输注速率对尼索地平在人体中的药代动力学及血流动力学效应的影响。
The influence of infusion rate on the pharmacokinetics and haemodynamic effects of nisoldipine in man.
作者信息
van Harten J, van Brummelen P, Zeegers R R, Danhof M, Breimer D D
机构信息
Center for Bio-Pharmaceutical Sciences, Division of Pharmacology, Leiden, The Netherlands.
出版信息
Br J Clin Pharmacol. 1988 Jun;25(6):709-17. doi: 10.1111/j.1365-2125.1988.tb05257.x.
Abstract
- The pharmacokinetics and haemodynamic effects of nisoldipine on long term i.v. infusion of 2.40 mg and 9.59 mg in 25 h were studied in six healthy subjects. Liver blood flow at 0.8 and 24 h was assessed by measuring indocyanine green (ICG) clearance. 2. After high-dose nisoldipine, systemic clearance was 0.99 +/- 0.16 1 min-1, volume of distribution was 5.8 +/- 1.5 1 kg-1 and elimination half-life was 10.7 +/- 2.4 h. The pharmacokinetic parameters were similar after low-dose nisoldipine. 3. No significant changes in apparent liver blood flow were observed after either high-dose or low-dose nisoldipine. 4. Systolic blood pressure did not change, whereas diastolic blood pressure decreased by approximately 10% during both treatments. Maximal increase in heart rate was approximately 37% at high-dose infusion, whereas this was one half lower during the low-dose regimen. 5. Increased infusion rate results in an unfavourable shift in the haemodynamic effect profile of nisoldipine.
摘要
- 在6名健康受试者中研究了尼索地平在25小时内静脉输注2.40毫克和9.59毫克时的药代动力学和血流动力学效应。通过测量吲哚菁绿（ICG）清除率评估0.8小时和24小时时的肝血流量。2. 高剂量尼索地平后，全身清除率为0.99±0.16升/分钟，分布容积为5.8±1.5升/千克，消除半衰期为10.7±2.4小时。低剂量尼索地平后的药代动力学参数相似。3. 高剂量或低剂量尼索地平后，表观肝血流量均未观察到显著变化。4. 收缩压未改变，而两种治疗期间舒张压均下降约10%。高剂量输注时心率最大增加约37%，而低剂量方案时则低一半。5. 输注速率增加会导致尼索地平血流动力学效应曲线出现不利变化。
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