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静脉输注异丙肾上腺素对人体生理性手指震颤的增强作用:评估其在β-肾上腺素能受体拮抗剂评估中的作用。

Enhancement of physiological finger tremor by intravenous isoprenaline infusions in man: evaluation of its role in the assessment of beta-adrenoceptor antagonists.

作者信息

Arnold J M, McDevitt D G

出版信息

Br J Clin Pharmacol. 1984 Aug;18(2):145-52. doi: 10.1111/j.1365-2125.1984.tb02446.x.

Abstract

Graded intravenous isoprenaline infusions produce dose-related increases in finger tremor. The dose-response curves constructed with intra-arterial or intravenous isoprenaline behave similarly in the presence of both atenolol 50 mg and propranolol 40 mg. In Five subjects, practolol 120 mg, atenolol 50 mg, propranolol 40 mg and sotalol 200 mg reduced exercise heart rate by 20.2 +/- 2.3, 21.4 +/- 1.8, 17.4 +/- 2.5, 23.9 +/- 3.6% respectively: the differences were not significant. The corresponding dose-ratios for reduction of an isoprenaline tachycardia were 2.8, 2.3, 19.1 and 16.9 respectively. At doses which had comparable effects on an exercise tachycardia, the non-selective beta-adrenoceptor antagonists, propranolol 40 mg and sotalol 200 mg, attenuated the finger response to isoprenaline (dose ratios 33.3 and greater than 25.0 respectively) more than the beta 1-selective adrenoceptor antagonists, practolol 120 mg and atenolol 50 mg (dose ratios 1.0 and 2.3 respectively). In two out of five subjects, dose-response curves could not be constructed with sotalol, either at a dose of 200 or 100 mg. The enhancement of physiological finger tremor by intravenous infusions of isoprenaline may be useful in the investigation of beta 2-adrenoceptors and their antagonists in man.

摘要

静脉注射不同剂量的异丙肾上腺素会导致手指震颤呈剂量依赖性增加。在同时使用50毫克阿替洛尔和40毫克普萘洛尔的情况下,用动脉内或静脉内注射异丙肾上腺素构建的剂量反应曲线表现相似。在5名受试者中,120毫克醋丁洛尔、50毫克阿替洛尔、40毫克普萘洛尔和200毫克索他洛尔分别使运动心率降低了20.2±2.3%、21.4±1.8%、17.4±2.5%、23.9±3.6%:差异不显著。降低异丙肾上腺素引起的心动过速的相应剂量比分别为2.8、2.3、19.1和16.9。在对运动性心动过速有类似作用的剂量下,非选择性β肾上腺素能受体拮抗剂40毫克普萘洛尔和200毫克索他洛尔对异丙肾上腺素引起的手指反应的减弱作用(剂量比分别为33.3和大于25.0)比β1选择性肾上腺素能受体拮抗剂120毫克醋丁洛尔和50毫克阿替洛尔(剂量比分别为1.0和2.3)更强。在5名受试者中的2名中,无论是200毫克还是100毫克剂量的索他洛尔,都无法构建剂量反应曲线。静脉输注异丙肾上腺素增强生理性手指震颤可能有助于研究人体中的β2肾上腺素能受体及其拮抗剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27ef/1463531/ef78ea16c815/brjclinpharm00157-0029-a.jpg

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