Magder S, Rubenson D, Griffin G, Kernoff R, Harrison D C
J Cardiovasc Pharmacol. 1983 Jul-Aug;5(4):691-6. doi: 10.1097/00005344-198307000-00026.
In six conscious dogs we compared the hemodynamic effects of propranolol, acebutolol, and acebutolol's primary metabolite at equipotent beta-blocking doses. Aortic pressure, heart rate, left ventricular end-diastolic pressure, dP/dt, and aortic flow velocity were measured 3 weeks after sterile surgery during three infusions of each drug. Only one drug was given on each day. The equipotent beta-blocking dose of each drug was obtained by comparing isoproterenol dose-response curves. All three drugs produced a fall in dP/dt. Left ventricular end-diastolic pressure increased in most dogs, but this was only significant for acebutolol. The heart rate tended to fall and the blood pressure rise, but this was variable and not significant. The concentration of the equipotent blocking dose of acebutolol was 44 times that of propranolol, and while the concentration of acebutolol's metabolite was 1.6 times that of acebutolol. In conclusion, at a concentration similar to acebutolol, acebutolol's metabolite has heart rate blocking and myocardial depressive effects similar to those of propranolol and acebutolol.
在6只清醒犬中，我们比较了普萘洛尔、醋丁洛尔及其主要代谢产物在等效β受体阻滞剂量下的血流动力学效应。在无菌手术3周后，每种药物进行三次输注期间，测量主动脉压、心率、左心室舒张末期压力、dp/dt以及主动脉流速。每天仅给予一种药物。通过比较异丙肾上腺素剂量反应曲线获得每种药物的等效β受体阻滞剂量。所有三种药物均使dp/dt下降。大多数犬的左心室舒张末期压力升高，但仅醋丁洛尔的这种升高具有统计学意义。心率有下降趋势，血压有升高趋势，但变化不定且无统计学意义。醋丁洛尔等效阻滞剂量的浓度是普萘洛尔的44倍，而醋丁洛尔代谢产物的浓度是醋丁洛尔的1.6倍。总之，在与醋丁洛尔相似的浓度下，醋丁洛尔的代谢产物具有与普萘洛尔和醋丁洛尔相似的心率阻滞和心肌抑制作用。
