Comparative effects of verapamil and isradipine on steady‐state digoxin kinetics
Comparative effects of verapamil and isradipine on steady‐state digoxin kinetics
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维拉帕米和伊拉地平对稳态地高辛动力学的比较影响
DOI：
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发表时间：
1988
期刊：
影响因子：
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通讯作者：
Johanna Johnson
中科院分区：
文献类型：
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作者：
S. Rodin;B. Johnson;John Wilson;P. Ritchie;Johanna Johnson
比较了维拉帕米（240 mg/天）和一种新的二氢吡啶钙通道阻滞剂伊地拉平（15 mg/天）对地高辛稳态药代动力学的影响。19名年龄在23至40岁之间的健康白人男性，每12小时服用0.25 mg地高辛片，连续两周。每个受试者也在其中一个时期接受一种钙通道阻滞剂，药物和顺序随机化。分析盲RIA血清地高辛测定显示，接受isradipine， 5mg t.i.d的9名受试者地高辛峰值水平从2.3±0.6增加到2.9±0.7 ng/ml (p < 0.05)，但在12小时内稳态水平或AUC没有显著变化。相比之下，服用维拉帕米80 mg / d的10名受试者的稳态（0.9±0.1至1.3±0.2 ng/ml, p < 0.001）和峰值血清地高辛浓度（2.5±0.7至3.6±0.8ng/ml, p < 0.001）和AUC（15.7±1.7至23.6±2.9 ng·hr/ml, p < 0.001）显著增加。钙通道阻滞剂均不能降低肾地高辛清除率。维拉帕米增加地高辛水平而不影响肾脏清除率。以拉西平与地高辛没有重要的临床相互作用。
The effects on the steady‐state digoxin pharmacokinetics of verapamil (240 mg/day) and a new dihydropyridine calcium channel blocker, isradipine (15 mg/day), were compared. Nineteen healthy white men, aged 23 to 40 years, ingested 0.25 mg digoxin tablets every 12 hours for two consecutive periods of 2 weeks. Each subject also received one of the calcium channel blockers during one of these periods, with agent and sequence randomized. Analyst‐blind RIA serum digoxin determinations demonstrated that the nine subjects who received isradipine, 5 mg t.i.d., had a small increment in peak digoxin level from 2.3 ± 0.6 to 2.9 ± 0.7 ng/ml (p < 0.05) but no significant change in steady‐state level or AUC over 12 hours. By contrast, the 10 subjects who received verapamil, 80 mg t.i.d., showed significant increases in steady‐state (0.9 ± 0.1 to 1.3 ± 0.2 ng/ml; p < 0.001) and peak serum digoxin concentrations (2.5 ± 0.7 to 3.6 ± 0.8ng/ml; p < 0.001) and in AUC (15.7 ± 1.7 to 23.6 ± 2.9 ng · hr/ml; p < 0.001). Neither calcium channel blocker reduced renal digoxin clearance. Verapamil increases digoxin levels without affecting renal clearance. Isradipine has no clinically important interaction with digoxin.