Nisoldipine coat-core. A review of its pharmacology and therapeutic efficacy in hypertension

Abstract

Nisoldipine coat-core is a long-acting formulation of the dihydropyridine calcium antagonist (calcium channel blocker) nisoldipine, suitable for once daily administration in the treatment of patients with hypertension. In clinical trials in patients with mild to moderate hypertension, nisoldipine coat-core has efficacy and tolerability similar to those of other calcium antagonists, and antihypertensive efficacy equivalent to that of agents from various other drug classes including beta-blockers, thiazide diuretics and ACE inhibitors. Unlike beta-blockers and thiazide diuretics, calcium antagonists (including nisoldipine coat-core) are not associated with clinically significant adverse metabolic effects on the serum lipid profile or glycaemic control. Nevertheless, published guidelines or consensus papers on the pharmacological management of patients with hypertension recommend calcium antagonists (and other drugs) as "alternative first-line' agents, while beta-blockers and diuretics are generally considered to be first-line therapy because of demonstrated benefits in terms of cardiovascular morbidity and mortality in this clinical setting. Nisoldipine coat-core maintains consistent plasma drug concentrations and antihypertensive effects throughout the 24-hour dosage interval, thereby attenuating intermittent reflex increases in sympathetic activity. This pharmacological profile may have important clinical implications; recent retrospective data suggest an association between moderate to high dosages of short-acting dihydropyridine calcium antagonists and adverse cardiovascular events, although this has yet to be confirmed in large prospective trials. In addition, the high degree of vasoselectivity of nisoldipine minimises negative inotropic effects which may be observed with less selective agents such as nifedipine. Nisoldipine coat-core is, therefore, a useful alternative to other antihypertensive agents in the management of patients with hypertension, providing consistent antihypertensive efficacy and good tolerability with once daily administration.