Calcium channel antagonists part V: Second-generation agents

Abstract

Second-generation agents include new dihydropyridines, such as amlodipine, felodipine, isradipine, nicardipine, nimodipine, nisoldipine, and nitrendipine. Verapamil-like agents include tiapamil, gallopamil, and anipamil. Among the diphenylalkylamines, bepridil is of special interest. New preparations of existing agents include slow-release formulations of nifedipine, verapamil, and diltiazem. From all these agents will be selected those that are longer-acting and provide higher vascular selectivity.

Pharmacology and Therapeutic Potential of Lemildipine, a Highly Vasculoselective Dihydropyridine Derivative with Slow Onset and Long Duration of Action

“…A primary target for developing improved Ca2+ channel antagonists is to achieve a higher vascular selectivity compared with nifedipine. The newly developed secondgeneration agents of the 1,4-dihydropyridine class, structurally related to nifedipine, have much greater vascular selectivity and are important alternatives to the older agents (34,38). They are better tolerated and cause fewer adverse cardiac effects (36), which may allow their use in patients with congestive heart failure or other instances of compromised ventricular function.…”

Scintigraphic Evaluation of the Short- and Long-Term Renal Effects of Oral Felodipine Using Technetium-99m-Mercaptoacetyl Triglycine

“…The other indications for calcium antagonists include congestive heart failure, hypertrophic cardiomyopathy, methyl-3,5-pyridinedicarboxylate], effectively lowers ar terial blood pressure in animals and humans [2][3][4][5], This is due to a selective primary action on the smooth muscle of the arterial resistance vessel. It has also a wide spectrum of effects on the kidney [6].…”