Bayer R, Mannhold R
Institut fuer Klinische Physiologie, Universität Düsseldorf, Federal Republic of Germany.
Pharmatherapeutica. 1987;5(2):103-36.
Fendiline is an anti-anginal agent for the treatment of coronary heart disease. Together with other diphenylalkylamines it is sub-classified in the group of lipophilic calcium antagonists. It binds to the calcium channel and to calmodulin with rather similar affinities. Pharmaco-dynamically, it exerts the typical calcium as well as calmodulin antagonistic actions: inhibition of the transmembrane calcium current, smooth muscle relaxation, negative inotropism, cardioprotection, inhibition of calmodulin-activated myosin light-chain kinase and phosphodiesterase. Pharmacokinetics reveal slow onset of action and a long half-life. The anti-anginal and anti-ischaemic efficacy of fendiline has been proven in several placebo-controlled, double-blind trials. It does not interfere with digoxin therapy. Direct comparison with other calcium antagonists by means of controlled studies revealed that its potency is at least equal to that of nifedipine but, in contrast to nifedipine, verapamil, and diltiazem, its anti-anginal action increases during chronic therapy, reaching a steady state of action after 2 to 3 weeks. In addition, the anti-ischaemic and anti-anginal potency is about equal to that of isosorbide dinitrate but fendiline has the advantage of lacking tolerance development. Nevertheless, the data presented indicate that a combination of fendiline with low doses of ISDN may be beneficial. Adverse cardiac and haemodynamic actions, such as increase or decrease in heart rate, disturbance of AV nodal conduction, impairment of cardiac contractile performance or considerable decrease in arterial pressure in hypotensives and normotensives, are lacking.
芬地林是一种用于治疗冠心病的抗心绞痛药物。它与其他二苯烷基胺一起被归类为亲脂性钙拮抗剂。它以相当相似的亲和力与钙通道和钙调蛋白结合。在药效学方面，它发挥典型的钙以及钙调蛋白拮抗作用：抑制跨膜钙电流、平滑肌松弛、负性肌力作用、心脏保护作用、抑制钙调蛋白激活的肌球蛋白轻链激酶和磷酸二酯酶。药代动力学显示起效缓慢且半衰期长。芬地林的抗心绞痛和抗缺血疗效已在多项安慰剂对照、双盲试验中得到证实。它不干扰地高辛治疗。通过对照研究与其他钙拮抗剂直接比较表明，其效力至少与硝苯地平相当，但与硝苯地平、维拉帕米和地尔硫䓬不同的是，其抗心绞痛作用在长期治疗期间会增强，在2至3周后达到稳定的作用状态。此外，其抗缺血和抗心绞痛效力约与硝酸异山梨酯相当，但芬地林具有不会产生耐受性的优点。然而，所提供的数据表明芬地林与低剂量的硝酸异山梨酯联合使用可能有益。它不存在不良的心脏和血流动力学作用，如心率增加或降低、房室结传导紊乱、心脏收缩性能受损或低血压和正常血压者动脉压显著下降等情况。
