Pharmacokinetics, pharmacodynamics, and clinical utility of nisoldipine coat core in the treatment of essential hypertension

Nisoldipine coat core (CC) is a second-generation dihydropyridine calcium antagonist. The structure-activity relationship of the dihydropyridine calcium antagonists has been exploited to produce highly specific and potent agents for the relaxation of arterial smooth muscle. The clinical effects of nisoldipine CC extend well into the once-daily dosing range due to its novel, sustained-release, CC formulation. The drug appears to be well tolerated in combination with other widely prescribed antihypertensive agents and other cardiovascular compounds. Preliminary data are reported from 5 randomized, controlled, double-blind trials that compared the efficacy and tolerability of nisoldipine CC with placebo, amlodipine, hydro-chlorothiazide (HCTZ), lisinopril, and in combination with lisinopril or atenolol in the treatment of mild-to-moderate hypertension. Nisoldipine CC was as effective as these established antihypertensive agents in lowering blood pressure and was equally well tolerated as placebo, amlodipine, and lisinopril. Use of nisoldipine CC was associated with a slightly higher incidence of adverse effects than HCTZ. However, unlike the diuretic, nisoldipine CC did not induce adverse metabolic effects, Administered as a once-daily dose of 10 mg/d to 40 mg/d, nisoldipine CC demonstrated a smooth onset of action, no effect on heart rate, and constant 24-hour blood pressure control. The results of these 5 trials establish nisoldipine CC as both efficacious and well tolerated. This fact, along with a once-daily dosing regimen, establish it as a useful agent for the treatment of essential hypertension.