Felodipine Grapefruit juice

The bioavailability of felodipine was increased approximately twofold when taken with grapefruit juice. Orange juice does not appear to modify the kinetics of PLENDIL Grapefruit juice—Coadministration of felodipine with grapefruit juice resulted in more than twofold increase in the AUC and Cmax, but no prolongation in the half-life of felodipine Grapefruit juice increased the of cilostazol by approximately 50%, but had no effect on AUC... 

Takanaga H, Ohnishi A, Matsuo H, et al. Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model. Br J Clin Pharmacol 2000 49(l) 49-58. 

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 (1997) Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. J Clin Invest. 99 2545-53. 

GK Dresser, DG Bailey, SG Carruthers. Grapefruit juice-felodipine interaction in the elderly. Clin Pharmacol Ther 68 28-34, 2000. 

Lundahl, J., Regardh, C. G., Edgar, B., Johnsson, G., Effects of grapefruit juice ingestion pharmacokinetics and haemodynamics of intravenous and orally administered felodipine in healthy men, Ear. J. Clin. Pharmacol. 1997, 52, 139-145. 

Bioavailability of felodipine is not affected by food, but increased more than 2-fold when taken with doubly concentrated grapefruit juice vs water or orange juice. High-fat meals and grapefruit juice with nisoldipine should be avoided. 

Amlodipine shows a preference for binding vascular smooth muscle cells over cardiac muscle cells, thus acting as a peripheral arterial vasodilator (Pfizer, Inc. 2005). Like most other CCB dihydropyridines, amlodipine is highly protein bound and heavily metabolized. In contrast to felodipine, this compound is not influenced by grapefruit juice and appears to show fewer drug-drug interactions. 

Bailey, D.G., Kreeft, J.H., Munoz, C., Freeman, D.J., and Bend, J.R., Grapefruit juice-felodipine interaction effect of naringin and 6, 7 -dihydroxybergamottin in humans, Clin. Pharm. Ther., 64, 248, 1998. 

Gray lines represent grapefruit juice (path of felodipine in presence of grapefruit juice... 

Malhotra S, Bailey DG, Paine MF, Watkins PB. Seville orange juice-felodipine interaction comparison with dilute grapefruit juice and involvement of furocoumarins. Clin Pharmacol Ther 2001 69(l) 14-23. 

Goosen TC, Cillie D, Bailey DG, et al. Bergamottin contribution to the grapefruit juice-felodipine interaction and disposition in humans. Clin Pharmacol Ther 2004 76(6) 607-617. 

Bailey DG, Bend JR, Arnold JM, Tran LT, Spence ID. Erythromycin-felodipine interaction magnitude, mechanism, and comparison with grapefruit juice. Clin Pharmacol Ther 1996 60(l) 25-33. 

Edgar B, Bailey D, Bergstrand R, Johnsson G, Regardh CG. Acute effects of drinking grapefruit juice on the pharmacokinetics and dynamics of felodipine— and its potential clinical relevance. Eur J Clin Pharmacol 1992 42(3) 313-317. 

Bailey DG, Arnold JM, Bend JR, Tran LT, Spence JD. Grapefruit juice-felodipine interaction reproducibility and characterization with the extended release drug formulation. Br J Clin Pharmacol 1995 40(2) 135-140. 

Paine MF, Widmer WW, Hart HL, et al. A furanocoumarin-free grapefruit juice establishes furanocoumarins as the mediators of the grapefruit juice-felodipine interaction. Am J Clin Nutr 2006 83(5) 1097-1105. 

Bailey DG, Arnold JM, Munoz C, et al. Grapefruit juice-felodipine interaction mechanism, predictability, and effect of naringin. Clin Pharmacol Ther 1993 53 (6) 637-642. 

Lundahl J, Regardh CG, Edgar B, et al. Relationship between time of intake of grapefruit juice and its effect on pharmacokinetics and pharmacodynamics of felodipine in healthy subjects. Eur J Clin Pharmacol 1995 49(l-2) 61-67. 

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