Cellular action of nicardipine
- PMID: 2801573
- DOI: 10.1016/0002-9149(89)90973-9
Cellular action of nicardipine
Abstract
Nicardipine, a calcium antagonist of the 1:4 dihydropyridine type, has been used to treat angina and hypertension and is currently being examined as an agent for treating ischemia of cerebral and myocardial tissue. Nicardipine shows high affinity for the dihydropyridine binding site (pKi = 9.7) and inhibits the L-type calcium ion channel as demonstrated by its ability to decrease the calcium ion-dependent action potential dose-dependently in ventricular papillary muscle (pIC50 = 7.15). Nicardipine shows greater potency in inhibiting the response of vascular smooth muscle (pIC50 = 8.20) than that of cardiac muscle (pIC50 = 7.15). The nicardipine selectivity for vascular smooth muscle is greater than that shown by other dihydropyridine calcium antagonists such as nifedipine and accounts for the efficacy of nicardipine in the treatment of angina and hypertension. Various mechanisms have been proposed to account for the beneficial action of nicardipine in treating animal models of cerebral ischemia and myocardial infarction. For example, it has been suggested that (1) nicardipine has a specific membrane-stabilizing effect on cell membranes, (2) the compound blocks certain sodium channels, (3) it may become concentrated in ischemic cells, or (4) it may stimulate calcium ion efflux from mitochondria, and these actions may account for the inhibition by nicardipine of veratrine-induced contraction of myocytes. In this study, some of these effects of nicardipine were examined. However, the suggestion that nicardipine concentrates in ischemic cells owing to the tertiary amine structure could not be conclusively demonstrated.(ABSTRACT TRUNCATED AT 250 WORDS)
Similar articles
-
Animal pharmacology of nicardipine and its clinical relevance.Am J Cardiol. 1987 Jun 30;59(17):3J-8J. doi: 10.1016/0002-9149(87)90206-2. Am J Cardiol. 1987. PMID: 2440294 Review.
-
Tissue response selectivity of calcium antagonists is not due to heterogeneity of [3H]-nitrendipine binding sites.Br J Pharmacol. 1984 Jun;82(2):309-20. doi: 10.1111/j.1476-5381.1984.tb10765.x. Br J Pharmacol. 1984. PMID: 6329392 Free PMC article.
-
Clinical pharmacology, pharmacokinetics, and hemodynamic effects of nicardipine.Am Heart J. 1990 Feb;119(2 Pt 2):427-34. doi: 10.1016/s0002-8703(05)80063-8. Am Heart J. 1990. PMID: 1967896 Review.
-
Differential effect of a dihydropyridine derivative to Ca2+ entry pathways in neuronal preparations.Brain Res. 1984 Jun 3;301(2):323-30. doi: 10.1016/0006-8993(84)91101-6. Brain Res. 1984. PMID: 6329451
-
Cardiac and vascular effects of NZ-105, a novel dihydropyridine derivative, in vitro.Arch Int Pharmacodyn Ther. 1991 Nov-Dec;314:57-73. Arch Int Pharmacodyn Ther. 1991. PMID: 1668604
Cited by
-
Preventive effect of nicardipine on hyperplastic changes in venous bypass grafts.World J Surg. 1993 Jan-Feb;17(1):94-9; discussion 99-100. doi: 10.1007/BF01655716. World J Surg. 1993. PMID: 8447148
-
Potentiation of the cardiovascular effects of nicardipine by enflurane anesthesia in canine blood-perfused heart preparations.J Anesth. 1992 Apr;6(2):176-82. doi: 10.1007/s0054020060176. J Anesth. 1992. PMID: 15278563
-
Effect of nicardipine on pulmonary hypertension after repair of congenital heart defects in early postoperative period.J Anesth. 1993 Jan;7(1):95-101. doi: 10.1007/s0054030070095. J Anesth. 1993. PMID: 15278502
-
Nicardipine suppresses bronchoconstrictor actions of pharmacologic agents in guinea pigs.Lung. 1991;169(6):343-55. doi: 10.1007/BF02714171. Lung. 1991. PMID: 1758203
-
Intravenous nicardipine: its use in the short-term treatment of hypertension and various other indications.Drugs. 2006;66(13):1755-82. doi: 10.2165/00003495-200666130-00010. Drugs. 2006. PMID: 16978041 Review.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources