Pharmacodynamics of nilvadipine, a new dihydropyridine-type calcium antagonist
1Institute for Pharmacology and Toxicology, Technical University Munich, Germany.
Abstract:
Nilvadipine is a new calcium antagonist of the dihydropyridine type. It reduces blood pressure by high-affinity blockade of calcium channels in arterial cells, which leads to relaxation of arterial vessels. Nilvadipine has both pharmacokinetic and pharmacodynamic advantages compared to nifedipine (the prototype of the dihydropyridines). The duration of action is longer and it has a 4- to 16-fold higher vasodilatory potency that is accompanied by less cardiodepression and adrenergic counterregulation. The higher vascular selectivity of nilvadipine is documented by its vascular/cardiac potency ratio of 251, which is 9- to 10-fold greater than that of nifedipine. When used therapeutically as an antihypertensive agent, even in patients with heart failure or concomitant beta-blockade, nilvadipine has no negative inotropic, chronotropic, or dromotropic effects. Nilvadipine has been shown to have a more potent antiatherogenic effect than that of nifedipine in vitro and in animal models.
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