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.