van Zwieten P A
Eur Neurol. 1986;25 Suppl 1:57-67. doi: 10.1159/000116061.
The heterogeneity of the several subgroups of calcium-antagonistic drugs requires a rigid and well-defined differentiation of this type of agents. From the chemical point of view verapamil-like drugs, dihydropyridines, benzothiazepines and diphenylalkylamines should be distinguished. Among these largely different groups no obvious relationship between chemical structure and calcium-antagonistic activity can be recognized. Irrespective of the chemical classification all above-mentioned compounds inhibit the entry of calcium into cells. However, from a pharmacological point of view a distinction should be made between calcium channel blockers and calcium overload blockers. Calcium channel blockers selectively and competitively inhibit the transmembranous slow inward current, which is carried by calcium ions both in cardiac tissues and in vascular smooth muscle under physiological conditions. However, calcium overload blockers only inhibit the overload of the cell with calcium ions, which occurs under pathological, ischemic conditions. Finally, a survey is given of the various subtypes of calcium-antagonistic drugs with respect to their organ specificity and therapeutic applicability.
钙拮抗药物几个亚组的异质性要求对这类药物进行严格且明确的区分。从化学角度来看，应区分维拉帕米类药物、二氢吡啶类、苯并硫氮䓬类和二苯烷基胺类。在这些差异很大的类别中，无法识别出化学结构与钙拮抗活性之间的明显关系。无论化学分类如何，上述所有化合物均抑制钙离子进入细胞。然而，从药理学角度来看，应区分钙通道阻滞剂和钙超载阻滞剂。钙通道阻滞剂选择性且竞争性地抑制跨膜慢内向电流，在生理条件下，该电流由心脏组织和血管平滑肌中的钙离子携带。然而，钙超载阻滞剂仅抑制在病理缺血条件下发生的细胞钙离子超载。最后，就其器官特异性和治疗适用性对钙拮抗药物的各种亚型进行了综述。
