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硝酸异山梨酯治疗心绞痛的剂量效应关系(作者译)

[Dose-effect relationship of isosorbide dinitrate in the treatment of angina pectoris (author's transl)].

作者信息

Schneider W, Stahl B, Kaltenbach M, Bussmann W D

出版信息

Dtsch Med Wochenschr. 1982 May 21;107(20):771-6. doi: 10.1055/s-2008-1070018.

Abstract

Fifteen males with angiographic evidence of coronary heart disease and stable, exercise-induced angina pectoris were given placebo or isosorbide dinitrate (ISDN) in a dialy dose of 30 mg, 120 mg, 240 mg and 480 mg in a randomized single-blind trial. The daily doses were given as a single oral dose of 5 mg, 20 mg, 40 mg and 80 mg tablets. Each dose and placebo was given for seven days. On the seventh day an exercise ECG of standardized level and duration of exercise was recorded. The ischaemia response in the ECG revealed a dose-dependent reduction by 28% (5 mg ISDN), 43% (20 mg), 60% (40 mg) and 73% (80 mg). The number of anginal attacks similarly fell parallel to dose. Plasma level of ISDN and the mononitrates, measured one and four hours after drug intake, rose almost linearly in relation to dose. Oral ISDN thus has a dose-dependent effect on the frequency of angina and ischaemia parameters during ergometric exercise. The protracted anti-anginal effect of ISDN is largely due to its metabolites. At high doses there is presumably an added effect of the high blood level of the basic substance.U

摘要

在一项随机单盲试验中,15名经血管造影证实患有冠心病且有稳定的运动诱发型心绞痛的男性,被给予安慰剂或每日剂量为30毫克、120毫克、240毫克和480毫克的硝酸异山梨酯(ISDN)。每日剂量以单次口服5毫克、20毫克、40毫克和80毫克片剂的形式给予。每种剂量和安慰剂均服用7天。在第7天记录标准化运动水平和持续时间的运动心电图。心电图中的缺血反应显示出剂量依赖性降低,分别为28%(5毫克ISDN)、43%(20毫克)、60%(40毫克)和73%(80毫克)。心绞痛发作次数同样与剂量呈平行下降。在服药后1小时和4小时测量的ISDN及其单硝酸盐的血浆水平与剂量几乎呈线性上升。因此,口服ISDN对运动试验期间心绞痛频率和缺血参数具有剂量依赖性作用。ISDN的长效抗心绞痛作用很大程度上归因于其代谢产物。在高剂量时,基本物质的高血药水平可能会产生额外作用。

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