Differences in cardiovascular profile among calcium antagonists.
Differences in cardiovascular profile among calcium antagonists.
复制标题
钙拮抗剂之间心血管特征的差异。
DOI：
10.1016/0002-9149(87)90078-6
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发表时间：
1987
期刊：
影响因子：
--
通讯作者：
Norio Taira
中科院分区：
文献类型：
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作者：
Norio Taira
钙拮抗剂是一组具有不同化学结构的有机化合物。尽管它们的主要药效作用是血管舒张和心肌抑制，但它们在产生这些作用方面并不一致。根据使用分离的、血液灌注的狗的乳头肌、窦房结和房室结制剂测定的个体钙拮抗剂产生负性肌力、变时性和促速作用与冠状血管舒张剂效力的效力比较，钙拮抗剂分为两大类。二氢吡啶类药物、尼卡地平、硝苯地平、尼莫地平、尼索地平、尼群地平、PN 200-110（伊拉地平）和 PY 108-068 通常在产生冠状血管扩张方面比产生负性肌力、变时性和促速性（一级房室传导阻滞）作用更有效，尽管它们之间存在微小差异。非二氢吡啶类钙拮抗剂维拉帕米、地尔硫卓、KB-944、苯普地尔和MCl-176在产生冠状血管舒张和负性促肌作用方面几乎是等价的，尽管它们在产生负性肌力作用方面均较弱。非二氢吡啶类钙拮抗剂可进一步分为2个亚组。维拉帕米、地尔硫卓和 KB-944 在产生负向趋向性和变时性作用方面几乎是等价的。 Bepridil 和 MCI-176 产生负变时性的效力不如产生负变时性的效力。
Calcium antagonists constitute a group of organic compounds with diverse chemical structures. Although their main pharmacodynamic actions are vasodilatation and myocardial depression, they are not uniform in producing these effects. Based on comparison of the potencies in producing negative inotropic, chronotropic and dromotropic effects to the coronary vasodilator potency of individual calcium antagonists determined by use of isolated, blood-perfused papillary muscle, sinoatrial node and atrioventricular node preparations of dogs, calcium antagonists are classified into 2 major groups. The dihydropyridines, nicardipine, nifedipine, nimodipine, nisoldipine, nitrendipine, PN 200-110 (isradipine) and PY 108-068, are generally far more potent in producing coronary vasodilatation than in producing negative inotropic, chronotropic and dromotropic (first-degree atrioventricular block) effects, although there are minor differences among them. The non-dihydropyridine calcium antagonists, verapamil, diltiazem, KB-944, bepridil and MCl-176, are nearly equipotent in producing coronary vasodilatation and a negative dromotropic effect, although all of them are less potent in producing negative inotropy. The non-dihydropyridine calcium antagonists can be further divided into 2 subgroups. Verapamil, diltiazem and KB-944 are nearly equipotent in producing negative dromotropic and chronotropic effects. Bepridil and MCI-176 are less potent in producing negative chronotropy than in producing negative dromotropy.