Nisoldipine is a second-generation
dihydropyridine calcium channel blocker (CCB). It is the most vascular selective of the currently available CCBs, and thus has the capacity to lower blood pressure without affecting the functioning of the myocardium and skeletal muscle, and without producing any negative inotropic effects.
Nisoldipine coat core (CC) is an
extended-release formulation that allows
nisoldipine to be released gradually over 24 hours, minimizing fluctuations in plasma concentration and providing a good trough/peak ratio. It has a slow onset and long duration of action, and ambulatory blood pressure monitoring has demonstrated that its
antihypertensive effect is maintained over 24 hours with no evidence of reflex
tachycardia,
hypotension, or sympathetic neurohormonal activation and no effects on circadian variation. Studies in patients with
hypertension have shown that
nisoldipine CC provides reductions in blood pressure that are at least equivalent to those seen with
diuretics, beta-blockers,
angiotensin-converting enzyme inhibitors, and other CCBs, without deleterious effects on metabolic parameters. In particular, it has been found to be effective in elderly patients and in black patients with severe
hypertension. The DEFIANT studies have demonstrated that
nisoldipine CC improves cardiac function and exercise tolerance in patients recovering from acute
myocardial infarction, without increasing the risk of mortality compared with placebo. It also improves exercise performance in patients with
stable angina pectoris.
Nisoldipine CC is well tolerated in all groups of patients, with the most frequently reported side effects being
headache and peripheral
edema, which are usually mild and transient.