Plasma concentration‐response relationships for some cardiovascular effects of dihydropyridines in healthy subjects
Plasma concentration‐response relationships for some cardiovascular effects of dihydropyridines in healthy subjects
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二氢吡啶对健康受试者的一些心血管影响的血浆浓度-反应关系
DOI：
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发表时间：
1988
期刊：
影响因子：
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通讯作者：
H. Schmitz
中科院分区：
文献类型：
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作者：
K. Graefe;R. Ziegler;W. Wingender;K‐D Rämsch;H. Schmitz
在健康受试者中研究了三种二氢吡啶 (DHP) 钙通道阻滞剂的药代动力学和一些血流动力学效应。以随机顺序，每位受试者静脉注射 24 μg/kg 硝苯地平、40 μg/kg 尼群地平或 10 μg/kg 尼索地平。三种 DHP 的总清除率和分布容积不同（硝苯地平 < 尼索地平 < 尼群地平），但消除半衰期值相似。所有三种药物都会引起心率和前臂血流量（FBF）增加以及血压小幅下降。虽然三种药物观察到的心率峰值变化实际上是相同的（比基线高出约 45%），但尼群地平和尼索地平（比基线高出 200%）的 FBF 峰值变化比硝苯地平（比基线高出 79%）的反应更明显。心率和 FBF 对 DHP 的反应与血浆中的药物浓度直接相关。血浆水平响应曲线服从希尔方程。他们表明，DHP 的主要区别在于其扩张前臂阻力血管的功效（硝苯地平 < 尼群地平 < 尼索地平）。
The pharmacokinetics and some hemodynamic effects of three dihydropyridine (DHP) calcium channel blockers were studied in healthy subjects. In a randomized order, each subject was given 24 μg/kg nifedipine, 40 μg/kg nitrendipine, or 10 μg/kg nisoldipine intravenously. The three DHPs differed as to their total clearance and volume of distribution (nifedipine < nisoldipine < nitrendipine) but showed similar values for elimination half‐lives. All three drugs evoked increases in heart rate and forearm blood flow (FBF) and small decreases in blood pressure. Whereas the observed peak changes in heart rate were virtually identical for the three drugs (about 45% above baseline), the peak changes in FBF were more pronounced in response to nitrendipine and nisoldipine (>200% above baseline) than in response to nifedipine (79% above baseline). The heart rate and FBF responses to the DHPs were related directly to the drug concentrations in plasma. The plasma level‐response curves obeyed Hill's equation. They showed that the DHPs differ mainly in their potencies at dilating the forearm resistance vessels (nifedipine < nitrendipine < nisoldipine).
Ca 通道拮抗剂 [3H]尼群地平与豚鼠回肠平滑肌结合的表征。
DOI：
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发表时间：
1983
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
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作者：
Bolger,GT;Gengo,P;Klockowski,R;Luchowski,E;Siegel,H;Janis,RA;Triggle,AM;Triggle,DJ
通讯作者：
Triggle,DJ