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外周多巴胺受体激动剂口服非诺多泮(SKF 82526-J)对正常男性血压及肾功能的影响。

The effect of oral fenoldopam (SKF 82526-J), a peripheral dopamine receptor agonist, on blood pressure and renal function in normal man.

作者信息

Harvey J N, Worth D P, Brown J, Lee M R

出版信息

Br J Clin Pharmacol. 1985 Jan;19(1):21-7. doi: 10.1111/j.1365-2125.1985.tb02608.x.

Abstract

The effect of a single oral dose of 100 mg of fenoldopam on renal function and blood pressure was investigated in seven healthy male subjects in a double-blind placebo controlled study. Mean diastolic blood pressure fell by 10 mm Hg, 45 min after oral dosing and then gradually returned to baseline values. There was an increase in pulse rate and a delayed rise in systolic blood pressure. Measured from 30 to 120 min after drug ingestion, mean effective renal plasma flow increased to 158% of the value observed after placebo; mean glomerular filtration rate rose to 109% of the placebo value. Measured from 120 to 210 min after administration of the drug, effective renal plasma flow and glomerular filtration rate had returned to baseline values. Fenoldopam produced a small increase in the mean sodium excretion rate which was not significantly different from the fall after placebo. No change was detected in urine flow or potassium excretion rate. Mean plasma renin activity increased three-fold 1 h after oral dosing. Plasma aldosterone did not show a parallel increase although the plasma concentration at 1 h was significantly higher than after placebo. The results show a pronounced renal vasodilator effect lasting about 2 h. The findings are consistent with marked DA1 receptor agonist activity.

摘要

在一项双盲安慰剂对照研究中,对7名健康男性受试者研究了单次口服100毫克非诺多泮对肾功能和血压的影响。口服给药45分钟后,平均舒张压下降了10毫米汞柱,然后逐渐恢复到基线值。脉搏率增加,收缩压延迟上升。在药物摄入后30至120分钟测量,平均有效肾血浆流量增加到安慰剂后观察值的158%;平均肾小球滤过率上升到安慰剂值的109%。在给药后120至210分钟测量,有效肾血浆流量和肾小球滤过率已恢复到基线值。非诺多泮使平均钠排泄率略有增加,与安慰剂后的下降无显著差异。未检测到尿流量或钾排泄率的变化。口服给药1小时后,平均血浆肾素活性增加了三倍。血浆醛固酮虽在1小时时的血浆浓度显著高于安慰剂后,但未呈现平行增加。结果显示出持续约2小时的明显肾血管舒张作用。这些发现与显著的DA1受体激动剂活性一致。

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