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口服单硝酸异山梨酯:药代动力学与临床疗效

Oral isosorbide-5-mononitrate: pharmacokinetics and clinical efficacy.

作者信息

Kanto J H

出版信息

Int J Clin Pharmacol Ther Toxicol. 1987 Mar;25(3):129-35.

PMID:3557738
Abstract

Isosorbide-5-mononitrate is a longer acting active metabolite than the parent drug, isosorbide dinitrate (ISDN), with a half-life of around 4 hours. In coronary heart disease, myocardial infarction and in heart failure it causes a typical nitrate action on the central hemodynamics, but due to a complete systemic availability with high and predictable systemic drug levels, a drug action with a lower interindividual variability than with ISDN is to be expected. There is a close correlation between serum level and effect. The antianginal exercise tolerance increasing and unwanted effects as well as the development of tolerance to the drug action are comparable with those of ISDN. This naturally long-acting metabolite in ISDN works usually with a standard dosage of 20 mg twice daily.

摘要

5-单硝酸异山梨酯是一种比母体药物硝酸异山梨酯(ISDN)作用时间更长的活性代谢产物,半衰期约为4小时。在冠心病、心肌梗死和心力衰竭中,它对中心血流动力学产生典型的硝酸盐作用,但由于具有完全的全身可用性以及高且可预测的全身药物水平,预期其药物作用的个体间变异性低于ISDN。血清水平与效应之间存在密切相关性。其增加抗心绞痛运动耐量、不良反应以及药物作用耐受性的发展与ISDN相当。ISDN中的这种天然长效代谢产物通常以每日两次、每次20毫克的标准剂量起作用。

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Oral isosorbide-5-mononitrate: pharmacokinetics and clinical efficacy.口服单硝酸异山梨酯:药代动力学与临床疗效
Int J Clin Pharmacol Ther Toxicol. 1987 Mar;25(3):129-35.
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Antianginal and anti-ischemic efficacy of nicorandil in comparison with isosorbide-5-mononitrate and isosorbide dinitrate: results from two multicenter, double-blind, randomized studies with stable coronary heart disease patients.
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[Long-term tolerance and effect of isosorbide-5-mononitrate in comparison to isosorbide dinitrate (ISDN retard) in patients with coronary disease].[冠心病患者中5-单硝酸异山梨酯与二硝酸异山梨酯(缓释片)相比的长期耐受性及疗效]
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