Jansen W, Prenzel R, Kümper H, Weidmann B, Tauchert M
Medizinische Klinik I/Kardiologie, Städtisches Krankenhaus Leverkusen.
Z Kardiol. 1989;78 Suppl 2:72-8; discussion 115-7.
Fluctuating mononitrate plasma levels in the course of 24 h are a prerequisite for prevention of nitrate tolerance in patients with angina pectoris undergoing longterm treatment. In 12 patients with angiographically proven coronary artery disease (54 +/- 7 years) effects of 50 mg Isosorbide-5-mononitrate (IS-5-MN) in a slow-release (SR) formulation on hemodynamics and exercise tolerance were evaluated after a first dose and at the end of a 1-week treatment period with 50 mg given once-daily. 1 and 2 h after medication mean pulmonary artery pressure (PAP) at rest was reduced by 30% (p less than 0.001) and 25% (p less than 0.01 respectively. During submaximal bicycle exercise (50 W, 3 min) PAP was significantly reduced by IS-5-MN by 35% (1 and 2 h after medication). At the end of exercise (discontinuation), drug-induced reductions of PAP were 19% (1 h) and 21% (2 h) (p less than 0.05), respectively. IS-5-MN led to a marked increase of exercise capacity (base-line: 396 +/- 119 W x min); 1 h: 646 +/- 153 W x min (p less than 0.01). At stress testing 2, 4 and 10 h post medication improvements were 67% (p less than 0.01), 49% (p less than 0.01) and 28% (p less than 0.01), respectively. 24 h after medication baseline values were reached again. After a 1-week treatment with 50 mg IS-5-MN SR daily, beneficial effects of the drug on hemodynamics and working capacity could be demonstrated. Again, significant effects could be shown up to 10 h after drug administration. Thus, IS-5-MN SR administered once daily proved effective in intermediate-term treatment of patients with coronary artery disease with regard to hemodynamics and exercise capacity.(ABSTRACT TRUNCATED AT 250 WORDS)
对于接受长期治疗的心绞痛患者,24小时内单硝酸酯血浆水平波动是预防硝酸酯耐受性的前提条件。在12例经血管造影证实患有冠状动脉疾病的患者(年龄54±7岁)中,评估了50毫克缓释(SR)制剂的单硝酸异山梨酯(IS-5-MN)首剂给药后以及每日一次给予50毫克、为期1周的治疗期结束时对血流动力学和运动耐量的影响。用药后1小时和2小时,静息时平均肺动脉压(PAP)分别降低30%(p<0.001)和25%(p<0.01)。在次极量自行车运动(50瓦,3分钟)期间,IS-5-MN使PAP显著降低35%(用药后1小时和2小时)。运动结束时(停止运动),药物引起的PAP降低分别为19%(1小时)和21%(2小时)(p<0.05)。IS-5-MN使运动能力显著提高(基线:396±119瓦·分钟);1小时:646±153瓦·分钟(p<0.01)。在用药后2小时、4小时和10小时的应激测试中,改善分别为67%(p<0.01)、49%(p<0.01)和28%(p<0.01)。用药后24小时再次达到基线值。每日服用50毫克IS-5-MN SR进行1周治疗后,可证明该药物对血流动力学和工作能力有有益影响。同样,在给药后长达10小时仍可显示出显著效果。因此,每日一次给予IS-5-MN SR在冠状动脉疾病患者的中期治疗中,在血流动力学和运动能力方面被证明是有效的。(摘要截取自250字)