单次给药后β-肾上腺素能受体拮抗剂对华法林药代动力学和药效学的影响。
The effect of beta-adrenoceptor antagonists on the pharmacokinetics and pharmacodynamics of warfarin after a single dose.
作者信息
Bax N D, Lennard M S, Tucker G T, Woods H F, Porter N R, Malia R G, Preston F E
出版信息
Br J Clin Pharmacol. 1984 May;17(5):553-7. doi: 10.1111/j.1365-2125.1984.tb02389.x.
Abstract
The effects of three beta-adrenoceptor antagonists (propranolol, metoprolol and atenolol) on the serum kinetics and pharmacodynamics of warfarin given in a single oral dose (15 mg) were studied in six normal subjects. At the same degree of beta-adrenoceptor blockade, as assessed by the decrease of exercise tachycardia, propranolol increased the area under the serum warfarin concentration time curve (AUC) by 16.3 +/- 14.2 s.d.% (P less than 0.01) and the maximum serum warfarin concentration by 23.0 +/- 14.3 s.d.% (P less than 0.001). Atenolol increased the maximum serum warfarin concentration by 12.5 +/- 12.3% s.d. (P less than 0.05) but was without effect on warfarin AUC. Metoprolol had no effect on warfarin kinetics. The extent of changes in the prothrombin time and the plasma clotting Factor VII activity caused by warfarin were not altered by any of the beta-adrenoceptor antagonists.
摘要
在6名正常受试者中研究了三种β-肾上腺素受体拮抗剂（普萘洛尔、美托洛尔和阿替洛尔）对单次口服15毫克华法林的血清动力学和药效学的影响。以运动性心动过速的降低来评估，在相同程度的β-肾上腺素受体阻滞下，普萘洛尔使血清华法林浓度-时间曲线下面积（AUC）增加了16.3±14.2标准差%（P<0.01），使血清华法林最大浓度增加了23.0±14.3标准差%（P<0.001）。阿替洛尔使血清华法林最大浓度增加了12.5±12.3%标准差（P<0.05），但对华法林AUC无影响。美托洛尔对华法林动力学无影响。华法林引起的凝血酶原时间和血浆凝血因子VII活性的变化程度未被任何一种β-肾上腺素受体拮抗剂改变。
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