Kmieć M, Ochmański W
I Katedry i Kliniki Chorób Wewnetrznych Collegium Medicum, Unwiersytetu Jagiellońskiego w Krakowie.
Przegl Lek. 1998;55(10):532-6.
Molsidomine, coronary drug which acts similar to organic nitrates, belongs to the drug class of sydnones . SIN-1A metabolite of Molsidomine has pharmacologically active group of NO, which by increasing levels of cGMP, decreases levels of intracellular calcium ions in smooth muscle cells. This effect leads to relaxation of smooth muscle vasculature, inhibits platelets aggregation and has indirect antiproliferative effect. In clinical observations no effect of tolerance to the drug was observed. Experimental data show additional mechanism of action of the drug: SIN-1C metabolites protects the reoxygenated cardiomyocyte from post-reperfusion damage. Indications for use of Molsidomine are: ischaemic heart disease, chronic heart failure and pulmonary hypertension. Effects of Molsidomine use in acute myocardial infarction and unstable angina were compared in clinical trials to effects of nitroglycerin use. Both drugs were found equally potent, but authors underline the fact of better Molsidomine tolerability comparing NTG, but longer serum half-time of Molsidomin effects that control of the treatment is worse. In clinical trials it was suggested that intravenous use of Molsidomine metabolite SIN-1 during PTCA procedures is more effective than use of isosorbide dinitrate in the same procedures. In other clinical trials molsidomin was found to produce beneficial effects in patients with heart failure due to ischaemic cardiomyopathy, dilatative cardiomyopathy, in essential hypertension, pulmonary artery hypertension in COPD patients and in congestive heart failure.
莫索尼定是一种作用类似于有机硝酸盐的冠状血管药物，属于 sydnones 类药物。莫索尼定的 SIN-1A 代谢产物具有 NO 药理活性基团，通过增加 cGMP 水平，降低平滑肌细胞内钙离子水平。这种作用导致平滑肌血管舒张，抑制血小板聚集，并具有间接抗增殖作用。在临床观察中未观察到对该药物的耐受性影响。实验数据显示了该药物的额外作用机制：SIN-1C 代谢产物可保护再灌注心肌细胞免受再灌注后损伤。莫索尼定的适应证为：缺血性心脏病、慢性心力衰竭和肺动脉高压。在临床试验中比较了莫索尼定用于急性心肌梗死和不稳定型心绞痛的效果与硝酸甘油使用的效果。发现两种药物同样有效，但作者强调与硝酸甘油相比，莫索尼定耐受性更好，但莫索尼定作用的血清半衰期更长，这使得治疗控制更差。在临床试验中表明，在经皮冠状动脉腔内血管成形术（PTCA）过程中静脉使用莫索尼定代谢产物 SIN-1 比在相同过程中使用硝酸异山梨酯更有效。在其他临床试验中，发现莫索尼定对缺血性心肌病、扩张型心肌病所致心力衰竭患者、原发性高血压患者、慢性阻塞性肺疾病（COPD）患者的肺动脉高压以及充血性心力衰竭患者产生有益作用。
