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氨氯地平和硝苯地平控释片在血压正常受试者中作用持续时间的比较评估。

A comparative assessment of the duration of action of amlodipine and nifedipine GITS in normotensive subjects.

作者信息

Ueda S, Meredith P A, Howie C A, Elliott H L

机构信息

University Department of Medicine and Therapeutics, Western Infirmary, Glasgow G11 6NT, Scotland.

出版信息

Br J Clin Pharmacol. 1993 Dec;36(6):561-6. doi: 10.1111/j.1365-2125.1993.tb00415.x.

Abstract

1 This study in normotensive subjects compared the duration and consistency of action of amlodipine (5 mg) and nifedipine GITS (60 mg) by assessment of the attenuation of pressor responses to noradrenaline and angiotensin II. 2 Both drugs significantly attenuated pressor responses to both vasoconstrictors at 6 and 24 h post-dose with rightward shifts of up to 2.3-fold in the dose-response curves. 3 There was significantly less pharmacokinetic variability with amlodipine: for example, intra-subject variability was 33% with amlodipine and 59% with nifedipine GITS. 4 There were no significant differences in the pressor dose ratios up to 48 h post-dose with amlodipine whereas there was a significant and progressive reduction in the pressor dose ratios with nifedipine. 5 These results suggest that both drugs are broadly comparable as once daily treatments but amlodipine displayed less intra- and inter-subject variability and provided a significantly more sustained effect with a reserve of pharmacological activity up to 48 h post-dose.

摘要
  1. 本研究在血压正常的受试者中,通过评估去甲肾上腺素和血管紧张素II升压反应的减弱情况,比较了氨氯地平(5毫克)和硝苯地平控释片(60毫克)作用的持续时间和一致性。2. 两种药物在给药后6小时和24小时均显著减弱了对两种血管收缩剂的升压反应,剂量反应曲线向右移动高达2.3倍。3. 氨氯地平的药代动力学变异性显著更小:例如,氨氯地平的受试者内变异性为33%,硝苯地平控释片为59%。4. 氨氯地平给药后48小时内升压剂量比无显著差异,而硝苯地平的升压剂量比则显著且逐渐降低。5. 这些结果表明,作为每日一次的治疗药物,两种药物大致相当,但氨氯地平在受试者内和受试者间的变异性更小,且在给药后48小时内具有显著更持久的效果和药理活性储备。

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The first pass metabolism of nifedipine in man.硝苯地平在人体中的首过代谢。
Br J Clin Pharmacol. 1984 Dec;18(6):951-4. doi: 10.1111/j.1365-2125.1984.tb02569.x.
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Analysis of the pressor dose response.升压剂量反应分析
Clin Pharmacol Ther. 1982 Oct;32(4):450-8. doi: 10.1038/clpt.1982.188.
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Nifedipine and alpha adrenoceptor antagonism.硝苯地平与α肾上腺素能受体拮抗作用
Clin Pharmacol Ther. 1984 Dec;36(6):745-9. doi: 10.1038/clpt.1984.252.
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Nifedipine gastrointestinal therapeutic system.
Am J Med. 1987 Dec 21;83(6B):3-9. doi: 10.1016/0002-9343(87)90629-2.
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The pressor dose-response in clinical cardiovascular pharmacology.临床心血管药理学中的升压剂量反应
Br J Clin Pharmacol. 1987 May;23(5):499-503. doi: 10.1111/j.1365-2125.1987.tb03084.x.

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