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1,4-二氢吡啶类钙通道阻滞剂的差异效应:治疗意义

Differential effects of 1,4-dihydropyridine calcium channel blockers: therapeutic implications.

作者信息

Katz A M, Leach N M

机构信息

Division of Cardiology, University of Connecticut, Farmington 06032.

出版信息

J Clin Pharmacol. 1987 Nov;27(11):825-34. doi: 10.1002/j.1552-4604.1987.tb05576.x.

DOI:10.1002/j.1552-4604.1987.tb05576.x
PMID:3323259
Abstract

Increasing recognition of the importance of calcium in the pathogenesis of cardiovascular disease has stimulated research into the use of calcium channel blocking agents for treatment of a variety of cardiovascular diseases. The favorable efficacy and tolerability profiles of these agents make them attractive therapeutic modalities. Clinical applications of calcium channel blockers parallel their tissue selectivity. In contrast to verapamil and diltiazem, which are roughly equipotent in their actions on the heart and vascular smooth muscle, the dihydropyridine calcium channel blockers are a group of potent peripheral vasodilator agents that exert minimal electrophysiologic effects on cardiac nodal or conduction tissue. As the first dihydropyridine available for use in the United States, nifedipine controls angina and hypertension with minimal depression of cardiac function. Additional members of this group of calcium channel blockers have been studied for a variety of indications for which they may offer advantages over current therapy. Once or twice daily dosage possible with nitrendipine and nisoldipine offers a convenient administration schedule, which encourages patient compliance in long-term therapy of hypertension. The coronary vasodilating properties of nisoldipine have led to the investigation of this agent for use in angina. Selectivity for the cerebrovascular bed makes nimodipine potentially useful in the treatment of subarachnoid hemorrhage, migraine headache, dementia, and stroke. In general, the dihydropyridine calcium channel blockers are usually well tolerated, with headache, facial flushing, palpitations, edema, nausea, anorexia, and dizziness being the more common adverse effects.

摘要

对钙在心血管疾病发病机制中的重要性的认识不断提高,激发了对使用钙通道阻滞剂治疗各种心血管疾病的研究。这些药物良好的疗效和耐受性使其成为有吸引力的治疗方式。钙通道阻滞剂的临床应用与其组织选择性平行。与维拉帕米和地尔硫䓬对心脏和血管平滑肌的作用大致相当不同,二氢吡啶类钙通道阻滞剂是一组强效的外周血管扩张剂,对心脏节点或传导组织的电生理作用极小。作为美国首个可供使用的二氢吡啶类药物,硝苯地平在对心功能影响最小的情况下控制心绞痛和高血压。这组钙通道阻滞剂的其他成员已针对多种适应症进行了研究,它们可能比目前的治疗方法更具优势。尼群地平和尼索地平每日一次或两次给药提供了方便的给药方案,这有利于患者长期治疗高血压时的依从性。尼索地平的冠状动脉扩张特性已促使对该药物用于心绞痛进行研究。对脑血管床的选择性使尼莫地平在治疗蛛网膜下腔出血、偏头痛、痴呆和中风方面具有潜在用途。一般来说,二氢吡啶类钙通道阻滞剂通常耐受性良好,头痛、面部潮红、心悸、水肿、恶心、厌食和头晕是较常见的不良反应。

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Differential effects of 1,4-dihydropyridine calcium channel blockers: therapeutic implications.1,4-二氢吡啶类钙通道阻滞剂的差异效应:治疗意义
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Principal component analysis of HPLC retention data and molecular modeling structural parameters of cardiovascular system drugs in view of their pharmacological activity.基于心血管系统药物的药理活性,对其高效液相色谱保留数据和分子模拟结构参数进行主成分分析。
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Nimodipine has no effect on the cerebral circulation in conscious pigs, despite an increase in cardiac output.尽管尼莫地平可增加心输出量,但对清醒猪的脑循环没有影响。
Br J Pharmacol. 1990 Jun;100(2):277-82. doi: 10.1111/j.1476-5381.1990.tb15795.x.