Bassenge E, Strein K
Naunyn Schmiedebergs Arch Pharmacol. 1986 Sep;334(1):100-4. doi: 10.1007/BF00498746.
Isosorbide-5-mononitrate (IS-5-MN), the main metabolite of isosorbide dinitrate shows antianginal efficacy and is being used increasingly as a drug for practical therapy. In conscious dogs we therefore measured the effects of increasing doses of IS-5-MN on hemodynamic parameters and the diameter of the circumflex artery. We found a dose dependent reduction of the mean right atrial pressure, the systolic blood pressure and a dilatation of the circumflex artery. For all three parameters threshold dosages were between 0.01 and 0.03 mg/kg. On the contrary peripheral and coronary resistance did not change at doses less than or equal to 0.3 mg/kg. The heart rate was significantly increased only at doses above 1 mg/kg and the diastolic blood pressure also showed a tendency to fall only at doses above 1 mg/kg. Cardiac output and coronary flow were not significantly altered over the entire dose range investigated, with the exception of a transient rise in coronary blood flow after the injection of 2.5 mg/kg IS-5-MN. From our results we can deduce that in the low dose range reduction of preload and dilatation of large arteries are the main effects of IS-5-MN. In contrast, no reduction of the coronary or peripheral resistance is to be expected.
单硝酸异山梨酯(IS-5-MN)是硝酸异山梨酯的主要代谢产物,具有抗心绞痛疗效,且越来越多地被用作实际治疗药物。因此,我们在清醒犬中测量了递增剂量的IS-5-MN对血流动力学参数和左旋支动脉直径的影响。我们发现平均右心房压力、收缩压呈剂量依赖性降低,左旋支动脉扩张。对于所有这三个参数,阈剂量在0.01至0.03mg/kg之间。相反,当剂量小于或等于0.3mg/kg时,外周阻力和冠状动脉阻力没有变化。仅在剂量高于1mg/kg时心率显著增加,舒张压也仅在剂量高于1mg/kg时呈下降趋势。在所研究的整个剂量范围内,心输出量和冠状动脉血流量没有显著改变,但注射2.5mg/kg IS-5-MN后冠状动脉血流量有短暂增加。从我们的结果可以推断,在低剂量范围内,IS-5-MN的主要作用是降低前负荷和扩张大动脉。相比之下,预计冠状动脉或外周阻力不会降低。