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近10年来,心血管疾病的药物治疗取得较大的进展,其中以钙拮抗剂,即钙通道阻滞剂(或慢通道抑制剂)如异搏停、硝苯吡啶,地尔硫(艹卓)以及新近提出的 Bepridil 的研究与应用最具代表性。为此,本文就其药理学进行介绍。作用机制钙拮抗剂的基本作用机制系抑制离子的跨膜内流,尤其是抑制钙在动作电位期间经过慢通道的内流。这种抑制机能与细胞内外的电压差和药物的剂量存在一定的依赖关系。唯在疾病组织,钙进入细胞可不必通过慢通道;其次,有作用于细胞内某些部位的可能性,目前正在研究。各种钙拮抗剂的作用具有选择性,这是由于:(1)不同的活化机
Over the past 10 years, cardiovascular disease drug treatment made great progress, which calcium antagonists, namely calcium channel blockers (or slow channel inhibitors) such as verapamil, nifedipine, diltiazem ) And the newly proposed Bepridil research and application of the most representative. To this end, this article describes its pharmacology. Mechanism of Action The basic mechanism of action of calcium antagonists is to inhibit the transmembrane influx of ions and in particular to inhibit the influx of calcium through the slow channels during the action potential. This inhibitory function with the voltage difference between the inside and outside the cell and the dose of the drug there is a certain degree of dependence. Only in diseased tissues, calcium does not have to pass through the slow pathway into the cell; second, the possibility of acting on some parts of the cell is currently under investigation. The role of various calcium antagonists is selective, due to: (1) different activators