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[具有间断释放硝酸甘油功能的贴片的急性和亚慢性效应]

[Acute and subchronic effect of a patch with discontinuous nitroglycerin liberation].

作者信息

Schirnick C, Reifart N

机构信息

Rotes Kreuz Krankenhaus, Abt. Kardiologie, Frankfurt.

出版信息

Z Kardiol. 1989;78 Suppl 2:79-82; discussion 115-7.

PMID:2511698
Abstract

We investigated a new patch with 15 mg nitroglycerine and a drug release of 70% during the first 12 h of application, designed to prevent tolerance. In a double blind placebo controlled trial 12 patients with angiographically significant coronary artery disease, angina and reproducible ST-segment depression during exercise were studied. Stress-tests with a constant workload were performed before, 1 h, 4 h and 8 h after first day application as well as after 8-10 days of therapy. At the first day the sum of ST-segment depression (lead V 5) during each minute of exercise and the 5 minutes of recovery decreased by 55.5% (1 h, p less than 0.001), 47.4% (4 h, p less than 0.001) and 28.4% (8 h, n.s.). After subchronical application the relative values were 32% (1 h, p less than 0.05), 23.8% (4 h, n.s.) and no change after 8 h. Thus the new patch is effective between 1 h and 8 h of acute application. With chronic therapy however tolerance occurs despite the fact that only a small amount of nitroglycerine is released during the last half of a 24 h application.

摘要

我们研究了一种新的贴剂,其含有15毫克硝酸甘油,在应用的前12小时药物释放率为70%,旨在预防耐受性。在一项双盲安慰剂对照试验中,研究了12例患有血管造影显示有明显冠状动脉疾病、心绞痛且运动时可再现ST段压低的患者。在首次应用后1小时、4小时和8小时以及治疗8 - 10天后,进行了恒定工作量的应激试验。第一天,运动期间每分钟以及恢复的5分钟内ST段压低(V5导联)的总和在1小时时下降了55.5%(p<0.001),4小时时下降了47.4%(p<0.001),8小时时下降了28.4%(无统计学意义)。亚慢性应用后,相对值分别为32%(1小时,p<0.05),23.8%(4小时,无统计学意义),8小时后无变化。因此,这种新贴剂在急性应用的1小时至8小时之间有效。然而,在慢性治疗中,尽管在24小时应用的后半段仅释放少量硝酸甘油,但仍会出现耐受性。

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