Thuillez C
Service de Pharmacologie Clinique, C.H.U. de Rouen.
Therapie. 1993 Nov-Dec;48 Spec No:671-6.
Calcium antagonists share common property of blocking calcium influx and decreasing intracellular calcium in cardiac and vascular smooth muscle cells. They however differ from each other by their pharmacological properties. All calcium antagonist induce coronary and systemic vascular relaxation, thus increasing myocardial oxygen supply and decreasing myocardial oxygen demand, respectively. Only subgroups of diltiazem and verapamil, however, can exert negative chronotropic and/or inotropic effect which contribute to a further decrease in myocardial oxygen demand. In this pharmacological context, long term clinical studies in large groups of patients show that vasospastic angina is the first choice therapeutic indication of calcium antagonists. Furthermore, stable angina is a good indication only for subgroups of diltiazem and verapamil, and unstable angina is a contra-indication for the actually known phenyldihydropyridines, thus confirming the heterogeneity of this class of drugs and probably the major role of myocardial tropism in their antiischemic properties.
钙拮抗剂具有共同特性，即阻断钙内流并减少心脏和血管平滑肌细胞内的钙。然而，它们在药理特性上彼此不同。所有钙拮抗剂均可引起冠状动脉和全身血管舒张，从而分别增加心肌氧供和降低心肌氧耗。然而，只有地尔硫䓬和维拉帕米亚组可发挥负性变时和/或变力作用，这有助于进一步降低心肌氧耗。在此药理背景下，针对大量患者的长期临床研究表明，血管痉挛性心绞痛是钙拮抗剂的首选治疗适应证。此外，稳定型心绞痛仅对地尔硫䓬和维拉帕米亚组是良好适应证，而不稳定型心绞痛是目前已知的苯基二氢吡啶类药物的禁忌证，从而证实了这类药物的异质性以及心肌靶向性在其抗缺血特性中可能起的主要作用。
