Théroux P, Taeymans Y, Waters D D
Drugs. 1983 Feb;25(2):178-95. doi: 10.2165/00003495-198325020-00005.
Angina pectoris results from an imbalance between the oxygen supply and the oxygen needs of the myocardium. While the classic form of angina is usually caused by demands exceeding supply, a primary and transient decrease in coronary blood flow is more and more often recognised as an aetiological factor of myocardial ischaemia. Calcium antagonists, although new in cardiovascular therapeutics, are already recognised as the treatment of choice for some forms of angina and as useful therapeutic adjuncts in others. Few contraindications to their use exist. They are potent vasodilators and they can prevent the occurrence of coronary artery spasm responsible for the Prinzmetal's variant form of angina. They can also reduce coronary artery tone, which if high, can compromise flow through a narrowed coronary artery. Nifedipine, diltiazem and verapamil can also influence the various determinants of myocardial oxygen consumption to reduce myocardial oxygen needs. Their effects on heart rate, blood pressure and on the inotropic state of the left ventricle is, in vivo, the balance between their direct effects on the vascular wall and myocardial muscular cells and their indirect effects represented by the reflex physiological responses. Significant variations in these effects exist between the 3 calcium antagonists such that treatment can be individualised to a particular patient's needs. Precautions with their use as well as most of their side effects can be understood from a knowledge of their direct and indirect properties. Other pharmacological effects of these drugs include a regional redistribution of coronary blood flow, cardioprotection, delay in cell death and possibly in the progression of atherosclerosis. The clinical significance of these properties remains to be investigated.
心绞痛是由心肌氧供与氧需之间的失衡所致。虽然典型形式的心绞痛通常是由需求超过供应引起的,但冠状动脉血流的原发性短暂减少越来越多地被认为是心肌缺血的一个病因。钙拮抗剂虽然在心血管治疗领域是新药,但已被公认为某些形式心绞痛的首选治疗药物,在其他情况下也是有用的治疗辅助药物。其使用的禁忌证很少。它们是强效血管扩张剂,可预防导致变异型心绞痛(普林兹金属心绞痛)的冠状动脉痉挛的发生。它们还可降低冠状动脉张力,过高的冠状动脉张力会妨碍血液流经狭窄的冠状动脉。硝苯地平、地尔硫䓬和维拉帕米还可影响心肌氧消耗的各种决定因素,以减少心肌氧需求。它们对心率、血压和左心室收缩状态的影响,在体内是其对血管壁和心肌细胞的直接作用与反射性生理反应所代表的间接作用之间的平衡。这三种钙拮抗剂在这些作用方面存在显著差异,因此治疗可根据特定患者的需求进行个体化。了解它们的直接和间接特性,就可以理解其使用时的注意事项以及大多数副作用。这些药物的其他药理作用包括冠状动脉血流的区域重新分布、心脏保护、延迟细胞死亡以及可能延缓动脉粥样硬化的进展。这些特性的临床意义仍有待研究。