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Substrate

Grapefruit juice-drug interaction studies as a method to assess the extent of intestinal
availability: utility and limitations
Michael Gertz, John D. Davis, Anthony Harrison, J. Brian Houston and Aleksandra Galetin
Referenced bioavailability and FG,GFJ values for 32 CYP3A substrates used in figure 1A.
Accepted for publication in Curr Drug Metab, September 2008
Substrate
Bioavailability, F (%) [1]
GFJ References
n

[1] Benet, L.Z.; Oie, S. and Schwartz, J.B., Appendix II Design and Optimization of Dosage Regimens;
Pharmacokinetic Data. In: The Pharmacological Basis of Therapeutics, Ninth Edition. 9, ed. JG
Hardman, Limbird, LE, Molinoff, PB, et al. 1996: The McGraw Companies, Inc. 1697-1791.
[2] Kantola, T.; Kivisto, K.T. and Neuvonen, P.J. Grapefruit juice greatly increases serum
concentrations of lovastatin and lovastatin acid (1998) Clin. Pharmacol. Ther., 63(4), 397-402.
[3] Lilja, J.J.; Kivisto, K.T.; Backman, J.T.; Lamberg, T.S. and Neuvonen, P.J. Grapefruit juice
substantially increases plasma concentrations of buspirone (1998) Clin. Pharmacol. Ther., 64(6), 655-
660.
[4] Lilja, J.J.; Kivisto, K.T. and Neuvonen, P.J. Duration of effect of grapefruit juice on the
pharmacokinetics of the CYP3A4 substrate simvastatin (2000) Clin. Pharmacol. Ther., 68(4), 384-390.
[5] Lilja, J.J.; Kivisto, K.T. and Neuvonen, P.J. Grapefruit juice-simvastatin interaction: effect on
serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors (1998) Clin.
Pharmacol. Ther.
, 64(5), 477-483.
[6] Lilja, J.J.; Neuvonen, M. and Neuvonen, P.J. Effects of regular consumption of grapefruit juice on
the pharmacokinetics of simvastatin (2004) Br. J. Clin. Pharmacol., 58(1), 56-60.
[7] Nagy, J.; Schipper, H.G.; Koopmans, R.P.; Butter, J.J.; Van Boxtel, C.J. and Kager, P.A. Effect of
grapefruit juice or cimetidine coadministration on albendazole bioavailability (2002) Am J Trop Med
Hyg
, 66(3), 260-263.
[8] Takanaga, H.; Ohnishi, A.; Murakami, H.; Matsuo, H.; Higuchi, S.; Urae, A.; Irie, S.; Furuie, H.;
Matsukuma, K.; Kimura, M.; Kawano, K.; Orii, Y.; Tanaka, T. and Sawada, Y. Relationship between
time after intake of grapefruit juice and the effect on pharmacokinetics and pharmacodynamics of
nisoldipine in healthy subjects (2000) Clin. Pharmacol. Ther., 67(3), 201-214.
[9] Bailey, D.G.; Arnold, J.M.; Strong, H.A.; Munoz, C. and Spence, J.D. Effect of grapefruit juice and
naringin on nisoldipine pharmacokinetics (1993) Clin. Pharmacol. Ther., 54(6), 589-594.
[10] Charbit, B.; Becquemont, L.; Lepere, B.; Peytavin, G. and Funck-Brentano, C. Pharmacokinetic
and pharmacodynamic interaction between grapefruit juice and halofantrine (2002) Clin. Pharmacol.
Ther.
, 72(5), 514-523.
[11] Bailey, D.G.; Arnold, J.M.; Bend, J.R.; Tran, L.T. and Spence, J.D. Grapefruit juice-felodipine
interaction: reproducibility and characterization with the extended release drug formulation (1995) Br.
J. Clin. Pharmacol.
, 40(2), 135-140.
[12] Bailey, D.G.; Arnold, J.M.; Munoz, C. and Spence, J.D. Grapefruit juice - felodipine interaction:
mechanism, predictability, and effect of naringin (1993) Clin. Pharmacol. Ther., 53(6), 637-642.
[13] Bailey, D.G.; Bend, J.R.; Arnold, J.M.; Tran, L.T. and Spence, J.D. Erythromycin-felodipine
interaction: magnitude, mechanism, and comparison with grapefruit juice (1996) Clin. Pharmacol.
Ther.
, 60(1), 25-33.
[14] Bailey, D.G.; Dresser, G.K. and Bend, J.R. Bergamottin, lime juice, and red wine as inhibitors of
cytochrome P450 3A4 activity: comparison with grapefruit juice (2003) Clin. Pharmacol. Ther., 73(6),
529-537.
[15] Bailey, D.G.; Dresser, G.K.; Kreeft, J.H.; Munoz, C.; Freeman, D.J. and Bend, J.R. Grapefruit-
felodipine interaction: effect of unprocessed fruit and probable active ingredients (2000) Clin.
Pharmacol. Ther.
, 68(5), 468-477.
[16] 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 (1998) Clin. Pharmacol.
Ther.
, 64(3), 248-256.
[17] Bailey, D.G.; Spence, J.D.; Munoz, C. and Arnold, J.M. Interaction of citrus juices with felodipine
and nifedipine (1991) Lancet., 337(8736), 268-269.
[18] Edgar, B.; Bailey, D.; Bergstrand, R.; Johnsson, G. and Regardh, C.G. Acute effects of drinking
grapefruit juice on the pharmacokinetics and dynamics of felodipine--and its potential clinical
relevance (1992) Eur. J. Clin. Pharmacol., 42(3), 313-317.
[19] Goosen, T.C.; Cillie, D.; Bailey, D.G.; Yu, C.; He, K.; Hollenberg, P.F.; Woster, P.M.; Cohen, L.;
Williams, J.A.; Rheeders, M. and Dijkstra, H.P. Bergamottin contribution to the grapefruit juice-
felodipine interaction and disposition in humans (2004) Clin. Pharmacol. Ther., 76(6), 607-617.
[20] Lown, K.S.; Bailey, D.G.; Fontana, R.J.; Janardan, S.K.; Adair, C.H.; Fortlage, L.A.; Brown,
M.B.; Guo, W. and Watkins, P.B. Grapefruit juice increases felodipine oral availability in humans by
decreasing intestinal CYP3A protein expression (1997) J. Clin. Invest., 99(10), 2545-2553.
[21] Lundahl, J.; Regardh, C.G.; Edgar, B. and Johnsson, G. Relationship between time of intake of
grapefruit juice and its effect on pharmacokinetics and pharmacodynamics of felodipine in healthy
subjects (1995) Eur. J. Clin. Pharmacol., 49(1-2), 61-67.
[22] Lundahl, J.U.; Regardh, C.G.; Edgar, B. and Johnsson, G. The interaction effect of grapefruit juice
is maximal after the first glass (1998) Eur. J. Clin. Pharmacol., 54(1), 75-81.
[23] Malhotra, S.; Bailey, D.G.; Paine, M.F. and Watkins, P.B. Seville orange juice-felodipine
interaction: comparison with dilute grapefruit juice and involvement of furocoumarins (2001) Clin.
Pharmacol. Ther.
, 69(1), 14-23.
[24] Paine, M.F.; Widmer, W.W.; Hart, H.L.; Pusek, S.N.; Beavers, K.L.; Criss, A.B.; Brown, S.S.;
Thomas, B.F. and Watkins, P.B. A furanocoumarin-free grapefruit juice establishes furanocoumarins as
the mediators of the grapefruit juice-felodipine interaction (2006) Am. J. Clin. Nutr., 83(5), 1097-1105.
[25] Lundahl, J.; Regardh, C.G.; Edgar, B. and Johnsson, G. Effects of grapefruit juice ingestion--
pharmacokinetics and haemodynamics of intravenously and orally administered felodipine in healthy
men (1997) Eur. J. Clin. Pharmacol., 52(2), 139-145.
[26] Soons, P.A.; Vogels, B.A.; Roosemalen, M.C.; Schoemaker, H.C.; Uchida, E.; Edgar, B.; Lundahl,
J.; Cohen, A.F. and Breimer, D.D. Grapefruit juice and cimetidine inhibit stereoselective metabolism of
nitrendipine in humans (1991) Clin. Pharmacol. Ther., 50(4), 394-403.
[27] Edsbacker, S. and Andersson, T. Pharmacokinetics of budesonide (Entocort EC) capsules for
Crohn's disease (2004) Clin. Pharmacokinet., 43(12), 803-821.
[28] Desta, Z.; Kivisto, K.T.; Lilja, J.J.; Backman, J.T.; Soukhova, N.; Neuvonen, P.J. and Flockhart,
D.A. Stereoselective pharmacokinetics of cisapride in healthy volunteers and the effect of repeated
administration of grapefruit juice (2001) Br. J. Clin. Pharmacol., 52(4), 399-407.
[29] Gross, A.S.; Goh, Y.D.; Addison, R.S. and Shenfield, G.M. Influence of grapefruit juice on
cisapride pharmacokinetics (1999) Clin. Pharmacol. Ther., 65(4), 395-401.
[30] Kivisto, K.T.; Lilja, J.J.; Backman, J.T. and Neuvonen, P.J. Repeated consumption of grapefruit
juice considerably increases plasma concentrations of cisapride (1999) Clin. Pharmacol. Ther., 66(5),
448-453.
[31] Offman, E.M.; Freeman, D.J.; Dresser, G.K.; Munoz, C.; Bend, J.R. and Bailey, D.G. Red wine-
cisapride interaction: comparison with grapefruit juice (2001) Clin. Pharmacol. Ther., 70(1), 17-23.
[32] Kupferschmidt, H.H.; Fattinger, K.E.; Ha, H.R.; Follath, F. and Krahenbuhl, S. Grapefruit juice
enhances the bioavailability of the HIV protease inhibitor saquinavir in man (1998) Br. J. Clin.
Pharmacol.
, 45(4), 355-359.
[33] Fuhr, U. Drug interactions with grapefruit juice. Extent, probable mechanism and clinical
relevance (1998) Drug Saf., 18(4), 251-272.
[34] Ando, H.; Tsuruoka, S.; Yanagihara, H.; Sugimoto, K.; Miyata, M.; Yamazoe, Y.; Takamura, T.;
Kaneko, S. and Fujimura, A. Effects of grapefruit juice on the pharmacokinetics of pitavastatin and
atorvastatin (2005) Br. J. Clin. Pharmacol., 60(5), 494-497.
[35] Fukazawa, I.; Uchida, N.; Uchida, E. and Yasuhara, H. Effects of grapefruit juice on
pharmacokinetics of atorvastatin and pravastatin in Japanese (2004) Br. J. Clin. Pharmacol., 57(4),
448-455.
[36] Lilja, J.J.; Kivisto, K.T. and Neuvonen, P.J. Grapefruit juice increases serum concentrations of
atorvastatin and has no effect on pravastatin (1999) Clin. Pharmacol. Ther., 66(2), 118-127.
[37] Galetin, A.; Gertz, M. and Houston, J.B. Potential role of intestinal first-pass metabolism in the
prediction of drug-drug interactions (2008) Expert Opin. Drug Metab. Toxicol., 4(7), 1-14.
[38] Farkas, D.; Oleson, L.E.; Zhao, Y.; Harmatz, J.S.; Zinny, M.A.; Court, M.H. and Greenblatt, D.J.
Pomegranate juice does not impair clearance of oral or intravenous midazolam, a probe for cytochrome
P450-3A activity: comparison with grapefruit juice (2007) J. Clin. Pharmacol., 47(3), 286-294.
[39] Greenblatt, D.J.; von Moltke, L.L.; Harmatz, J.S.; Chen, G.; Weemhoff, J.L.; Jen, C.; Kelley, C.J.;
LeDuc, B.W. and Zinny, M.A. Time course of recovery of cytochrome p450 3A function after single
doses of grapefruit juice (2003) Clin. Pharmacol. Ther., 74(2), 121-129.
[40] Kharasch, E.D.; Walker, A.; Hoffer, C. and Sheffels, P. Intravenous and oral alfentanil as in vivo
probes for hepatic and first-pass cytochrome P450 3A activity: noninvasive assessment by use of
pupillary miosis (2004) Clin. Pharmacol. Ther., 76(5), 452-466.
[41] Kupferschmidt, H.H.; Ha, H.R.; Ziegler, W.H.; Meier, P.J. and Krahenbuhl, S. Interaction between
grapefruit juice and midazolam in humans (1995) Clin. Pharmacol. Ther., 58(1), 20-28.
[42] Rogers, J.D.; Zhao, J.; Liu, L.; Amin, R.D.; Gagliano, K.D.; Porras, A.G.; Blum, R.A.; Wilson,
M.F.; Stepanavage, M. and Vega, J.M. Grapefruit juice has minimal effects on plasma concentrations
of lovastatin-derived 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (1999) Clin.
Pharmacol. Ther.
, 66(4), 358-366.
[43] Veronese, M.L.; Gillen, L.P.; Burke, J.P.; Dorval, E.P.; Hauck, W.W.; Pequignot, E.; Waldman,
S.A. and Greenberg, H.E. Exposure-dependent inhibition of intestinal and hepatic CYP3A4 in vivo by
grapefruit juice (2003) J. Clin. Pharmacol., 43(8), 831-839.
[44] Castro, N.; Jung, H.; Medina, R.; Gonzalez-Esquivel, D.; Lopez, M. and Sotelo, J. Interaction
between grapefruit juice and praziquantel in humans (2002) Antimicrob Agents Chemother, 46(5),
1614-1616.
[45] Varis, T.; Kivisto, K.T. and Neuvonen, P.J. Grapefruit juice can increase the plasma
concentrations of oral methylprednisolone (2000) Eur. J. Clin. Pharmacol., 56(6-7), 489-493.
[46] Rashid, J.; McKinstry, C.; Renwick, A.G.; Dirnhuber, M.; Waller, D.G. and George, C.F.
Quercetin, an in vitro inhibitor of CYP3A, does not contribute to the interaction between nifedipine and
grapefruit juice (1993) Br. J. Clin. Pharmacol., 36(5), 460-463.
[47] Rashid, T.J.; Martin, U.; Clarke, H.; Waller, D.G.; Renwick, A.G. and George, C.F. Factors
affecting the absolute bioavailability of nifedipine (1995) Br. J. Clin. Pharmacol., 40(1), 51-58.
[48] Sigusch, H.; Hippius, M.; Henschel, L.; Kaufmann, K. and Hoffmann, A. Influence of grapefruit
juice on the pharmacokinetics of a slow release nifedipine formulation (1994) Pharmazie, 49(7), 522-
524.
[49] Uno, T.; Ohkubo, T.; Sugawara, K.; Higashiyama, A.; Motomura, S. and Ishizaki, T. Effects of
grapefruit juice on the stereoselective disposition of nicardipine in humans: evidence for dominant
presystemic elimination at the gut site (2000) Eur. J. Clin. Pharmacol., 56(9-10), 643-9.
[50] Culm-Merdek, K.E.; von Moltke, L.L.; Gan, L.; Horan, K.A.; Reynolds, R.; Harmatz, J.S.; Court,
M.H. and Greenblatt, D.J. Effect of extended exposure to grapefruit juice on cytochrome P450 3A
activity in humans: comparison with ritonavir (2006) Clin. Pharmacol. Ther., 79(3), 243-254.
[51] Hukkinen, S.K.; Varhe, A.; Olkkola, K.T. and Neuvonen, P.J. Plasma concentrations of triazolam
are increased by concomitant ingestion of grapefruit juice (1995) Clin. Pharmacol. Ther., 58(2), 127-
131.
[52] Lilja, J.J.; Kivisto, K.T.; Backman, J.T. and Neuvonen, P.J. Effect of grapefruit juice dose on
grapefruit juice-triazolam interaction: repeated consumption prolongs triazolam half-life (2000) Eur. J.
Clin. Pharmacol.
, 56(5), 411-415.
[53] Sugimoto, K.; Araki, N.; Ohmori, M.; Harada, K.; Cui, Y.; Tsuruoka, S.; Kawaguchi, A. and
Fujimura, A. Interaction between grapefruit juice and hypnotic drugs: comparison of triazolam and
quazepam (2006) Eur. J. Clin. Pharmacol., 62(3), 209-215.
[54] Ohnishi, A.; Ohtani, H. and Sawada, Y. Major determinant factors of the extent of interaction
between grapefruit juice and calcium channel antagonists (2006) Br. J. Clin. Pharmacol., 62(2), 196-
199.
[55] Fuhr, U.; Maier-Bruggemann, A.; Blume, H.; Muck, W.; Unger, S.; Kuhlmann, J.; Huschka, C.;
Zaigler, M.; Rietbrock, S. and Staib, A.H. Grapefruit juice increases oral nimodipine bioavailability
(1998) Int. J. Clin. Pharmacol. Ther., 36(3), 126-132.
[56] Kanazawa, S.; Ohkubo, T. and Sugawara, K. The effects of grapefruit juice on the
pharmacokinetics of erythromycin (2001) Eur. J. Clin. Pharmacol., 56(11), 799-803.
[57] Libersa, C.C.; Brique, S.A.; Motte, K.B.; Caron, J.F.; Guedon-Moreau, L.M.; Humbert, L.;
Vincent, A.; Devos, P. and Lhermitte, M.A. Dramatic inhibition of amiodarone metabolism induced by
grapefruit juice (2000) Br. J. Clin. Pharmacol., 49(4), 373-378.
[58] Hollander, A.A.; van Rooij, J.; Lentjes, G.W.; Arbouw, F.; van Bree, J.B.; Schoemaker, R.C.; van
Es, L.A.; van der Woude, F.J. and Cohen, A.F. The effect of grapefruit juice on cyclosporine and
prednisone metabolism in transplant patients (1995) Clin. Pharmacol. Ther., 57(3), 318-324.
[59] Edwards, D.J.; Fitzsimmons, M.E.; Schuetz, E.G.; Yasuda, K.; Ducharme, M.P.; Warbasse, L.H.;
Woster, P.M.; Schuetz, J.D. and Watkins, P. 6',7'-Dihydroxybergamottin in grapefruit juice and Seville
orange juice: effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein (1999) Clin.
Pharmacol. Ther.
, 65(3), 237-244.
[60] Ku, Y.M.; Min, D.I. and Flanigan, M. Effect of grapefruit juice on the pharmacokinetics of
microemulsion cyclosporine and its metabolite in healthy volunteers: does the formulation difference
matter? (1998) J. Clin. Pharmacol., 38(10), 959-965.
[61] Lee, M.; Min, D.I.; Ku, Y.M. and Flanigan, M. Effect of grapefruit juice on pharmacokinetics of
microemulsion cyclosporine in African American subjects compared with Caucasian subjects: does
ethnic difference matter? (2001) J. Clin. Pharmacol., 41(3), 317-323.
[62] Schwarz, U.I.; Johnston, P.E.; Bailey, D.G.; Kim, R.B.; Mayo, G. and Milstone, A. Impact of
citrus soft drinks relative to grapefruit juice on ciclosporin disposition (2006) Br. J. Clin. Pharmacol.,
62(4), 485-491.
[63] Yee, G.C.; Stanley, D.L.; Pessa, L.J.; Dalla Costa, T.; Beltz, S.E.; Ruiz, J. and Lowenthal, D.T.
Effect of grapefruit juice on blood cyclosporin concentration (1995) Lancet., 345(8955), 955-956.
[64] Ducharme, M.P.; Warbasse, L.H. and Edwards, D.J. Disposition of intravenous and oral
cyclosporine after administration with grapefruit juice (1995) Clin. Pharmacol. Ther., 57(5), 485-491.
[65] Garg, S.K.; Kumar, N.; Bhargava, V.K. and Prabhakar, S.K. Effect of grapefruit juice on
carbamazepine bioavailability in patients with epilepsy (1998) Clin. Pharmacol. Ther., 64(3), 286-288.
[66] Ho, P.C.; Ghose, K.; Saville, D. and Wanwimolruk, S. Effect of grapefruit juice on
pharmacokinetics and pharmacodynamics of verapamil enantiomers in healthy volunteers (2000) Eur.
J. Clin. Pharmacol.
, 56(9-10), 693-698.
[67] Fuhr, U.; Muller-Peltzer, H.; Kern, R.; Lopez-Rojas, P.; Junemann, M.; Harder, S. and Staib, A.H.
Effects of grapefruit juice and smoking on verapamil concentrations in steady state (2002) Eur. J. Clin.
Pharmacol.
, 58(1), 45-53.
[68] Lee, M. and Min, D.I. Determination of sildenafil citrate in plasma by high-performance liquid
chromatography and a case for the potential interaction of grapefruit juice with sildenafil citrate (2001)
Ther. Drug. Monit., 23(1), 21-26.
[69] Nichols, D.J.; Muirhead, G.J. and Harness, J.A. Pharmacokinetics of sildenafil after single oral
doses in healthy male subjects: absolute bioavailability, food effects and dose proportionality (2002)
Br. J. Clin. Pharmacol., 53 (Suppl 1), 5S-12S.
[70] Jetter, A.; Kinzig-Schippers, M.; Walchner-Bonjean, M.; Hering, U.; Bulitta, J.; Schreiner, P.;
Sorgel, F. and Fuhr, U. Effects of grapefruit juice on the pharmacokinetics of sildenafil (2002) Clin.
Pharmacol. Ther.
, 71(1), 21-29.
[71] Kharasch, E.D.; Hoffer, C.; Whittington, D. and Sheffels, P. Role of hepatic and intestinal
cytochrome P450 3A and 2B6 in the metabolism, disposition, and miotic effects of methadone (2004)
Clin. Pharmacol. Ther., 76(3), 250-269.
[72] Benmebarek, M.; Devaud, C.; Gex-Fabry, M.; Powell Golay, K.; Brogli, C.; Baumann, P.;
Gravier, B. and Eap, C.B. Effects of grapefruit juice on the pharmacokinetics of the enantiomers of
methadone (2004) Clin. Pharmacol. Ther., 76(1), 55-63.
[73] Yasui, N.; Kondo, T.; Furukori, H.; Kaneko, S.; Ohkubo, T.; Uno, T.; Osanai, T.; Sugawara, K.
and Otani, K. Effects of repeated ingestion of grapefruit juice on the single and multiple oral-dose
pharmacokinetics and pharmacodynamics of alprazolam (2000) Psychopharmacology (Berl), 150(2),
185-190.
[74] Bidstrup, T.B.; Damkier, P.; Olsen, A.K.; Ekblom, M.; Karlsson, A. and Brosen, K. The impact of
CYP2C8 polymorphism and grapefruit juice on the pharmacokinetics of repaglinide (2006) Br. J. Clin.
Pharmacol.
, 61(1), 49-57.
[75] Min, D.I.; Ku, Y.M.; Geraets, D.R. and Lee, H. Effect of grapefruit juice on the pharmacokinetics
and pharmacodynamics of quinidine in healthy volunteers (1996) J. Clin. Pharmacol., 36(5), 469-476.
[76] Damkier, P.; Hansen, L.L. and Brosen, K. Effect of diclofenac, disulfiram, itraconazole, grapefruit
juice and erythromycin on the pharmacokinetics of quinidine (1999) Br. J. Clin. Pharmacol., 48(6),
829-838.

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