Calcium antagonist and the peripheral circulation: differences and similarities between PY 108–068, nicardipine, verapamil and diltiazem
Calcium antagonist and the peripheral circulation: differences and similarities between PY 108–068, nicardipine, verapamil and diltiazem
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钙拮抗剂和外周循环：PY 108-068、尼卡地平、维拉帕米和地尔硫卓之间的异同
DOI：
10.1111/j.1476-5381.1983.tb09403.x
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发表时间：
1983
影响因子：
7.3
通讯作者：
R. Hof
中科院分区：
文献类型：
--
作者：
R. Hof
1 在用氯醛糖-尿烷麻醉的开胸猫中测量了两种二氢吡啶类药物 PY 108-068 (PY) 和尼卡地平 (N) 以及另外两种钙拮抗剂维拉帕米 (V) 和地尔硫卓 (D) 对局部血流的影响。 2 每种物质以 3 种不同的剂量率输注，每种剂量率 10 分钟。 PY 的总剂量为 5 + 10 + 35（总计 50）μg/kg，N 为 10 + 20 + 70（总计 100）μg/kg，V 和 D 为 100 + 200 + 700（总计 1000）μg/kg。 3 所有物质均降低血压并增加总外周电导。仅 V、D 和 PY 降低心率。仅使用二氢吡啶衍生物即可显着增加心输出量； D 影响很小，V 几乎没有影响。 4 所有物质都会增加冠状动脉流量，并将其重新分布到有利于心外膜下层。所有物质都会增加大脑的血流量。维拉帕米的作用相对较小。 5 两种二氢吡啶衍生物可显着增加骨骼肌流量。 D 和 V 的影响可以忽略不计。 6 胃和小肠的血流量仅略有增加。在地尔硫卓治疗的动物中，流向肾脏的流量略有增加，但与所有其他治疗相比没有变化。流向肝脏、肾上腺和脾脏的流量保持不变或呈减少趋势。 7 器官电导比血流量值更能反映血管张力的主动变化，表明即使在血流量趋于减少的大多数器官中也存在血管舒张的趋势。 8 早期硝苯地平系列实验中获得的结果与此处描述的 N 的结果非常相似，只是硝苯地平的效力大约是硝苯地平的两倍。 9 因此，钙拮抗剂既不是一般的外周血管扩张剂，也没有表现出统一的优先作用位点模式。最重要的共同特征是冠状动脉和脑血流量的增加，最重要的差异是一侧的二氢吡啶和另一侧的V和D对骨骼肌流量的不同影响。该血管床的大小可能有助于解释为什么二氢吡啶作为外周血管扩张剂似乎特别有效。
1 The effects of two dihydropyridines, PY 108–068 (PY) and nicardipine (N), and two other calcium antagonists, verapamil (V) and diltiazem (D), on regional blood flow were measured in open‐chest cats, anaesthetized with chloralose‐urethane. 2 Each substance was infused at 3 different dose rates, each for 10 min. The total doses given were 5 plus 10 plus 35 (total of 50) μg/kg for PY, 10 plus 20 plus 70 (total of 100) μg/kg for N and 100 plus 200 plus 700 (total of 1000) μg/kg for V and D. 3 All substances lowered blood pressure and increased total peripheral conductance. Heart rate was lowered only by V, D and PY. Cardiac output was markedly increased only by the diyhydroypridine derivatives; D had small and V almost no effects. 4 All substances increased coronary flow and redistributed it in favour of the subepicardial layer. All substances also increased blood flow to the brain. The effects of verapamil were comparatively small. 5 Skeletal muscle flow was increased strongly by the two dihydropyridine derivatives. D and V had negligible effects. 6 Blood flow to stomach and small intestine was only slightly increased. Flow to the kidneys increased slightly in diltiazem‐treated animals but did not change with all other treatments. Flow to the liver, the adrenals, and the spleen remained unchanged or showed a tendency to decrease. 7 The organ conductances which reflect the active changes in vascular tone better than blood flow values, showed that there was a tendency towards vasodilatation even in most organs where blood flow tended to decrease. 8 Results obtained in an earlier series of experiments with nifedipine were very similar to those described here for N, except that nifedipine was about twice as potent. 9 Calcium antagonists were thus neither general peripheral vasodilators nor did they show a uniform pattern of preferential sites of action. The most important common features were increases in coronary and cerebral blood flow and the most important differences the divergent effects of the dihydropyridines on one side and V and D on the other side on skeletal muscle flow. The size of this vascular bed may help to explain why dihydropyridines appear to be particularly potent as peripheral vasodilators.
影响因子：
20.1
作者：
Walus,KM;Fondacaro,JD;Jacobson,ED
通讯作者：
Jacobson,ED
地尔硫卓对心肌血流量的影响。
影响因子：
37.8
作者：
Bache,RJ;Dymek,DJ
通讯作者：
Dymek,DJ