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醋丁洛尔对心脏和肺部的影响。

Cardiac and pulmonary effects of acebutolol.

作者信息

Kumana C R, Kaye C M, Leighton M, Turner P, Hamer J

出版信息

Lancet. 1975 Jul 19;2(7925):89-93. doi: 10.1016/s0140-6736(75)90001-x.

Abstract

In a double-blind randomised study, single intravenous doses of propranolol (0-1 mg. per kg.), practolol (1 mg. per kg.), acebutolol (1 mg. per kg.), or placebo were each administered at weekly intervals to six healthy volunteers. Forced expiratory volume in 1 second (F.E.V.1), resting and exercise heart-rate, and resting and exercise peak flow-rate (P.F.R.) were determined before and at 2, 3, 4, and 6 hours after each treatment. Venous blood-samples were also obtained at these times. Compared with placebo, resting heart-rate was reduced after all three drugs, but the corresponding differences in exercise heart-rate were much greater, more consistent, and of greater statistical significance. At 2, 3, and 4 hours when acebutolol and propranolol produced equivalent cardiac beta-blocking activity (judged by reductions in exercise heart-rate), their mean plasma concentratios were in the ratio of about 8/1; and at 2 hours when practolol and acebutolol gave rise to almost equivalent cardiac beta blockade, their mean plasma concentratio ration was 3/1. At times, reductions in F.E.V.1 and resting P.F.R. after propranolol (but not after practolol or acebutolol) were significantly greater than the corresponding changes after placebo. The reductions in exercies P.F.R. after propranolol (6 hours) and acebutolol (4 hours) (but not after practolol) were significantly greater than the changes after placebo. Changes in F.E.V.1, resting and exercise P.F.R. after propranolol, and the corresponding changes after practolol, were significantly different, all of which confirmed that practolol was more cardioselective than propranolo. In general, the reductions in F.E.V.1 and resting P.F.R. after acebutolol were slightly smaller than after propranolol, excepting at 6 hours when the difference between them was significant. The reductions in exercise P;F.R. after acebutolol and propranolol were of the same order, there being no significant differences between the two, whereas the reductions after acebutolol were clearly greater than the corresponding changes after practolol, the differences being significant at 2, 3, and 4 hours.

摘要

在一项双盲随机研究中,每周给6名健康志愿者静脉注射一次单剂量的普萘洛尔(0 - 1毫克/千克)、普拉洛尔(1毫克/千克)、醋丁洛尔(1毫克/千克)或安慰剂。在每次治疗前以及治疗后2、3、4和6小时测定1秒用力呼气量(F.E.V.1)、静息和运动时的心率以及静息和运动时的峰值流速(P.F.R.)。在这些时间点还采集静脉血样。与安慰剂相比,所有三种药物治疗后静息心率均降低,但运动心率的相应差异更大、更一致且具有更大的统计学意义。在醋丁洛尔和普萘洛尔产生同等心脏β受体阻滞活性时(通过运动心率降低判断),2、3和4小时时它们的平均血浆浓度之比约为8/1;在普拉洛尔和醋丁洛尔产生几乎同等心脏β受体阻滞时,2小时时它们的平均血浆浓度之比为3/1。有时,普萘洛尔治疗后F.E.V.1和静息P.F.R.的降低(但普拉洛尔和醋丁洛尔治疗后未出现)显著大于安慰剂治疗后的相应变化。普萘洛尔(6小时)和醋丁洛尔(4小时)治疗后运动P.F.R.的降低(但普拉洛尔治疗后未出现)显著大于安慰剂治疗后的变化。普萘洛尔治疗后F.E.V.1、静息和运动P.F.R.的变化以及普拉洛尔治疗后的相应变化显著不同,所有这些均证实普拉洛尔比普萘洛尔更具心脏选择性。一般来说,醋丁洛尔治疗后F.E.V.1和静息P.F.R.的降低略小于普萘洛尔治疗后,但6小时时二者差异显著。醋丁洛尔和普萘洛尔治疗后运动P.F.R.的降低程度相当,二者之间无显著差异,而醋丁洛尔治疗后的降低明显大于普拉洛尔治疗后的相应变化,在2、3和4小时差异显著。

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