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[具有连续和间断药物释放的经皮硝酸甘油系统。抗缺血和血流动力学急性及长期效应的比较]

[Transdermal nitroglycerin systems with continuous and discontinuous drug release. A comparison of the anti-ischemic and hemodynamic acute and long-term effects].

作者信息

Odenthal H J, Wiechmann H W, Josephs W, Lenga P

机构信息

Medizinische Klinik, Ruhr-Universität Bochum, Marienhospital Herne.

出版信息

Dtsch Med Wochenschr. 1991 Feb 15;116(7):241-7. doi: 10.1055/s-2008-1063605.

Abstract

The anti-ischaemic and haemodynamic effects of two transdermal nitroglycerin systems, each offering 15 mg of nitroglycerine, the first giving continuous release (group 1) and the other discontinuous release (group 2), were compared in 30 men (mean age 56.5 [33-70] years) with coronary heart disease confirmed by angiography. Resting and exercise haemodynamics together with the degree of exercise-induced ST segment depression were measured on the first day, before and two hours after application of the plaster. After one week's therapy these measurements were repeated 24 hours after the application of the plaster on the previous day and two hours after the last application. Two hours after the first application both groups showed significant reduction (P less than 0.01) in exercise-induced ST segment depression (group 1: -60%, group 2: -50%) and in mean pulmonary artery pressure during exercise (group 1: -10%; group 2: -7%). After one week's therapy the reduction in exercise-induced ST segment depression was still significant in group 1 (-60%; P less than 0.01), but in group 2 (-30%) it was no longer significant. After one week had passed there was no longer any significant reduction in mean pulmonary artery pressure in either group (group 1: -6%; group 2: 0%). The acute anti-ischaemic and haemodynamic efficacy of both transdermal nitroglycerin systems was hence comparable; however, the emergence of nitrate tolerance during long-term use was not prevented even by phased release of the drug.

摘要

对30名经血管造影确诊为冠心病的男性(平均年龄56.5[33 - 70]岁),比较了两种均含15毫克硝酸甘油的经皮硝酸甘油系统的抗缺血和血流动力学效应,第一种为持续释放型(第1组),另一种为间断释放型(第2组)。在第一天,即在贴敷膏药前和贴敷后两小时,测量静息和运动时的血流动力学以及运动诱发的ST段压低程度。经过一周治疗后,在前一天贴敷膏药24小时后和最后一次贴敷后两小时重复这些测量。首次贴敷后两小时,两组运动诱发的ST段压低(第1组:-60%,第2组:-50%)和运动期间的平均肺动脉压(第1组:-10%;第2组:-7%)均显著降低(P<0.01)。经过一周治疗后,第1组运动诱发的ST段压低仍显著降低(-60%;P<0.01),但第2组(-30%)不再显著。一周后,两组的平均肺动脉压均不再有显著降低(第1组:-6%;第2组:0%)。因此,两种经皮硝酸甘油系统的急性抗缺血和血流动力学疗效相当;然而,即使采用药物的阶段性释放,也无法防止长期使用期间硝酸酯耐受性的出现。

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