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硝酸酯类刚于临床已有悠久的历史。早在1847年Sombero首先合成硝酸甘油(GTN),于1859年Guthrie用于心绞痛治疗,至今仍为治疗心绞痛的首选药物。其作用机理不很清楚。自1980年Furchgott发现乙酰胆碱、缓激肽等松弛血管作用是释放一种依赖于血管内皮的化学物质,称内皮衍生松弛因子(Endothelium Derived Relaxing Factor, EDRF)后,对这古老的药物增加了新的认识。下面以GTN为重点谈一些进展。一、药理作用 1.GTN能选择性扩张各种血管对静脉扩张较动脉为明显,而大动脉比小动脉扩张为著。由于血管平滑肌的扩张,使心脏前后负荷减轻,心肌耗氧量减少,以及使心肌缺血区的供氧量改善,发挥其抗心绞痛作
Nitrates have a long history in the clinic. As early as 1847 Sombero first synthesized nitroglycerin (GTN), in 1859 Guthrie for angina pectoris, is still the drug of choice for the treatment of angina. Its mechanism of action is not clear. Since 1980, Furchgott found that relaxing blood vessels such as acetylcholine and bradykinin release endothelium-dependent chemicals, called Endothelium Derived Relaxing Factor (EDRF), which adds a new understanding. Here to talk about some progress GTN focus. First, the pharmacological effects 1.GTN can selectively expand a variety of blood vessels on the venous expansion compared with the artery was obvious, while the larger arteries than the arterioles dilated. Due to the expansion of vascular smooth muscle, the heart before and after the load to reduce myocardial oxygen consumption decreased, and myocardial oxygen zone to improve the amount of oxygen, to play its anti-angina