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钙拮抗剂是作用于血管平滑肌和心肌(工作心肌、特殊心肌)具有兴奋收缩的钙拮抗性作用,使兴奋性降低,血管扩张,心肌收缩减弱,抑制传导作用的药物。近来研究表明该药对平滑肌和心肌作用的机制,是抑制Ca~(++)向细胞内流入。目前应用的钙拮抗剂,多数对冠状血管有较高的选择性,用于抗心绞痛,但由于用量和种类不同,出现心肌收缩抑制和抗心律失常的作用,所以用于治疗各种循环系统疾病,已引起注目。作用机制:心肌的收缩弛缓,受细胞内Ca~(++)浓度制约。收缩时细胞内Ca~(++)浓度约为10~(-3)M,舒张时约为10~(-7)M,而细胞内Ca~(++)浓度是通过细胞膜Ca~(++)流入、流出以及细胞内的微细结构进行调节。
Calcium antagonists act on calcium vascular smooth muscle and myocardial (working heart, special heart muscle) with contractile calcium antagonistic effect, so that reduced excitability, vasodilatation, myocardial contraction decreased, inhibition of conduction of the drug. Recent studies show that the drug’s mechanism of action on smooth muscle and myocardium is to inhibit the Ca ~ (++) influx into cells. Currently used calcium antagonists, the majority of coronary vessels have a high selectivity for anti-angina pectoris, but due to the different types and types of myocardial contractility and anti-arrhythmic effect, so for the treatment of various circulatory diseases , Has attracted attention. Mechanism of action: Myocardial contraction and relaxation, by the intracellular Ca ~ (++) concentration constraints. The contractile Ca ~ (++) concentration was about 10 ~ (-3) M and the diastolic pressure was about 10 ~ (-7) M, while the intracellular Ca ~ (+ +) Inflow, outflow and intracellular micro-structure adjustment.