Nicardipine, a new calcium channel blocker: Role for vascular selectivity

Abstract

Summary: Calcium channel blockers are important drugs for the treatment of chronic stable angina. However, negative inotropic and dromotropic effects may limit their usefulness in patients with atrioventricular conduction abnormalities or left ventricular dysfunction. A new generation of calcium channel blockers will soon be available that have a more vascular selective action than currently available agents. Of the new agents, nicardipine has been most extensively studied. In experimental studies, nicardipine is more specific for vascular smooth muscle than for cardiac smooth muscle and for coronary than peripheral vasculature. In controlled trials, nicardipine exhibited efficacy and safety that was comparable to older calcium blockers or beta blockers. However, nicardipine was associated with minimal negative inotropic or dromotropic effects even in patients with existing left ventricular dysfunction. Thus, nicardipine may have an advantage over existing calcium channel blockers, especially in patients with underlying cardiac disease.

Hemodynamic effects of intravenous nicardipine in severely pre‐eclamptic women with a hypertensive crisis

“…Its administration in intravenous form, rapid onset of action and short half‐life allow easy titration against blood pressure while transplacental passage is limited (15%). Nicardipine induces general arterial relaxation that is more pronounced in cerebrovascular and coronary arteries. The depressant action on myocardial muscle cells is less than with nifedipine and its cerebrovascular selectivity renders it more effective in preventing ischemic stroke and hypertensive brain damage than other antihypertensive drugs.…”

Efficacy of Nicardipine for Long-Term Therapy of Chronic Stable Angina

“…Nicardipine, like other calcium channel blockers, has the additional advantage of not having the tolerance, which occurs with round-the-clock nitroglycerin. Reduction in afterload caused by the peripheral vasodilating effects may also reduce symptomatic anginal episodes (2,12,14,15). One study also suggested that nicardipine may be effective in reducing the diastolic dysfunction, and potentially the in-creased workload, that can occur with angina (14).…”

“…Nicardipine hydrochloride is a second-generation dihydropyridine calcium channel blocker with little effect on myocardial contractility or conduction (1,2) that has been shown to be effective for treating chronic stable angina (3)(4)(5)(6) in several short-term studies. Although previous studies (7,8) do suggest long-term efficacy of nicardipine for the reduction of anginal symptoms, the open-label design did not exclude spontaneous improvement of anginal symptoms or an exercise training effect in the change in symptoms or improvement on exercise parameters (9,10).…”

Preventive effect of nicardipine on hyperplastic changes in venous bypass grafts

“…Prior studies have revealed the safety and efficacy of nicardipine during long-term use [8]. The hypotensive effect of this drug is correlated with initial blood pressure, permitting its administration to normotensive subjects with coronary artery disease as well as to subjects with mild to moderate arterial hypertension [8,9]. The duration of nicardipine therapy required to obtain a clinical reflection of its vascular hyperplasia-preventing effect and whether its chronic use would be followed by the development of tolerance to this beneficial effect remain to be determined.…”