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在用硝酸酯连续治疗的心绞痛、心力衰竭或隐性心肌缺血患者中,50～60%发生耐受性;增加剂量并不能使疗效恢复。事实上,剂量愈大,愈易产生耐受性,恢复疗效所需要的无药间隙期也就愈长。 N-乙酰半胱氨酸(N-Acetylcysteine)静滴本品可防治硝酸酯耐受性。理论依据是,有机硝酸酯在血管内代谢的终末产物氧化氮可松弛血管平滑肌,硝酸酯透入平滑肌细胞后,可直接转化为氧化氮,但在脱硝基作用的早期必须有巯基参与。巯基存在于谷胱甘肽部分;当发生耐受性时,巯基不足,以致不能
In patients with angina pectoris, heart failure, or recessive myocardial ischemia treated sequentially with nitrates, 50 to 60% of the patients develop tolerance; increasing the dose does not lead to a return of efficacy. In fact, the larger the dose, the more tolerable it is and the longer the drug-free gap needed to recover the effect. N-acetyl cysteine (N-Acetylcysteine) intravenous infusion of this product can prevent nitrate tolerance. The rationale is that nitric oxide, an end product of the metabolism of organic nitric oxide, can relax vascular smooth muscle. Nitrate permeates into smooth muscle cells and can be directly converted to nitric oxide. However, it must be involved in the early stage of denitration. Sulfhydryl groups are present in the glutathione moiety; when tolerance occurs, the sulfhydryl group is deficient so that no