健康志愿者中吲哚洛尔和普萘洛尔的β-肾上腺素受体阻断活性及作用持续时间
beta-Adrenoceptor blocking activity and duration of action of pindolol and propranolol in healthy volunteers.
作者信息
Aellig W H
出版信息
Br J Clin Pharmacol. 1976 Apr;3(2):251-7. doi: 10.1111/j.1365-2125.1976.tb00600.x.
Abstract
The beta-adrenoceptor blocking activities of pindolol and propranolol have been investigated in healthy male volunteers. Pindolol was about forty times more potent than propranolol in reducing isoprenaline-induced tachycardia. Pindolol (5 mg) and propranolol (u99 mg) were approximately equiactive in reducing exercise-induced tachycardia, 2 h after oral administration. The duration of action of pindolol is significantly longer than that of propranolol; 24 h after pindolol (kmg), 36+/-5% of the masimum effect were still present, and after propranolol (100 mg) 16+/-4% remained. Despite the long duration of action of pindolol, there was no evidence for cumulation during oral administration of 5 mg t.d.s. for 5 days.
摘要
已在健康男性志愿者中研究了吲哚洛尔和普萘洛尔的β-肾上腺素受体阻断活性。在降低异丙肾上腺素引起的心动过速方面，吲哚洛尔的效力约为普萘洛尔的40倍。口服给药2小时后，吲哚洛尔（5毫克）和普萘洛尔（99毫克）在降低运动诱发的心动过速方面活性大致相当。吲哚洛尔的作用持续时间明显长于普萘洛尔；吲哚洛尔（5毫克）给药24小时后，仍存在36±5%的最大效应，而普萘洛尔（100毫克）给药后则为16±4%。尽管吲哚洛尔作用持续时间长，但在每天口服5毫克、每日3次、连续服用5天的过程中，未发现有蓄积现象。
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