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Chemical Compound Review

Felobeta     ethyl methyl 4-(2,3-dichlorophenyl)-2,6...

Synonyms: Perfudal, Felocor, Felodur, Felogamma, Munobal, ...
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Disease relevance of Renedil


Psychiatry related information on Renedil


High impact information on Renedil

  • Interaction of the antihypertensive drug felodipine with calmodulin [9].
  • Before and after receiving grapefruit juice, small bowel and colon mucosal biopsies were obtained endoscopically, oral felodipine kinetics were determined, and liver CYP3A4 activity was measured with the [14C N-methyl] erythromycin breath test in each subject [10].
  • Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression [10].
  • In addition, enterocyte concentrations of CYP3A4 measured before grapefruit juice consumption correlated with the increase in Cmax when felodipine was taken with either the 1st or the 16th glass of grapefruit juice relative to water (r = 0. 67, P = 0.043, and r = 0.71, P = 0.022, respectively) [10].
  • The mean felodipine bioavailability with grapefruit juice was 284 (range 164-469)% of that with water [1].

Chemical compound and disease context of Renedil


Biological context of Renedil


Anatomical context of Renedil

  • In order to study the systemic and coronary haemodynamic effects of felodipine, a new dihydropyridine derivative, 10 patients with coronary artery disease were studied during cardiac catheterization [17].
  • Effects on the ischaemic and reperfused myocardium of felodipine, a vasoselective calcium blocker, retrogradely infused into the coronary vein was investigated in a porcine model [18].
  • Long-term treatment with the angiotensin I converting enzyme inhibitors during ischemia abolished the increase in the capillary-to-fiber ratio in the soleus muscle, whereas a comparable antihypertensive dose of felodipine had no effect [15].
  • These results suggest that felodipine may exert vascular protective effects by suppressing free radical generation in human smooth muscle cells during activation of inflammatory mechanisms and diabetic conditions [19].
  • Compared with vehicle alone, felodipine significantly increased NOx generation, Ca2+-dependent NOS activity, and eNOS protein mass in proliferating and quiescent endothelial cells [20].

Associations of Renedil with other chemical compounds


Gene context of Renedil


Analytical, diagnostic and therapeutic context of Renedil

  • Cardiomyocytes from four groups of rats were studied: untreated CRF, CRF with parathyroidectomy (PTX), CRF with the calcium channel blocker felodipine (F), and sham operation of the kidney (SO) [28].
  • In an open, 3-way, randomized crossover design, 18 healthy volunteers ingested felodipine (10 mg) with 1 of the 3 juices (240 mL) [29].
  • Either felodipine (felo-retro group, 7 n = 6) or the corresponding amount of vehicle (vehicle group: n = 5) was retroinfused over 30 min starting 5 min prior to reperfusion [18].
  • The ergonovine test was performed once in basal conditions and twice 5 days after beginning the oral administration of felodipine 20 mg o.d., 4 and 24 h after the last administration [30].
  • All patients (mean age 79 +/- 6 years, office BP > or = 160/95 mmHg) were evaluated off any antihypertensive or anti-ischaemic therapy and after 3 months treatment with either felodipine or the diuretic (randomized, double-blind study) for episodes of significant ST-D (> or = 0.1 mV, duration > or = 1 min, interval > or = 1 min) [31].


  1. Interaction of citrus juices with felodipine and nifedipine. Bailey, D.G., Spence, J.D., Munoz, C., Arnold, J.M. Lancet (1991) [Pubmed]
  2. Cardiovascular and neurohumoral postural responses and baroreceptor abnormalities during a course of adjunctive vasodilator therapy with felodipine for congestive heart failure. Kassis, E., Amtorp, O. Circulation (1987) [Pubmed]
  3. Effect of the calcium antagonist felodipine as supplementary vasodilator therapy in patients with chronic heart failure treated with enalapril: V-HeFT III. Vasodilator-Heart Failure Trial (V-HeFT) Study Group. Cohn, J.N., Ziesche, S., Smith, R., Anand, I., Dunkman, W.B., Loeb, H., Cintron, G., Boden, W., Baruch, L., Rochin, P., Loss, L. Circulation (1997) [Pubmed]
  4. Felodipine in addition to beta-adrenergic blockade for angina pectoris. a multicentre, randomized, placebo-controlled trial. Rønnevik, P.K., Silke, B., Ostergaard, O. Eur. Heart J. (1995) [Pubmed]
  5. The influence of infusion rate on the hemodynamic effects of felodipine. Cohen, A.F., van Hall, M.A., van Harten, J., Schoemaker, R.C., Johansson, P., Breimer, D.D., Visser, R., Edgar, B. Clin. Pharmacol. Ther. (1990) [Pubmed]
  6. Effects of nimodipine, felodipine and amlodipine on electroconvulsive shock-induced amnesia in the rat. Zupan, G., Vitezić, D., Mrsić, J., Matesić, D., Simonić, A. Eur. J. Pharmacol. (1996) [Pubmed]
  7. Comparison between felodipine and isosorbide mononitrate as adjunct to beta blockade in patients > 65 years of age with angina pectoris. de Vries, R.J., Dunselman, P.H., van Veldhuisen, D.J., van den Heuvel, A.F., Wielenga, R.P., Lie, K.I. Am. J. Cardiol. (1994) [Pubmed]
  8. Hormonal and hemodynamic changes following single-dose felodipine treatment during mental stress. Haedersdal, C., Petersen, C.L., Lund, J.O., Trap-Jensen, J. Angiology. (1993) [Pubmed]
  9. Interaction of the antihypertensive drug felodipine with calmodulin. Bostróm, S.L., Ljung, B., Mårdh, S., Forsen, S., Thulin, E. Nature (1981) [Pubmed]
  10. Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. Lown, K.S., Bailey, D.G., Fontana, R.J., Janardan, S.K., Adair, C.H., Fortlage, L.A., Brown, M.B., Guo, W., Watkins, P.B. J. Clin. Invest. (1997) [Pubmed]
  11. 24 h anti-anginal and anti-ischaemic effects with once daily felodipine. A double-blind comparison with nifedipine, twice daily, and placebo in patients with stable exercise induced angina pectoris. Schulte, K.L. Eur. Heart J. (1995) [Pubmed]
  12. Increased exercise tolerance and reduced electrocardiographic ischaemia 3 and 12 hours after oral felodipine in effort angina. Verdecchia, P., Gatteschi, C., Benemio, G., Guerrieri, M., Boldrini, F., Pollavini, G., Porcellati, C. Eur. Heart J. (1989) [Pubmed]
  13. Addition of felodipine to metoprolol vs replacement of metoprolol by felodipine in patients with angina pectoris despite adequate beta-blockade. Results of the Felodipine ER and Metoprolol CR in Angina (FEMINA) Study. Working Group on Cardiovascular Research, The Netherlands (WCN). Dunselman, P., Liem, A.H., Verdel, G., Kragten, H., Bosma, A., Bernink, P. Eur. Heart J. (1997) [Pubmed]
  14. Different results in cardiopulmonary exercise tests after long-term treatment with felodipine and enalapril in patients with congestive heart failure due to ischaemic heart disease. Dunselman, P.H., van der Mark, T.W., Kuntze, C.E., van Bruggen, A., Hamer, J.P., Scaf, A.H., Wesseling, H., Lie, K.I. Eur. Heart J. (1990) [Pubmed]
  15. Antihypertensive therapy and adaptive mechanisms in peripheral ischemia. Nelissen-Vrancken, H.J., Boudier, H.A., Daemen, M.J., Smits, J.F. Hypertension (1993) [Pubmed]
  16. Reduced felodipine bioavailability in patients taking anticonvulsants. Capewell, S., Freestone, S., Critchley, J.A., Pottage, A., Prescott, L.F. Lancet (1988) [Pubmed]
  17. Effects of felodipine on systemic and coronary haemodynamics in patients with angina pectoris. Emanuelsson, H., Hjalmarson, A., Holmberg, S., Waagstein, F. Eur. Heart J. (1984) [Pubmed]
  18. Coronary venous retroinfusion of felodipine reducing infarct size without affecting regional myocardial blood flow. Haga, Y., Hatori, N., Nordlander, M., Nordlander, R., Sjöquist, P.O., Rydén, L. Eur. Heart J. (1993) [Pubmed]
  19. Felodipine inhibits free-radical production by cytokines and glucose in human smooth muscle cells. Hishikawa, K., Lüscher, T.F. Hypertension (1998) [Pubmed]
  20. Calcium channel blockade enhances nitric oxide synthase expression by cultured endothelial cells. Ding, Y., Vaziri, N.D. Hypertension (1998) [Pubmed]
  21. Metal ions as allosteric regulators of calmodulin. Mills, J.S., Johnson, J.D. J. Biol. Chem. (1985) [Pubmed]
  22. Antihypertensive 1,4-dihydropyridines as correctors of the cystic fibrosis transmembrane conductance regulator channel gating defect caused by cystic fibrosis mutations. Pedemonte, N., Diena, T., Caci, E., Nieddu, E., Mazzei, M., Ravazzolo, R., Zegarra-Moran, O., Galietta, L.J. Mol. Pharmacol. (2005) [Pubmed]
  23. Divergent effects of dihydropyridine and phenylalkylamine calcium channel antagonist classes on autonomic function in human hypertension. Kailasam, M.T., Parmer, R.J., Cervenka, J.H., Wu, R.A., Ziegler, M.G., Kennedy, B.P., Adegbile, I.A., O'Connor, D.T. Hypertension (1995) [Pubmed]
  24. Urinary excretion of aquaporin-2 after furosemide and felodipine in healthy humans. Starklint, J., Bech, J.N., Pedersen, E.B. Scand. J. Clin. Lab. Invest. (2005) [Pubmed]
  25. The effect of Ca2+ channel antagonists on plasma concentrations of matrix metalloproteinase-2 and -9 in essential hypertension. Zervoudaki, A., Economou, E., Pitsavos, C., Vasiliadou, K., Aggeli, C., Tsioufis, K., Toutouza, M., Stefanadis, C., Toutouzas, P. Am. J. Hypertens. (2004) [Pubmed]
  26. Selective biotransformation of taxol to 6 alpha-hydroxytaxol by human cytochrome P450 2C8. Rahman, A., Korzekwa, K.R., Grogan, J., Gonzalez, F.J., Harris, J.W. Cancer Res. (1994) [Pubmed]
  27. Felodipine inhibits nuclear translocation of p42/44 mitogen-activated protein kinase and human smooth muscle cell growth. Yang, Z., Madinova, A., Kozai, T., Joch, H., Aebi, U., Lüscher, T.F. Cardiovasc. Res. (2002) [Pubmed]
  28. Elevated myocardial cytosolic calcium impairs insulin-like growth factor-1-stimulated protein synthesis in chronic renal failure. Qing, D.P., Ding, H., Vadgama, J., Wu, Y.Y., Kopple, J.D. J. Am. Soc. Nephrol. (1999) [Pubmed]
  29. A furanocoumarin-free grapefruit juice establishes furanocoumarins as the mediators of the grapefruit juice-felodipine interaction. Paine, M.F., Widmer, W.W., Hart, H.L., Pusek, S.N., Beavers, K.L., Criss, A.B., Brown, S.S., Thomas, B.F., Watkins, P.B. Am. J. Clin. Nutr. (2006) [Pubmed]
  30. Once daily felodipine in preventing ergonovine-induced myocardial ischaemia in Prinzmetal's variant angina. Chimienti, M., Negroni, M.S., Pusineri, E., Regazzi, M.B., Inglese, L., Klersy, C., De Ambroggi, L. Eur. Heart J. (1994) [Pubmed]
  31. Antihypertensive treatment with felodipine but not with a diuretic reduces episodes of myocardial ischaemia in elderly patients with hypertension. Trenkwalder, P., Dobrindt, R., Aulehner, R., Lydtin, H. Eur. Heart J. (1994) [Pubmed]
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