力参数进一步降低。由于其强大的负性肌力和降压作用,建议在心脏效率降低的患者中极其谨慎地使用阿替洛尔。