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Chemical Compound Review

nicardipine     2-(benzyl-methyl-amino)ethyl methyl 2,6...

Synonyms: Nicardipino, Nicardipinum, Nicardipine LA, Cardene IV, Cardene SR, ...
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Disease relevance of nicardipine


Psychiatry related information on nicardipine


High impact information on nicardipine

  • Thyroid carcinoma in rats has been associated with treatment with nicardipine and after exposure to several aromatic hydrocarbons.(ABSTRACT TRUNCATED AT 400 WORDS)[9]
  • The calcium antagonists nifedipine, nicardipine, and diltiazem did not compete for the same binding site [10].
  • The Ca2+ responses to endothelin and thrombin were not affected by nicardipine (1 microM), (+) Bay K 8644, or Ca2+-free solutions [11].
  • Nicardipine, a calcium channel blocker, also increased the skin blood flow, but the blood flow increment and blood pressure fall were comparable [12].
  • In the Montreal Heart Institute trial, nicardipine did not influence the overall rate of progression and regression; however, nicardipine-treated patients experienced significantly less progression of minimal lesions, defined as stenoses of < or = 20% severity [13].

Chemical compound and disease context of nicardipine


Biological context of nicardipine


Anatomical context of nicardipine

  • Thus, nicardipine administered before or early after coronary artery occlusion limited infarct size by 37% to 49%, whereas when administration was delayed for 3 hr infarct size was not reduced [5].
  • Furthermore, nicardipine had more striking effects on the ischemic myocardium of dogs with small hypoperfused zones than on that of dogs with large hypoperfused zones [5].
  • In isolated feline papillary muscle, nicardipine produced a dose-dependent calcium antagonistic effect manifested by depressed indexes of contraction and relaxation [3].
  • The effects of calcium antagonists (verapamil, diltiazem, and nicardipine) on beta-adrenergic receptors of cultured cardiac myocytes isolated from neonatal rat ventricle were studied with the hydrophilic ligand [3H]CGP-12177, which identifies cell surface-bound beta-receptors [22].
  • Nicardipine prevents calcium loading and "oxygen paradox" in anoxic single rat myocytes by a mechanism independent of calcium channel blockade [23].

Associations of nicardipine with other chemical compounds


Gene context of nicardipine

  • The increase in BDNF mRNA expression induced at high K(+) was repressed not only by nicardipine, an antagonist for L-VDCC, but also by dl-amino-5-phosphonovalerate, an antagonist for NMDA-R, which was supported by the effects of antagonists on the Ca(2+) influx [27].
  • Intracellular mobilization was linked to increases in IP3 turnover because 1 microM ET-1 increased IP3 content by 48% from its control value (EC50 = 23 nM), whereas Ca2+ influx occurred through a non-L-type Ca2+ channel because preexposure to 1 microM nicardipine did not affect either the height or the duration of a [Ca2+]i transient [28].
  • The IC(50) values for the inhibition of CYP2D6 and CYP2C9 for nicardipine were 3 to 9 microM, whereas those for all others ranged from 14 to >150 microM [29].
  • Niguldipine, nicardipine, and nitrendipine also demonstrated potent BCRP inhibition, whereas nifedipine had no effect [30].
  • Nicardipine strongly inhibited two-pathways of triazolam hydroxylation both catalyzed by CYP3A4 [31].

Analytical, diagnostic and therapeutic context of nicardipine


  1. Nicardipine and urinary retention. Eicher, J.C., Chalopin, J.M., Tanter, Y., Louis, P., Rifle, G. JAMA (1987) [Pubmed]
  2. Effects of nicardipine on regional diastolic left ventricular function in patients with angina pectoris. Hanet, C., Rousseau, M.F., van Eyll, C., Pouleur, H. Circulation (1990) [Pubmed]
  3. Effects of nicardipine on myocardial function in vitro and in vivo. Lambert, C.R., Buss, D.D., Pepine, C.J. Circulation (1990) [Pubmed]
  4. Changes in myocardial metabolism during therapy in patients with chronic stable angina: a comparison of long-term dosing with propranolol and nicardipine. Rousseau, M.F., Hanet, C., Pardonge-Lavenne, E., Van den Berghe, G., Van Hoof, F., Pouleur, H. Circulation (1986) [Pubmed]
  5. Comparative effects of nicardipine, a new calcium antagonist, on size of myocardial infarction after coronary artery occlusion in dogs. Endo, T., Nejima, J., Fujita, S., Kiuchi, K., Iida, N., Kikuchi, K., Hayakawa, H., Okumura, H. Circulation (1986) [Pubmed]
  6. The use of nicardipine for electroconvulsive therapy: a dose-ranging study. Zhang, Y., White, P.F., Thornton, L., Perdue, L., Downing, M. Anesth. Analg. (2005) [Pubmed]
  7. Effect of oral nicardipine on anorectal function in normal human volunteers and patients with irritable bowel syndrome. Sun, W.M., Edwards, C.A., Prior, A., Rao, S.S., Read, N.W. Dig. Dis. Sci. (1990) [Pubmed]
  8. Bioequivalence study of nicardipine solution versus nicardipine tablets. Mignini, F., Bisbocci, D., Paglieri, C., Streccioni, V., Veglio, F., Amenta, F. Clin. Exp. Hypertens. (2004) [Pubmed]
  9. The effect of hepatic enzyme-inducing drugs on thyroid hormones and the thyroid gland. Curran, P.G., DeGroot, L.J. Endocr. Rev. (1991) [Pubmed]
  10. Specific binding of endothelin on human vascular smooth muscle cells in culture. Clozel, M., Fischli, W., Guilly, C. J. Clin. Invest. (1989) [Pubmed]
  11. Endothelin-induced increases in vascular smooth muscle Ca2+ do not depend on dihydropyridine-sensitive Ca2+ channels. Mitsuhashi, T., Morris, R.C., Ives, H.E. J. Clin. Invest. (1989) [Pubmed]
  12. Low-dose L-arginine administration increases microperfusion of hindlimb muscle without affecting blood pressure in rats. Ohta, F., Takagi, T., Sato, H., Ignarro, L.J. Proc. Natl. Acad. Sci. U.S.A. (2007) [Pubmed]
  13. Interventions that beneficially influence the evolution of coronary atherosclerosis. The case for calcium channel blockers. Waters, D., Lespérance, J. Circulation (1992) [Pubmed]
  14. Exaggerated vascular response due to endothelial dysfunction and role of the renin-angiotensin system at early stage of renal hypertension in rats. Hoshino, J., Sakamaki, T., Nakamura, T., Kobayashi, M., Kato, M., Sakamoto, H., Kurashina, T., Yagi, A., Sato, K., Ono, Z. Circ. Res. (1994) [Pubmed]
  15. Noninvasive assessment of the direct action of oral nifedipine and nicardipine on left ventricular contractile state in patients with systemic hypertension: importance of reflex sympathetic responses. Borow, K.M., Neumann, A., Lang, R.M., Ehler, D., Valentine-Bates, B., Wolff, A., Friday, K., Murphy, M. J. Am. Coll. Cardiol. (1993) [Pubmed]
  16. Intravenous nicardipine for the treatment of severe hypertension. A double-blind, placebo-controlled multicenter trial. Wallin, J.D., Fletcher, E., Ram, C.V., Cook, M.E., Cheung, D.G., MacCarthy, E.P., Townsend, R., Saunders, E., Davis, W.R., Langford, H.G. Arch. Intern. Med. (1989) [Pubmed]
  17. Calcium entry blockade and alpha-adrenergic vascular reactivity in human beings: differences between nicardipine and verapamil. Pedrinelli, R., Taddei, S., Salvetti, A. Clin. Pharmacol. Ther. (1989) [Pubmed]
  18. Calcium antagonists in patients with aneurysmal subarachnoid hemorrhage: a systematic review. Feigin, V.L., Rinkel, G.J., Algra, A., Vermeulen, M., van Gijn, J. Neurology (1998) [Pubmed]
  19. A controlled clinical trial to assess the effect of a calcium channel blocker on the progression of coronary atherosclerosis. Waters, D., Lespérance, J., Francetich, M., Causey, D., Théroux, P., Chiang, Y.K., Hudon, G., Lemarbre, L., Reitman, M., Joyal, M. Circulation (1990) [Pubmed]
  20. D1 receptor activation enhances evoked discharge in neostriatal medium spiny neurons by modulating an L-type Ca2+ conductance. Hernández-López, S., Bargas, J., Surmeier, D.J., Reyes, A., Galarraga, E. J. Neurosci. (1997) [Pubmed]
  21. In vivo characterization of combination antitumor chemotherapy with calcium channel blockers and cis-diamminedichloroplatinum(II). Onoda, J.M., Nelson, K.K., Taylor, J.D., Honn, K.V. Cancer Res. (1989) [Pubmed]
  22. Effects of calcium antagonists on beta-receptors of cultured cardiac myocytes isolated from neonatal rat ventricle. Yonemochi, H., Saikawa, T., Takakura, T., Ito, S., Takaki, R. Circulation (1990) [Pubmed]
  23. Nicardipine prevents calcium loading and "oxygen paradox" in anoxic single rat myocytes by a mechanism independent of calcium channel blockade. Hano, O., Silverman, H.S., Blank, P.S., Mellits, E.D., Baumgardner, R., Lakatta, E.G., Stern, M.D. Circ. Res. (1991) [Pubmed]
  24. Regulation of Ca2+ channels by cAMP and cGMP in vascular smooth muscle cells. Ishikawa, T., Hume, J.R., Keef, K.D. Circ. Res. (1993) [Pubmed]
  25. Central and peripheral vasopressin interact differently with sympathetic nervous system and renin-angiotensin system in renal hypertensive rabbits. Kumagai, H., Suzuki, H., Ichikawa, M., Matsumura, Y., Jimbo, M., Ryuzaki, M., Saruta, T. Circ. Res. (1993) [Pubmed]
  26. Systemic and pulmonary hemodynamic responses to nicardipine during graded ergometric exercise in patients with moderate to severe essential hypertension. Cody, R.J., Kubo, S.H., Ryman, K.S., Shaknovich, A., Laragh, J.H. J. Am. Coll. Cardiol. (1987) [Pubmed]
  27. Differential activation of brain-derived neurotrophic factor gene promoters I and III by Ca2+ signals evoked via L-type voltage-dependent and N-methyl-D-aspartate receptor Ca2+ channels. Tabuchi, A., Nakaoka, R., Amano, K., Yukimine, M., Andoh, T., Kuraishi, Y., Tsuda, M. J. Biol. Chem. (2000) [Pubmed]
  28. Endothelin-mediated cell signaling and proliferation in cultured rabbit corneal epithelial cells. Takagi, H., Reinach, P.S., Tachado, S.D., Yoshimura, N. Invest. Ophthalmol. Vis. Sci. (1994) [Pubmed]
  29. Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Ma, B., Prueksaritanont, T., Lin, J.H. Drug Metab. Dispos. (2000) [Pubmed]
  30. Effects of dihydropyridines and pyridines on multidrug resistance mediated by breast cancer resistance protein: in vitro and in vivo studies. Zhou, X.F., Yang, X., Wang, Q., Coburn, R.A., Morris, M.E. Drug Metab. Dispos. (2005) [Pubmed]
  31. Inhibitory effects of nicardipine to cytochrome P450 (CYP) in human liver microsomes. Nakamura, K., Ariyoshi, N., Iwatsubo, T., Fukunaga, Y., Higuchi, S., Itoh, K., Shimada, N., Nagashima, K., Yokoi, T., Yamamoto, K., Horiuchi, R., Kamataki, T. Biol. Pharm. Bull. (2005) [Pubmed]
  32. Nicardipine as antihypertensive therapy in liver transplant recipients: results of long-term use. Duvoux, C., Cherqui, D., Di Martino, V., Métreau, J.M., Salvat, A., Lauzet, J.Y., Fagniez, P.L., Dhumeaux, D. Hepatology (1997) [Pubmed]
  33. Renal effects of nicardipine, a calcium entry blocker, in hypertensive type II diabetic patients with nephropathy. Baba, T., Ishizaki, T., Ido, Y., Aoyagi, K., Murabayashi, S., Takebe, K. Diabetes (1986) [Pubmed]
  34. Short- and long-term efficacy of nicardipine, assessed by placebo-controlled single- and double-blind crossover trials in patients with chronic stable angina. Khurmi, N.S., Bowles, M.J., Bala Subramanian, V., Raftery, E.B. J. Am. Coll. Cardiol. (1984) [Pubmed]
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