Grapefruit-drug interactions

Drugs

Volumn 70, Issue 18, 2010, Pages 2373-2407

  Seden, Kay ^a,b,c   Dickinson, Laura ^a,b   Khoo, Saye ^b   Back, David ^b  

^a ROYAL LIVERPOOL AND BROADGREEN UNIVERSITY HOSPITALS NHS TRUST   (United Kingdom)

^b UNIVERSITY OF LIVERPOOL   (United Kingdom)

^c ROYAL LIVERPOOL UNIVERSITY HOSPITAL   (United Kingdom)

Author keywords

Aliskiren; Amiodarone; Amlodipine; Artemether; Atorvastatin; Budesonide; Buspirone; Carbamazepine; Ciclosporin; Cisapride; Citrus paradisi; Darifenacin; Dasatinib; Dronedarone; Drug interactions; Erlotinib; Felodipine; Fexofenadine; Grapefruit seed extract; Imatinib; Isradipine; Ivabradine; Lacidipine; Lapatinib; Lercanidipine; Lovastatin; Midazolam; Nicardipine; Nifedipine; Nilotinib; Nimodipine; Nisoldipine; Oxycodone; Pimozide; Primaquine; Propafenone; Ranolazine; Research and development; Sildenafil; Simvastatin; Sirolimus; Sunitinib; Tacrolimus; Tadalafil; Temsirolimus; Triazolam; Vardenafil; Verapamil

Indexed keywords

6' 7' DIHYDROXYBERGAMOTTIN; ALISKIREN; AMLODIPINE; ARTEMETHER; ATORVASTATIN; AURANTIIN; BERGAMOTTIN; CLOMIPRAMINE; CLOZAPINE; CYCLOSPORIN A; CYTOCHROME P450 3A4; DIGOXIN; FELODIPINE; FEXOFENADINE; GLIBENCLAMIDE; GLYCOPROTEIN P; GRAPEFRUIT EXTRACT; ISRADIPINE; LANSOPRAZOLE; LERCANIDIPINE; MEVINOLIN; MIDAZOLAM; NILOTINIB; NISOLDIPINE; OMEPRAZOLE; OXYCODONE; PRIMAQUINE; TRIAZOLAM; UNCLASSIFIED DRUG; UNINDEXED DRUG; VERAPAMIL;

DROWSINESS; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG MECHANISM; ENZYME ACTIVITY; ENZYME INACTIVATION; GASTROINTESTINAL ABSORPTION; GRAPEFRUIT JUICE; HUMAN; MYALGIA; MYOPATHY; MYOSITIS; PSYCHOMOTOR DISORDER; REVIEW; RHABDOMYOLYSIS; SINGLE DRUG DOSE;

ANIMALS; BEVERAGES; BIOLOGICAL AVAILABILITY; CITRUS PARADISI; CYTOCHROME P-450 ENZYME SYSTEM; FOOD-DRUG INTERACTIONS; HUMANS; PHARMACEUTICAL PREPARATIONS;

CITRUS X PARADISI;

EID: 78649925436     PISSN: 00126667     EISSN: 11791950     Source Type: Journal    
DOI: 10.2165/11585250-000000000-00000     Document Type: Review

References (275)

1. Mertens-Talcott SU, Zadezensky I, De Castro WV, et al. Grapefruit-drug interactions: can interactions with drugs be avoided? J Clin Pharmacol 2006 Dec; 46 (12): 1390-416.
2. Gmitter Jr FG. Origin, evolution and breeding of the grapefruit. Plant Breed Rev 1995; 13: 345-63.
3. Nicolosi E, Deng ZN, Gentile A, et al. Citrus phylogeny and genetic origin of important species as investigated by molecular markers. Theor Appl Genet 2000; 100 (8): 1155-66.
4. Moore GA. Oranges and lemons: clues to the taxonomy of Citrus from molecular markers. Trends Genet 2001 Sep; 17 (9): 536-40.
5. Bailey DG, Spence JD, Edgar B, et al. Ethanol enhances the hemodynamic effects of felodipine. Clin Invest Med 1989 Dec; 12 (6): 357-62.
6. Bailey DG, Dresser GK. Interactions between grapefruit juice and cardiovascular drugs. Am J Cardiovasc Drugs 2004; 4 (5): 281-97.
7. Neuvonen PJ, Backman JT, Niemi M. Pharmacokinetic comparison of the potential over-the-counter statins sim-vastatin, lovastatin, fluvastatin and pravastatin. Clin Pharmacokinet 2008; 47 (7): 463-74.
8. Sica DA. Interaction of grapefruit juice and calcium channel blockers. Am J Hypertens 2006 Jul; 19 (7): 768-73.
9. Hukkinen SK, Varhe A, Olkkola KT, et al. Plasma con- centrations of triazolam are increased by concomitant ingestion of grapefruit juice. Clin Pharmacol Ther 1995 Aug; 58 (2): 127-31.
10. Kupferschmidt HH, Ha HR, Ziegler WH, et al. Interaction between grapefruit juice and midazolam in humans. Clin Pharmacol Ther 1995 Jul; 58 (1): 20-8.
11. Ozdemir M, Aktan Y, Boydag BS, et al. Interaction be- tween grapefruit juice and diazepam in humans. Eur J Drug Metab Pharmacokinet 1998 Jan-Mar; 23 (1): 55-9.
12. Benton RE, Honig PK, Zamani K, et al. Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram. Clin Pharmacol Ther 1996 Apr; 59 (4): 383-8.
13. Clifford CP, Adams DA, Murray S, et al. The cardiac ef- fects of terfenadine after inhibition of its metabolism by grapefruit juice. Eur J Clin Pharmacol 1997; 52 (4): 311-5.
14. Honig PK, Wortham DC, Lazarev A, et al. Grapefruit juice alters the systemic bioavailability and cardiac repolariza-tion of terfenadine in poor metabolizers of terfenadine. J Clin Pharmacol 1996 Apr; 36 (4): 345-51.
15. Rau SE, Bend JR, Arnold MO, et al. Grapefruit juice- terfenadine single-dose interaction: magnitude, mechanism, and relevance. Clin Pharmacol Ther 1997 Apr; 61 (4): 401-9.
16. Ducharme MP, Warbasse LH, Edwards DJ. Disposition of intravenous and oral cyclosporine after administration with grapefruit juice. Clin Pharmacol Ther 1995 May; 57 (5): 485-91.
17. Hollander AA, van Rooij J, Lentjes GW, et al. The effect of grapefruit juice oncyclosporine and prednisone metabolism in transplant patients. Clin Pharmacol Ther 1995 Mar; 57 (3): 318-24.
18. Min DI, Ku YM, Perry PJ, et al. Effect of grapefruit juice on cyclosporine pharmacokinetics in renal transplant patients. Transplantation 1996 Jul 15; 62 (1): 123-5.
19. Yee GC, Stanley DL, Pessa LJ, et al. Effect of grapefruit juice on blood cyclosporin concentration. Lancet 1995 Apr 15; 345 (8955): 955-6.
20. Goosen TC, Cillie D, Bailey DG, et al. Bergamottin con- tribution to the grapefruit juice-felodipine interaction and disposition in humans. Clin Pharmacol Ther 2004 Dec; 76 (6): 607-17.
21. He K, Iyer KR, Hayes RN, et al. Inactivation of cyto- chrome P450 3A4 by bergamottin, a component of grapefruit juice. Chem Res Toxicol 1998 Apr; 11 (4): 252-9.
22. 0-dihydroxybergamottin, a cytochrome P450 inhibitor, in grapefruit juice. Drug Metab Dispos 1996 Dec; 24 (12): 1287-90.
23. Schmiedlin-Ren P, Edwards DJ, Fitzsimmons ME, et al. Mechanisms of enhanced oral availability of CYP3A4 substrates by grapefruit constituents: decreased en-terocyte CYP3A4 concentration and mechanism-based inactivation by furanocoumarins. Drug Metab Dispos 1997 Nov; 25 (11): 1228-33.
24. Fukuda K, Ohta T, Oshima Y, et al. Specific CYP3A4 in- hibitors in grapefruit juice: furocoumarin dimers as components of drug interaction. Pharmacogenetics 1997 Oct; 7 (5): 391-6.
25. Guo LQ, Fukuda K, Ohta T, et al. Role of furanocoumarin derivatives on grapefruit juice-mediated inhibition of human CYP3A activity. Drug Metab Dispos 2000 Jul; 28 (7): 766-71.
26. Lilja JJ, Kivisto KT, Backman JT, et al. Effect of grape- fruit juice dose on grapefruit juice-triazolam interaction: repeated consumption prolongs triazolam half-life. Eur J Clin Pharmacol 2000 Aug; 56 (5): 411-5.
27. Lilja JJ, Kivisto KT, Neuvonen PJ. Grapefruit juice in- creases serum concentrations of atorvastatin and has no effect on pravastatin. Clin Pharmacol Ther 1999 Aug; 66 (2): 118-27.
28. Nieminen TH, Hagelberg NM, Saari TI, et al. Grapefruit juice enhances the exposure to oral oxycodone. Basic Clin Pharmacol Toxicol 2010 Oct; 107 (4): 782-8.
29. Bailey DG, Spence JD, Munoz C, et al. Interaction of citrus juices with felodipine and nifedipine. Lancet 1991 Feb 2; 337 (8736): 268-9.
30. Lundahl J, Regardh CG, Edgar B, et al. Effects of grapefruit juice ingestion-pharmacokinetics and haemo-dynamics of intravenously and orally administered felo-dipine in healthy men. Eur J Clin Pharmacol 1997; 52 (2): 139-45.
31. Lown KS, Bailey DG, Fontana RJ, et al. Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. J Clin Invest 1997 May 15; 99 (10): 2545-53.
32. Lundahl J, Regardh CG, Edgar B, et al. Relationship be- tween time of intake of grapefruit juice and its effect on pharmacokinetics and pharmacodynamics of felodipine in healthy subjects. Eur J Clin Pharmacol 1995; 49 (1-2): 61-7.
33. Lin JH, Lu AY. Interindividual variability in inhibition and induction of cytochrome P450 enzymes. Annu Rev Pharmacol Toxicol 2001; 41: 535-67.
34. Paine MF, Khalighi M, Fisher JM, et al. Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 1997 Dec; 283 (3): 1552-62.
35. Bailey DG, Arnold JM, Munoz C, et al. Grapefruit juice - felodipine interaction: mechanism, predictability, and effect of naringin. Clin Pharmacol Ther 1993 Jun; 53 (6): 637-42.
36. Bailey DG, Arnold JM, Strong HA, et al. Effect of grape- fruit juice and naringin on nisoldipine pharmacokinetics. Clin Pharmacol Ther 1993 Dec; 54 (6): 589-94.
37. Bailey DG, Dresser GK, Kreeft JH, et al. Grapefruit- felodipine interaction: effect of unprocessed fruit and probable active ingredients. Clin Pharmacol Ther 2000 Nov; 68 (5): 468-77.
38. Paine MF, Criss AB, Watkins PB. Two major grapefruit juice components differ in intestinal CYP3A4 inhibition kinetic and binding properties. Drug Metab Dispos 2004 Oct; 32 (10): 1146-53.
39. Paine MF, Criss AB, Watkins PB. Two major grapefruit juice components differ in time to onset of intestinal CYP3A4 inhibition. J Pharmacol Exp Ther 2005 Mar; 312 (3): 1151-60.
40. 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 May; 83 (5): 1097-105.
41. Girennavar B, Jayaprakasha GK, Patil BS. Potent inhibi- tion of human cytochrome P450 3A4, 2D6, and 2C9 iso-enzymes by grapefruit juice and its furocoumarins. J Food Sci 2007 Oct; 72 (8): C417-21.
42. Tassaneeyakul W, Guo LQ, Fukuda K, et al. Inhibition selectivity of grapefruit juice components on human cy-tochromes P450. Arch Biochem Biophys 2000 Jun 15; 378 (2): 356-63.
43. Fuhr U, Klittich K, Staib AH. Inhibitory effect of grape- fruit juice and its bitter principal, naringenin, on CYP1A2 dependent metabolism of caffeine in man. Br J Clin Pharmacol 1993 Apr; 35 (4): 431-6.
44. Lin HL, Kent UM, Hollenberg PF. The grapefruit juice effect is not limited to cytochrome P450 (P450) 3A4: evidence for bergamottin-dependent inactivation, heme destruction, and covalent binding to protein in P450s 2B6 and 3A5. J Pharmacol Exp Ther 2005 Apr; 313 (1): 154-64.
45. Baumgart A, Schmidt M, Schmitz HJ, et al. Natural fur- ocoumarins as inducers and inhibitors of cytochrome P450 1A1 in rat hepatocytes. Biochem Pharmacol 2005 Feb 15; 69 (4): 657-67.
46. Tassaneeyakul W, Vannaprasaht S, Yamazoe Y. Formation of omeprazole sulphone but not 5-hydroxyomeprazole is inhibited by grapefruit juice. Br J Clin Pharmacol 2000 Feb; 49 (2): 139-44.
47. Uno T, Yasui-Furukori N, Takahata T, et al. Lack of sig- nificant effect of grapefruit juice on the pharmacokinetics of lansoprazole and its metabolites in subjects with different CYP2C19 genotypes. J Clin Pharmacol 2005 Jun; 45 (6): 690-4.
48. Lane HY, Jann MW, Chang YC, et al. Repeated ingestion of grapefruit juice does not alter clozapine's steady-state plasma levels, effectiveness, and tolerability. J Clin Psychiatry 2001 Oct; 62 (10): 812-7.
49. Fuhr U, Maier A, Keller A, et al. Lacking effect of grape- fruit juice on theophylline pharmacokinetics. Int J Clin Pharmacol Ther 1995 Jun; 33 (6): 311-4.
50. Oesterheld J, Kallepalli BR. Grapefruit juice and clomi- pramine: shifting metabolitic ratios. J Clin Psycho-pharmacol 1997 Feb; 17 (1): 62-3.
51. Sullivan DM, Ford MA, Boyden TW. Grapefruit juice and the response to warfarin. Am J Health Syst Pharm 1998 Aug 1; 55 (15): 1581-3.
52. Takanaga H, Ohnishi A, Matsuo H, et al. Inhibition of vinblastine efflux mediated by P-glycoprotein by grapefruit juice components in caco-2 cells. Biol Pharm Bull 1998 Oct; 21 (10): 1062-6.
53. Ikegawa T, Ushigome F, Koyabu N, et al. Inhibition of P-glycoprotein by orange juice components, polymethoxy-flavones in adriamycin-resistant human myelogenous leukemia (K562/ADM) cells. Cancer Lett 2000 Nov 10; 160 (1): 21-8.
54. Edwards DJ, Bernier SM. Naringin and naringenin are not the primary CYP3A inhibitors in grapefruit juice. Life Sci 1996; 59 (13): 1025-30.
55. Takanaga H, Ohnishi A, Yamada S, et al. Poly- methoxylated flavones in orange juice are inhibitors of P-glycoprotein but not cytochrome P450 3A4. J Pharmacol Exp Ther 2000 Apr; 293 (1): 230-6.
56. Honda Y, Ushigome F, Koyabu N, et al. Effects of grape- fruit juice and orange juice components on P-glycoprotein-and MRP2-mediated drug efflux. Br J Pharmacol 2004 Dec; 143 (7): 856-64.
57. De Castro WV, Mertens-Talcott S, Derendorf H, et al. Grapefruit juice-drug interactions: Grapefruit juice and its components inhibit P-glycoprotein (ABCB1) mediated transport of talinolol in Caco-2 cells. J Pharm Sci 2007 Oct; 96 (10): 2808-17.
58. Dahan A, Amidon GL. Grapefruit juice and its con- stituents augment colchicine intestinal absorption: potential hazardous interaction and the role of p-glycoprotein. Pharm Res 2009 Apr; 26 (4): 883-92.
59. Becquemont L, Verstuyft C, Kerb R, et al. Effect of grapefruit juice on digoxin pharmacokinetics in humans. Clin Pharmacol Ther 2001 Oct; 70 (4): 311-6.
60. Dresser GK, Bailey DG, Leake BF, et al. Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. Clin Pharmacol Ther 2002 Jan; 71 (1): 11-20.
61. Glaeser H, Bailey DG, Dresser GK, et al. Intestinal drug transporter expression and the impact of grapefruit juice in humans. Clin Pharmacol Ther 2007 Mar; 81 (3): 362-70.
62. Satoh H, Yamashita F, Tsujimoto M, et al. Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B. Drug Metab Dispos 2005 Apr; 33 (4): 518-23.
63. Lilja JJ, Niemi M, Fredrikson H, et al. Effects of clari- thromycin and grapefruit juice on the pharmacokinetics of glibenclamide. Br J Clin Pharmacol 2007 Jun; 63 (6): 732-40.
64. Lilja JJ, Backman JT, Laitila J, et al. Itraconazole increases but grapefruit juice greatly decreases plasma concentrations of celiprolol. Clin Pharmacol Ther 2003 Mar; 73 (3): 192-8.
65. Schwarz UI, Seemann D, Oertel R, et al. Grapefruit juice ingestion significantly reduces talinolol bioavailability. Clin Pharmacol Ther 2005 Apr; 77 (4): 291-301.
66. Kato Y, Miyazaki T, Kano T, et al. Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol. J Pharm Sci 2009 Jul; 98 (7): 2529-39.
67. Shirasaka Y, Kuraoka E, Spahn-Langguth H, et al. Species difference in the effect of grapefruit juice on intestinal absorption of talinolol between human and rat. J Pharmacol Exp Ther 2010 Jan; 332 (1): 181-9.
68. Tapaninen T, Neuvonen PJ, Niemi M. Grapefruit juice greatly reduces the plasma concentrations of the OATP2B1 and CYP3A4 substrate aliskiren. Clin Pharmacol Ther 2010 Sep; 88 (3): 339-42.
69. Bailey DG, Dresser GK, Leake BF, et al. Naringin is a major and selective clinical inhibitor of organic anion-transporting polypeptide 1A2 (OATP1A2) in grapefruit juice. Clin Pharmacol Ther 2007 Apr; 81 (4): 495-502.
70. Nishimuta H, Ohtani H, Tsujimoto M, et al. Inhibitory effects of various beverages on human recombinant sulfotransferase isoforms SULT1A1 and SULT1A3. Biopharm Drug Dispos 2007 Dec; 28 (9): 491-500.
71. Li P, Callery PS, Gan LS, et al. Esterase inhibition attribute of grapefruit juice leading to a new drug interaction. Drug Metab Dispos 2007 Jul; 35 (7): 1023-31.
72. Dresser GK, Kim RB, Bailey DG. Effect of grapefruit juice volume on the reduction of fexofenadine bioavailability: possible role of organic anion transporting polypeptides. Clin Pharmacol Ther 2005 Mar; 77 (3): 170-7.
73. De Castro WV, Mertens-Talcott S, Rubner A, et al. Var- iation of flavonoids and furanocoumarins in grapefruit juices: a potential source of variability in grapefruit juice-drug interaction studies. J Agric Food Chem 2006 Jan 11; 54 (1): 249-55.
74. Garg SK, Kumar N, Bhargava VK, et al. Effect of grape- fruit juice on carbamazepine bioavailability in patients with epilepsy. Clin Pharmacol Ther 1998 Sep; 64(3): 286-8.
75. Tegretol Retard (carbamazepine 200mg, 400mg tablets): summary of product characterisitics. Novartis Pharmaceuticals UK Ltd. Updated 09/12/2009 [online]. Available from URL: http://www.medicines.org.uk/emc/medicine/ 1330 [Accessed 2010 Feb 1].
76. Tegretol® (carbamazepine) tablets, suspension: US pre- scribing information. Novartis Pharmaceutical corp. Revised February, 2009 [online]. Available from URL: http:// www.pharma.us.novartis.com/product/pi/pdf/tegretol. pdf [Accessed 2010 Jul 17].
77. Banfield C, Gupta S, Marino M, et al. Grapefruit juice reduces the oral bioavailability of fexofenadine but not desloratadine. Clin Pharmacokinet 2002; 41 (4): 311-8.
78. Telfast (fexofenadine) tablets: summary of product char- acteristics. sanofi-aventis. Updated 06/01/2009 [online]. Available from URL: http://www.medicines.org.uk/EMC/ medicine/6659/SPC/Telfast+120mg+film- coated+tablets/ [Accessed 2010 Jan 3].
79. Allegra (fexofenadine) tablets: US prescribing information. sanofi-aventis US. Updated 07/2007 [online]. Available from URL: http://products.sanofi-aventis.us/allegra/al legra-ODT.pdf [Accessed 2010 Jul 15].
80. van Agtmael MA, Gupta V, van der Graaf CA, et al. The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects. Clin Pharmacol Ther 1999 Oct; 66 (4): 408-14.
81. van Agtmael MA, Gupta V, van der Wosten TH, et al. Grapefruit juice increases the bioavailability of artemether. Eur J Clin Pharmacol 1999 Jul; 55 (5): 405-10.
82. Riamet (artemether/lumefantrine 20/120mg tablets): sum- mary of product characteristics. Novartis Pharmaceuticals UK Ltd. Updated 21/09/2009 [online]. Available from URL: http://www.medicines.org.uk/emc/medicine/9196 [Accessed 2010 Feb 1].
83. Coartem (artemether/lumefantrine) tablets: US prescribing information. Novartis Pharmaceuticals Corp. Updated February 2010 [online]. Available from URL: http:// www.pharma.us.novartis.com/product/pi/pdf/coartem.pdf [Accessed 2010 Jul 16].
84. Cuong BT, Binh VQ, Dai B, et al. Does gender, food or grapefruit juice alter the pharmacokinetics of primaquine in healthy subjects? Br J Clin Pharmacol 2006 Jun; 61 (6): 682-9.
85. Primaquine phosphate tablets, USP: US prescribing in- formation. Sanofi-Synthelabo Inc. Revised April 2003 [online]. Available from URL: http://products.sanofi-aventis.us/primaquine/primaquine.html [Accessed 2010 Jul 17].
86. Orap (pimozide) 4mg tablets: summary of product char- acteristics. Janssen-Cilag Ltd. Updated 15/02/2010 [online]. Available from URL: http://www.medicines.org.uk/ EMC/medicine/6753/SPC/Orap+4+mg+tablets [Accessed 2010 Sep 28].
87. Andersen V, Pedersen N, Larsen NE, et al. Intestinal first pass metabolism of midazolam in liver cirrhosis: effect of grapefruit juice. Br J Clin Pharmacol 2002 Aug; 54 (2): 120-4.
88. Vanakoski J, Mattila MJ, Seppala T. Grapefruit juice does not enhance the effects of midazolam and triazolam in man. Eur J Clin Pharmacol 1996; 50 (6): 501-8.
89. Sugimoto K, Araki N, Ohmori M, et al. Interaction be- tween grapefruit juice and hypnotic drugs: comparison of triazolam and quazepam. Eur J Clin Pharmacol 2006 Mar; 62 (3): 209-15.
90. Halcion® (triazolam) tablets: US prescribing information. Pfizer Inc. Updated 12/2008 [online]. Available from URL: http://media.pfizer.com/files/ products/uspi-halcion. pdf [Accessed 2010 Jul 26].
91. Gammans RE, Mayol RF, Mackenthun AV, et al. The relationship between buspirone bioavailability and dose in healthy subjects. Biopharm Drug Dispos 1985 Apr-Jun; 6 (2): 139-45.
92. Lilja JJ, Kivisto KT, Backman JT, et al. Grapefruit juice substantially increases plasma concentrations of buspirone. Clin Pharmacol Ther 1998 Dec; 64 (6): 655-60.
93. Buspar (buspirone 5mg and 10mg tablets): patient in- formation leaflet. E. R. Squibb & Sons Limited. Updated 10/03/2009 [online]. Available from URL: http://www. medicines.org.uk/emc/medicine/17856 [Accessed 2010 Feb 1].
94. BuSpar® (buspirone hydrochloride tablets USP) tablets: US prescribing information. Bristol-Myers Squibb Company. Revised March 2007 [online]. Available from URL: http://packageinserts.bms.com/pi/pi-buspar.pdf[Accessed 2010 Jul 15].
95. Libersa CC, Brique SA, Motte KB, et al. Dramatic inhibi- tion of amiodarone metabolism induced by grapefruit juice. Br J Clin Pharmacol 2000 Apr; 49 (4): 373-8.
96. Codarone (amiodarone) tablets: summary of product characteristics. sanofi-aventis. Updated 15/07/2010 [online]. Available from URL: http://www.medicines.org.uk/ EMC/medicine/7124/SPC/Cordarone+X+100%2c+Cord arone+X+200 [Accessed 2010 Jul 26].
97. Cordarone® (amiodarone HCl) tablets: US prescribing in- formation. Wyeth Pharmaceuticals Inc. Updated 08/2009 [online]. Available from URL: http://www.wyeth.com/ content/showlabeling.asp?id=93 [Accessed 2010 Jul 26].
98. Arythmol (propafenone 150mg and 300mg tablets): sum- mary of product characteristics. Abbott Laboratories Ltd. Updated 08/01/2010 [online]. Available from URL: http://www.medicines.org.uk/emc/medicine/10622/SPC/ Arythmol/ [Accessed 2010 Feb 1].
99. Rhythmol® (propafenone hydrochloride) tablets: US pre- scribing information. GlaxoSmithKline. October 2009 [online]. Available from URL: http://us.gsk.com/products/ assets/us-rythmol.pdf [Accessed 2010 Jul 17].
100. Multaq (dronedarone) 400mg tablets: summary of product characteristics. Sanofi-Aventis. Updated 31/03/2010 [online]. Available from URL: http://www.medicines.org.uk/ EMC/medicine/22894/SPC/Multaq+400mg+tablets/#table OfContents [Accessed 2010 Sep 28].
101. Multaq (dronedarone) 400mg tablets: US prescribing in- formation. sanofi-aventis. Issued July 2009 [online]. Available from URL: http://products.sanofi-aventis.us/Multaq/ Multaq.pdf [Accessed 2010 Sep 28].
102. Fuhr U, Muller-Peltzer H, Kern R, et al. Effects of grape- fruit juice and smoking on verapamil concentrations in steady state. Eur J Clin Pharmacol 2002 Apr; 58 (1): 45-53.
103. Ho PC, Ghose K, Saville D, et al. Effect of grapefruit juice on pharmacokinetics and pharmacodynamics of verapamil enantiomers in healthy volunteers. Eur J Clin Pharmacol 2000 Dec; 56 (9-10): 693-8.
104. Zaidenstein R, Dishi V, Gips M, et al. The effect of grape- fruit juice on the pharmacokinetics of orally administered verapamil. Eur J Clin Pharmacol 1998 Jun; 54 (4): 337-40.
105. Covera-HS (verapamil hydrochloride) controlled release tablets: US prescribing information. Pfizer Inc. Revised February 2010 [online]. Available from URL: http:// www.pfizer.com/files/products/uspi-covera.pdf [Accessed 2010 Jul 15].
106. Nakagawa K, Goto T. Effects of ingestion of grapefruit juice or grapefruit on the hypotensive effect and plasma concentrations of dihydropyridine calcium antagonists (amlodipine and nifedipine): a case study. Clin Exp Hy-pertens 2010 Jan; 32 (2): 71-5.
107. Josefsson M, Zackrisson AL, Ahlner J. Effect of grapefruit juice on the pharmacokinetics of amlodipine in healthy volunteers. Eur J Clin Pharmacol 1996; 51 (2): 189-93.
108. Vincent J, Harris SI, Foulds G, et al. Lack of effect of grapefruit juice on the pharmacokinetics and pharmacodynamics of amlodipine. Br J Clin Pharmacol 2000 Nov; 50 (5): 455-63.
109. Amlostin (amlodipine maleate) tablets: summary of pro- duct characteristics. Discovery Pharmaceuticals Ltd. Updated 19/02/2010 [online]. Available from URL: http:// www.medicines.org.uk/EMC/medicine/15144/SPC/Amlos tin+10mg/ [Accessed 2010 Jul 22].
110. Norvasc (amlodipine besylate) tablets: US prescribing infor- mation. Pfizer Inc. Revised March 2010 [online]. Available from URL: http://www.pfizer.com/files/products/ uspi-norvasc.pdf [Accessed 2010 Jul 22].
111. Istin (amlodipine besilate) tablets: summary of product characteristics. Pfizer Ltd. Updated 01/04/2010 [online]. Available from URL: http://www.medicines.org.uk/EMC/ medicine/1466/SPC/Istin [Accessed 2010 Jul 22].
112. Bailey DG, Arnold JM, Bend JR, et al. Grapefruit juice- felodipine interaction: reproducibility and characterization with the extended release drug formulation. Br J Clin Pharmacol 1995 Aug; 40 (2): 135-40.
113. 0-dihy- droxybergamottin in humans. Clin Pharmacol Ther 1998 Sep; 64 (3): 248-56.
114. Malhotra S, Bailey DG, Paine MF, et al. Seville orange juice-felodipine interaction: comparison with dilute grapefruit juice and involvement of furocoumarins. Clin Pharmacol Ther 2001 Jan; 69 (1): 14-23.
115. Dresser GK, Bailey DG, Carruthers SG. Grapefruit juice: felodipine interaction in the elderly. Clin Pharmacol Ther 2000 Jul; 68 (1): 28-34.
116. Edgar B, Bailey D, Bergstrand R, et al. 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): 313-7.
117. Uno T, Ohkubo T, Sugawara K, et al. Effects of grapefruit juice on the stereoselective disposition of nicardipine in humans: evidence for dominant presystemic elimination at the gut site. Eur J Clin Pharmacol 2000 Dec; 56 (9-10): 643-9.
118. Cardene SR (nicardipine hydrochloride) sustained release capsules: summary of product characteristics. Astellas Pharma Ltd. Updated 19/04/2010 [online]. Available from URL: http://www.medicines.org.uk/EMC/medicine/2250/ SPC/Cardene+SR+30+and+45mg [Accessed 2010 Jul 22].
119. Fuhr U, Maier-Bruggemann A, Blume H, et al. Grapefruit juice increases oral nimodipine bioavailability. Int J Clin Pharmacol Ther 1998 Mar; 36 (3): 126-32.
120. Nimotop (nimodipine) tablets: summary of product char- acteristics. Bayer Plc. Updated 17/06/2010 [online]. Available from URL: http://www.medicines.org. uk/EMC/medicine/ 8086/SPC/Nimotop+30mg+Tablets [Accessed 2010 Jul 22].
121. Odou P, Ferrari N, Barthelemy C, et al. Grapefruit juice- nifedipine interaction: possible involvement of several mechanisms. J Clin Pharm Ther 2005 Apr; 30 (2): 153-8.
122. Rashid J, McKinstry C, Renwick AG, et al. Quercetin, an in vitro inhibitor of CYP3A, does not contribute to the interaction between nifedipine and grapefruit juice. Br J Clin Pharmacol 1993 Nov; 36 (5): 460-3.
123. Adigun AQ, Mudasiru Z. Clinical effects of grapefruit juice-nifedipine interaction in a 54-year-old Nigerian: a case report. J Natl Med Assoc 2002 Apr; 94 (4): 276-8.
124. Adalat (nifedipine) capsules: summary of product char- acteristics. Bayer Plc. Updated 01/07/2010 [online]. Available from URL: http://www.medicines.org. uk/EMC/ medicine/20901/SPC/Adalat [Accessed 2010 Jul 22].
125. Procardia® (nifedipine) capsules: US prescribing informa- tion. Pfizer Inc. Revised March 2006 [online]. Available from URL: http://www.pfizer.com/files/products/uspi- procardia.pdf [Accessed 2010 Jul 22].
126. Prescal (isradipine) tablets: summary of product char- acteristics. Novartis Pharmaceuticals UK Ltd. Updated 12/12/2007 [online]. Available from URL: http://www. medicines.org.uk/EMC/medicine/1311/SPC/Prescal [Accessed 2010 Jul 26].
127. Motens (lacidipine) tablets: summary of product character- istics. Boehringer Ingelheim Ltd. Updated 24/05/2010 [online]. Available from URL: http://www.medicines.org. uk/EMC/medicine/297/SPC/Motens+Tablets+2mg [Accessed 2010 Jul 26].
128. Lercanidipine tablets: summary of product characteristics. Winthrop Pharmaceuticals UK Ltd. Updated 03/02/2010 [online]. Available from URL: http://www.medicines.org. uk/EMC/medicine/22757/SPC/Lercanidipine+Hydrochlo ride+10+mg+film-coated+tablets/#tableOfContents [Accessed 2010 Jul 26].
129. DYNACIRC CR (isradipine) controlled release tablets: US prescribing information. GlaxoSmithKline. February 2009 [online]. Available from URL: http://us.gsk.com/ products/assets/us-dynacirc-cr.pdf [Accessed 2010 Jul 15].
130. Takanaga H, Ohnishi A, Murakami H, et al. Relationship between time after intake of grapefruit juice and the effect on pharmacokinetics and pharmacodynamics of nisoldi-pine in healthy subjects. Clin Pharmacol Ther 2000 Mar; 67 (3): 201-14.
131. Sular (nisoldipine) extended release tablet: US prescribing information. Shionogi Pharma, Inc. Revised 02/2010 [online]. Available from URL: http://www.sular.com/pdf/ Sular-PI.pdf [Accessed 2010 Jul 17].
132. Fukazawa I, Uchida N, Uchida E, et al. Effects of grape- fruit juice on pharmacokinetics of atorvastatin and pravastatin in Japanese. Br J Clin Pharmacol 2004 Apr; 57 (4): 448-55.
133. Ando H, Tsuruoka S, Yanagihara H, et al. Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin. Br J Clin Pharmacol 2005 Nov; 60 (5): 494-7.
134. Lipitor (atorvastatin calcium) tablets: US prescribing in- formation. Pfizer Inc. Updated 06/2009 [online]. Available from URL: http://www.pfizer.com/ files/products/ uspi-lipitor.pdf [Accessed 2010 Jul 13].
135. Kantola T, Kivisto KT, Neuvonen PJ. Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1998 Apr; 63 (4): 397-402.
136. Mevacor (lovastatin) tablets: US prescribing information. Merck & Co Inc. Issued May 2010 [online]. Available from URL: http://www.merck.com/product/ usa/pi-cir culars/m/mevacor/mevacor-pi.pdf [Accessed 2010 Jul 15].
137. Lilja JJ, Neuvonen M, Neuvonen PJ. Effects of regular consumption of grapefruit juice on the pharmacokinetics of simvastatin. Br J Clin Pharmacol 2004 Jul; 58 (1): 56-60.
138. Lilja JJ, Kivisto KT, Neuvonen PJ. Grapefruit juice- simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. Clin Pharmacol Ther 1998 Nov; 64 (5): 477-83.
139. Lilja JJ, Kivisto KT, Neuvonen PJ. Duration of effect of grapefruit juice on the pharmacokinetics of the CYP3A4 substrate simvastatin. Clin Pharmacol Ther 2000 Oct; 68 (4): 384-90.
140. Dreier JP, Endres M. Statin-associated rhabdomyolysis triggered by grapefruit consumption. Neurology 2004 Feb 24; 62 (4): 670.
141. Zocor Heart-Pro (simvastatin 10mg film coated tablets). McNeil Ltd. Updated 06/11/2009 [online]. Available from URL: http://www.medicines.org.uk/ emc/document.aspx? documentId=20015 [Accessed 2010 Feb 1].
142. Zocor (simvastatin) tablets: US prescribing information. Merck & Co Inc. Issued May 2010 [online]. Available from URL: http://www.merck.com/product/ usa/pi-circulars/z/ zocor/zocor-pi.pdf [Accessed 2010 Jul 13].
143. Procoralan (ivabradine 5mg and 7.5mg film coated tablets): summary of product characteristics. Servier Laboratories Limited. Updated 13/11/2009 [online]. Available from URL: http://www.medicines.org.uk/emc/medicine/17188/ SPC/Procoralan [Accessed 2010 Feb 1].
144. Ranexa (ranolazine 375mg, 500mg and 750mg prolonged- release tablets): summary of product characteristics. A.Menarini Pharma U.K. S.R.L. Updated 10/08/2010 [online]. Available from URL: http://www.medicines.org. uk/emc/document.aspx?documentId=21402 [Accessed 2010 Feb 1].
145. Ranexa (ranolazine) extended release tablets: US prescrib- ing information. Gilead Sciences Inc. Revised 09/2009 [online]. Available from URL: http://www.ranexa.com/ download/RanexaPI.PDF [Accessed 2010 Jul 22].
146. EntocortCR (budesonide) 3mg capsules: summary of pro- duct characteristics. AstraZeneca UK Limited. Updated 26/11/ 2009 [online]. Available from URL: http://www. medicines.org.uk/EMC/medicine/172/SPC/Entocort+CR +3mg+Capsules/#tableOfContents [Accessed 28/09/2010].
147. EntocortEC (budesonide) 3mg capsules. AstraZeneca. Revised 06/ 2009 [online]. Available from URL: http:// www1.astrazeneca-us.com/pi/entocortec.pdf [Accessed 2010 Sep 28].
148. Yin OQ, Gallagher N, Li A, et al. Effect of grapefruit juice on the pharmacokinetics of nilotinib in healthy participants. J Clin Pharmacol 2010 Feb; 50 (2): 188-94.
149. Tasigna (nilotinib) capsules: summary of product char- acteristics. Novartis Pharmaceuticals UK Ltd. Updated 03/03/2010 [online]. Available from URL: http://www. medicines.org.uk/EMC/medicine/20827/SPC/Tasigna+200 +mg+hard+capsules [Accessed 2010 Jul 22].
150. Tasigna (nilotinib) capsules: US prescribing information. Novartis Inc. Updated 06/2010 [online]. Available from URL: http://www.pharma.us.novartis.com/ product/pi/pdf/ tasigna.pdf [Accessed 2010 Jul 22].
151. Tyverb (lapatinib) tablets: summary of product character- istics. GlaxoSmithKline UK. Updated 24/06/2010 [online]. Available from URL: http://www.medicines.org.uk/ EMC/medicine/20929/SPC/Tyverb [Accessed 2010 Jul 22].
152. Tykerb (lapatinib) tablets: summary of product character- istics. GlaxoSmithKline. Revised April 2010 [online]. Available from URL: http://us.gsk.com/products/assets/ us-tykerb.pdf [Accessed 2010 Jul 22].
153. Sutent (sunitinib) capsules: summary of product character- istics. Pfizer Ltd. Updated 09/07/2010 [online]. Available from URL: http://www.medicines.org. uk/EMC/medicine/ 18531/SPC/SUTENT+12.5mg%2c+25mg%2c+37.5mg+and +50mg+Hard+Capsules [Accessed 2010 Jul 22].
154. Sutent (sunitinib maleate) capsules: US prescribing in- formation. Pfizer Inc. Issued July 2010 [online]. Available from URL: http://www.pfizer.com/ files/products/uspi- sutent.pdf [Accessed 2010 Jul 22].
155. Sprycel (dasatinib) tablets: US prescribing information. Bristol-Myers Squibb Company. Updated 06/ 2009 [online]. Available from URL: http://packageinserts.bms. com/pi/pi-sprycel.pdf [Accessed 2010 Jul 22].
156. Tarceva (erlotinib) tablets: US prescribing information. OSI Pharmaceuticals Inc. Revised 04/2010 [online]. Available from URL: http://www.osip.com/pdf/Tarceva-PI- 042010.pdf [Accessed 2010 Jul 22].
157. Gleevec (imatinib mesylate) tablets: US prescribing in- formation. Novartis Inc. Updated 02/2010 [online]. Available from URL: http://www.pharma. us.novartis.com/ product/pi/pdf/gleevec-tabs.pdf [Accessed 2010 Jul 22].
158. Torisel (temsirolimus) IV injection: US prescribing in- formation. Wyeth Pharmaceuticals Inc. Revised 07/2010 [online]. Available from URL: http://www.wyeth.com/ content/showlabeling.asp?id=490 [Accessed 2010 Jul 22].
159. Kivisto KT, Lilja JJ, Backman JT, et al. Repeated con- sumption of grapefruit juice considerably increases plasma concentrations of cisapride. Clin Pharmacol Ther 1999 Nov; 66 (5): 448-53.
160. Propulsid (cisapride) official FDA information. FDA Professional Drug information. Updated 10/ 2009 [online]. Available from URL: http://www.drugs. com/pro/propulsid. html [Accessed 2010 Jul 13].
161. Bistrup C, Nielsen FT, Jeppesen UE, et al. Effect of grapefruit juice on Sandimmun Neoral absorption among stable renal allograft recipients. Nephrol Dial Transplant 2001 Feb; 16 (2): 373-7.
162. Brunner LJ, Pai KS, Munar MY, et al. Effect of grapefruit juice on cyclosporin A pharmacokinetics in pediatric renal transplant patients. Pediatr Transplant 2000 Nov; 4 (4): 313-21.
163. Ducharme MP, Provenzano R, Dehoorne-Smith M, et al. Trough concentrations of cyclosporine in blood following administration with grapefruit juice. Br J Clin Pharmacol 1993 Nov; 36 (5): 457-9.
164. 0 - Dihydroxybergamottin in grapefruit juice and Seville orange juice: effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein. Clin Pharmacol Ther 1999 Mar; 65 (3): 237-44.
165. Ku YM, Min DI, Flanigan M. Effect of grapefruit juice on the pharmacokinetics of microemulsion cyclosporine and its metabolite in healthy volunteers: does the formulation difference matter? J Clin Pharmacol 1998 Oct; 38 (10): 959-65.
166. Lee M, Min DI, Ku YM, et al. Effect of grapefruit juice on pharmacokinetics ofmicroemulsion cyclosporine inAfrican American subjects compared with Caucasian subjects: does ethnic difference matter? J Clin Pharmacol 2001 Mar; 41 (3): 317-23.
167. Mehrsai AR, Pourmand G, Mansour D, et al. Effect of grapefruit juice on serum concentration of cyclosporine in Iranian renal transplant patients. Transplant Proc 2003 Nov; 35 (7): 2739-41.
168. Proppe DG, Hoch OD, McLean AJ, et al. Influence of chronic ingestion of grapefruit juice on steady-state blood concentrations of cyclosporine A in renal transplant patients with stable graft function. Br J Clin Pharmacol 1995 Mar; 39 (3): 337-8.
169. Paine MF, Widmer WW, Pusek SN, et al. Further char- acterization of a furanocoumarin-free grapefruit juice on drug disposition: studies with cyclosporine. Am J Clin Nutr 2008 Apr 1; 87 (4): 863-71.
170. Schwarz UI, Johnston PE, Bailey DG, et al. Impact of ci- trus soft drinks relative to grapefruit juice on ciclosporin disposition. Br J Clin Pharmacol 2006 Oct; 62 (4): 485-91.
171. Neoral (ciclosporin) capsules/oral solution: US prescribing information. Novartis Pharmaceuticals Corp. Revised October 2009 [online]. Available from URL: http:// www.pharma.us.novartis.com/product/pi/pdf/neoral.pdf [Accessed 2010 Jul 17].
172. Liu C, Shang YF, Zhang XF, et al. Co-administration of grapefruit juice increases bioavailability of tacrolimus in liver transplant patients: a prospective study. Eur J Clin Pharmacol 2009 Sep; 65 (9): 881-5.
173. Fukatsu S, Fukudo M, Masuda S, et al. Delayed effect of grapefruit juice on pharmacokinetics and pharmacodynamics of tacrolimus in a living-donor liver transplant recipient. Drug Metab Pharmacokinet 2006 Apr; 21 (2): 122-5.
174. Peynaud D, Charpiat B, Vial T, et al. Tacrolimus severe overdosage after intake of masked grapefruit in orange marmalade. Eur J Clin Pharmacol 2007 Jul; 63 (7): 721-2.
175. Prograf (tacrolimus) capsules: summary of product char- acteristics. Astellas Pharma Ltd. Updated 25/05/ 2009 [online]. Available from URL: http://www.medicines.org. uk/EMC/medicine/11102/SPC/Prograf+0. 5mg%2c+1mg% 2c+5mg+Hard+Capsules [Accessed 2010 Feb 2].
176. Prograf® (tacrolimus) capsules: US prescribing informa- tion. Astellas Pharma US Inc. Revised August 2009 [online]. Available from URL: http://www.astellas.us/docs/ prograf.pdf [Accessed 2010 Jul 17].
177. Rapamune (sirolimus) tablets: summary of product char- acteristics. Wyeth Pharmaceuticals. Updated 27/07/2010 [online]. Available from URL: http://www.medicines.org. uk/EMC/medicine/5747/SPC/Rapamune [Accessed 2010 Jul 27].
178. Rapamune (sirolimus) tablets: US prescribing information. Wyeth Pharmaceuticals Inc. Updated 07/2010 [online]. Available from URL: http://www.wyeth.com/content/ showlabeling.asp?id=139 [Accessed 2010 Jul 27].
179. Jetter A, Kinzig-Schippers M, Walchner-Bonjean M, et al. Effects of grapefruit juice on the pharmacokinetics of sildenafil. Clin Pharmacol Ther 2002 Jan; 71 (1): 21-9.
180. Lee M, Min DI. Determination of sildenafil citrate in plasma by high-performance liquid chromatography and a case for the potential interaction of grapefruit juice with sildenafil citrate. Ther Drug Monit 2001 Feb; 23 (1): 21-6.
181. Viagra (sildenafil citrate) tablets: summary of product characteristics. Pfizer Ltd. Updated 19/07/2010 [online]. Available from URL: http://www.medicines.org.uk/EMC/ medicine/1474/SPC/Viagra+25mg%2c+50mg%2c+100mg [Accessed 2010 Jul 27].
182. Viagra® (sildenafil citrate) tablets: US prescribing infor- mation. Pfizer Inc. January 2010 [online]. Available from URL: http://www.pfizer.com/ files/products/uspi-viagra. pdf [Accessed 2010 Jul 16].
183. Cialis (tadalafil) tablets: summary of product characteristics. Eli Lilly and Company Limited. Updated 23/04/2010 [online]. Available from URL: http://www.medicines.org.uk/ EMC/medicine/11363/SPC/Cialis+2.5mg%2c+5mg%2c+ 10mg+%26+20mg+film-coated+tablets [Accessed 2010 Jul 27].
184. Cialis (tadalafil) tablet: US prescribing information. Eli Lilly & Co. Revised February 1, 2010 [online]. Available from URL: http://pi.lilly.com/ us/cialis-pi.pdf [Accessed 2010 Jul 13].
185. Levitra (vardenafil) tablets: summary of product character- istics. Bayer Plc. Updated 16/07/ 2009 [online]. Available from URL: http://www.medicines. org.uk/EMC/medicine/ 11775/SPC/Levitra+5mg%2c+10mg%2c+20mg+film-coat ed+tablets/ [Accessed 2010 Jan 13].
186. Levitra (vardenafil) tablets: US prescribing information. Bayer Healthcare Pharmaceuticals Inc. Updated 05/2010 [online]. Available from URL: http://www.univgraph. com/bayer/inserts/levitra.pdf [Accessed 2010 Jul 17].
187. Emselex (darifenacin) prolonged release tablets: summary of product characteristics. Novartis Pharmaceuticals UK Ltd. Updated 25/03/2010 [online]. Available from URL: http://www.medicines.org.uk/EMC/medicine/19164/SPC/ Emselex+7.5+mg+and+15+mg+prolonged-release+tablets [Accessed 2010 Sep 28].
188. Castro N, Jung H, Medina R, et al. Interaction between grapefruit juice and praziquantel in humans. Antimicrob Agents Chemother 2002 May; 46 (5): 1614-6.
189. Nagy J, Schipper HG, Koopmans RP, et al. Effect of grapefruit juice or cimetidine coadministration on albendazole bioavailability. Am J Trop Med Hyg 2002 Mar; 66 (3): 260-3.
190. Awadzi K, Hero M, Opoku NO, et al. The chemotherapy of onchocerciasis XVII. A clinical evaluation of albendazole in patients with onchocerciasis; effects of food and pretreatment with ivermectin on drug response and pharmacokinetics. Trop Med Parasitol 1994 Sep; 45 (3): 203-8.
191. Cheng KL, Nafziger AN, Peloquin CA, et al. Effect of grapefruit juice on clarithromycin pharmacokinetics. Antimicrob Agents Chemother 1998 Apr; 42 (4): 927-9.
192. Kanazawa S, Ohkubo T, Sugawara K. The effects of grapefruit juice on the pharmacokinetics of erythromycin. Eur J Clin Pharmacol 2001 Jan-Feb; 56 (11): 799-803.
193. Abbas R, Chow CP, Browder NJ, et al. In vitro metabolism and interaction of cilostazol with human hepatic cytochrome P450 isoforms. Hum Exp Toxicol 2000 Mar; 19 (3): 178-84.
194. Taniguchi K, Ohtani H, Ikemoto T, et al. Possible case of potentiation of the antiplatelet effect of cilostazol by grapefruit juice. J Clin Pharm Ther 2007 Oct; 32 (5): 457-9.
195. Pletal (cilostazol) 50mg tablets: summary of product char- acteristics. Otsuka Pharmaceuticals (UK) Ltd. Updated 03/09/ 2009 [online]. Available from URL: http://www. medicines.org.uk/emc/medicine/17181 [Accessed 2010 Feb 1].
196. Pletal (cilostazol) tablets: US prescribing information. Otsuka Pharmaceuticals, Inc. Updated 05/ 2007 [online]. Available from URL: http://www.otsuka-us.com/docu ments/Pletal-PI.pdf [Accessed 2010 Jul 19].
197. van rooij J, van der meer F, Schoemaker HC, et al. Com- parison of the effect of grapefruit juice and cimetidine on pharmacokinetics and anticoagulant effect of a single dose of acenocoumarol [abstract]. Br J Clin Pharmacol 1993 35: 548P.
198. Brandin H, Myrberg O, Rundlof T, et al. Adverse effects by artificial grapefruit seed extract products in patients on warfarin therapy. Eur J Clin Pharmacol 2007 Jun; 63 (6): 565-70.
199. Nemeroff CB, DeVane CL, Pollock BG. Newer antide- pressants and the cytochrome P450 system. Am J Psychiatry 1996 Mar; 153 (3): 311-20.
200. Stockley's drug interactions. 9th ed. London: Pharmaceu- tical Press, 2010 [online]. Available from URL: http:// www.medicinescomplete.com [Accessed 2010 Nov 15].
201. Preskorn SH. Clinically relevant pharmacology of selective serotonin reuptake inhibitors: an overview with emphasis on pharmacokinetics and effects on oxidative drug metabolism. Clin Pharmacokinet 1997; 32 Suppl. 1: 1-21.
202. Obach RS, Cox LM, Tremaine LM. Sertraline is metabo- lized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug Metab Dispos 2005 Feb; 33 (2): 262-70.
203. Ueda N, Yoshimura R, Umene-Nakano W, et al. Grape- fruit juice alters plasma sertraline levels after single in-gestion of sertraline in healthy volunteers. World J Biol Psychiatry 2009; 10 (4 Pt 3): 832-5.
204. Lee AJ, Chan WK, Harralson AF, et al. The effects of grapefruit juice on sertraline metabolism: an in vitro and in vivo study. Clin Ther 1999 Nov; 21 (11): 1890-9.
205. Fabre LF, Abuzzahab FS, Amin M, et al. Sertraline safety and efficacy in major depression: a double-blind fixed-dose comparison with placebo. Biol Psychiatry 1995 Nov 1; 38 (9): 592-602.
206. Sertraline (setraline 50mg and 100mg film coated tablets): summary of product characteristics. Wockhardt UK Ltd. Updated 11/06/ 2009 [online]. Available from URL: http:// www.medicines.org.uk/emc/medicine/18935/SPC/Sertrali ne+50mg+and+100mg+Film-Coated+Tablets [Accessed 2010 Feb 1].
207. Zoloft (sertraline) tablets/oral solution: US prescribing information. Updated 10/ 2008 [online]. Available from URL: http://media.pfizer.com/files/ products/uspi-zoloft. pdf [Accessed 2010 Jul 16].
208. DeSilva KE, Le Flore DB, Marston BJ, et al. Serotonin syndrome in HIV-infected individuals receiving antiretro-viral therapy and fluoxetine. AIDS 2001 Jul 6; 15 (10): 1281-5.
209. Fluoxetine (fluoxetine 20mg capsules): summary of prod- uct characteristics. Sandoz Ltd. Updated 23/12/ 2009 [online]. Available from URL: http://www.medicines.org. uk/emc/medicine/22921/SPC/Fluoxetine+20mg+Capsules [Accessed 2010 Feb 1].
210. Prozac (fluoxetine hydrochloride): US prescribing in- formation. Eli Lilly and Company. Revised October 29, 2009 [online]. Available from URL: http://pi.lilly.com/us/ prozac.pdf [Accessed 2010 Jan 18].
211. Hori H, Yoshimura R, Ueda N, et al. Grapefruit juice- fluvoxamine interaction: is it risky or not? J Clin Psycho-pharmacol 2003 Aug; 23 (4): 422-4.
212. Fluvoxamine (fluvoxamine 50mg & 100mg film coated tab- lets): summary of product characteristics. Wockhardt UK Ltd. Updated 02/09/ 2008 [online]. Available from URL: http://www.medicines.org.uk/EMC/medicine/18896/SPC/ Fluvoxamine%2050mg%20&%20100mg%20Film-Coated %20Tablets%20(Wockhardt%20UK%20Ltd)/ [Accessed 2010 Feb 1].
213. Luvox® CR (fluvoxamine maleate) extended release cap- sules: US prescribing information. Solvay Pharmaceuticals Inc. Revised 02/2009 [online]. Available from URL: http://www.luvoxcr.com/LUVOX-CR-PI.pdf [Accessed 2010 Jul 15].
214. Bidstrup TB, Damkier P, Olsen AK, et al. The impact of CYP2C8 polymorphism and grapefruit juice on the pharmacokinetics of repaglinide. Br J Clin Pharmacol 2006 Jan; 61 (1): 49-57.
215. Heykants J, Van Peer A, Van de Velde V, et al. The clinical pharmacokinetics of itraconazole: an overview. Mycoses 1989; 32 Suppl. 1: 67-87.
216. Kawakami M, Suzuki K, Ishizuka T, et al. Effect of grape- fruit juice on pharmacokinetics of itraconazole in healthy subjects. Int J Clin Pharmacol Ther 1998 Jun; 36(6): 306-8.
217. Penzak SR, Gubbins PO, Gurley BJ, et al. Grapefruit juice decreases the systemic availability of itraconazole capsules in healthy volunteers. Ther Drug Monit 1999 Jun; 21 (3): 304-9.
218. Gubbins PO, Gurley BJ, Williams DK, et al. Examining sex-related differences in enteric itraconazole metabolism in healthy adults using grapefruit juice. Eur J Clin Pharmacol 2008 Mar; 64 (3): 293-301.
219. Cvetkovic M, Leake B, Fromm MF, et al. OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. Drug Metab Dispos 1999 Aug; 27 (8): 866-71.
220. Wanwimolruk S, Chalcroft S, Coville PF, et al. Pharma- cokinetics of quinine in young and elderly subjects. Trans R Soc Trop Med Hyg 1991 Nov-Dec; 85 (6): 714-7.
221. Ho PC, Chalcroft SC, Coville PF, et al. Grapefruit juice has no effect on quinine pharmacokinetics. Eur J Clin Pharmacol 1999 Jul; 55 (5): 393-8.
222. Eiermann B, Engel G, Johansson I, et al. The involvement of CYP1A2 and CYP3A4 in the metabolism of clozapine. Br J Clin Pharmacol 1997; 44 (5): 439-46.
223. Raaska K, Neuvonen PJ. Serum concentrations of cloz- apine and N-desmethylclozapine are unaffected by the potent CYP3A4 inhibitor itraconazole. Eur J Clin Pharmacol 1998 Apr; 54 (2): 167-70.
224. Vandel S, Netillard C, Perault MC, et al. Plasma levels of clozapine and desmethylclozapine are unaffected by concomitant ingestion of grapefruit juice. Eur J Clin Pharmacol 2000 Jul; 56 (4): 347-8.
225. Ozdemir V, Kalow W, Okey AB, et al. Treatment-resistance to clozapine in association with ultrarapid CYP1A2 activity and the C->A polymorphism in intron 1 of the CYP1A2 gene: effect of grapefruit juice and low-dose fluvoxamine. J Clin Psychopharmacol 2001 Dec; 21 (6): 603-7.
226. Yasui N, Kondo T, Suzuki A, et al. Lack of significant pharmacokinetic interaction between haloperidol and grapefruit juice. Int Clin Psychopharmacol 1999 Mar; 14 (2): 113-8.
227. Demarles D, Gillotin C, Bonaventure-Paci S, et al. Single- dose pharmacokinetics of amprenavir coadministered with grapefruit juice. Antimicrob Agents Chemother 2002 May; 46 (5): 1589-90.
228. Telzir (fosamprenavir) tablets: summary of product char- acteristics. ViiV Healthcare UK Ltd. Updated 19/5/2010 [online]. Available from URL: http://www.medicines.org. uk/EMC/medicine/14819/SPC/Telzir+700+mg+film-coated +tablets [Accessed 2010 Jul 12].
229. Chiba M, Hensleigh M, Lin JH. Hepatic and intestinal metabolism of indinavir, an HIV protease inhibitor, in rat and human microsomes: major role of CYP3A. Biochem Pharmacol 1997 Apr 25; 53 (8): 1187-95.
230. Penzak SR, Acosta EP, Turner M, et al. Effect of Seville orange juice and grapefruit juice on indinavir pharmaco-kinetics. J Clin Pharmacol 2002 Oct; 42 (10): 1165-70.
231. Shelton MJ, Wynn HE, Hewitt RG, et al. Effects of grapefruit juice on pharmacokinetic exposure to indinavir in HIV-positive subjects. J Clin Pharmacol 2001 Apr; 41 (4): 435-42.
232. Kupferschmidt HH, Fattinger KE, Ha HR, et al. Grape- fruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man. Br J Clin Pharmacol 1998 Apr; 45 (4): 355-9.
233. Invirase (saquinavir 500mg film-coated tablets): summary of product characteristics. Roche Products Limited. Updated 05/08/2010 [online]. Available from URL: http:// www.medicines.org.uk/EMC/medicine/1694/SPC/Invirase +200+mg+hard+capsules+and+500+mg+film-coated+tablets/ [Accessed 2010 Feb 1].
234. Sustiva (efavirenz 600mg film coated tablets): summary of product characteristics. Bristol-Myers Squibb Pharmaceuticals Ltd. Updated 07/09/ 2009 [online]. Available from URL: http://www.medicines.org.uk/emc/document. aspx?documentid=11284&docType=SPC [Accessed 2010 Feb 1].
235. Renner UD, Oertel R, Kirch W. Pharmacokinetics and pharmacodynamics in clinical use of scopolamine. Ther Drug Monit 2005 Oct; 27 (5): 655-65.
236. Ebert U, Oertel R, Kirch W. Influence of grapefruit juice on scopolamine pharmacokinetics and pharmaco-dynamics in healthy male and female subjects. Int J Clin Pharmacol Ther 2000 Nov; 38 (11): 523-31.
237. Yasui N, Kondo T, Furukori H, et al. Effects of repeated ingestion of grapefruit juice on the single and multiple oral-dose pharmacokinetics and pharmacodynamics of alprazolam. Psychopharmacology (Berl) 2000 Jun; 150 (2): 185-90.
238. Lanoxin (digoxin 0.25mg tablets): summary of product characteristics. GlaxoSmithKline UK. Updated 08/03/2010 [online]. Available from URL: http://www.medicines.org. uk/emc/medicine/2178/SPC/Lanoxin%20Tablets%200.25mg [Accessed 2010 Feb 1].
239. Parker RB, Yates CR, Soberman JE, et al. Effects of grapefruit juice on intestinal P-glycoprotein: evaluation using digoxin in humans. Pharmacotherapy 2003 Aug; 23 (8): 979-87.
240. Lilja JJ, Raaska K,Neuvonen PJ. Effects of grapefruit juice on the pharmacokinetics of acebutolol. Br J Clin Pharmacol 2005 Dec; 60 (6): 659-63.
241. Christensen H, Asberg A, Holmboe AB, et al. Coadmin- istration of grapefruit juice increases systemic exposure of diltiazem in healthy volunteers. Eur J Clin Pharmacol 2002 Nov; 58 (8): 515-20.
242. Doppenschmitt S, Spahn-Langguth H, Regardh CG, et al. Role of P-glycoprotein-mediated secretion in absorptive drug permeability: an approach using passive membrane permeability and affinity to P-glycoprotein. J Pharm Sci 1999 Oct; 88 (10): 1067-72.
243. Edgar B, Regardh CG, Johnsson G, et al. Felodipine ki- netics in healthy men. Clin Pharmacol Ther 1985 Aug; 38 (2): 205-11.
244. Pisarik P. Blood pressure-lowering effect of adding grape- fruit juice to nifedipine and terazosin in a patient with severe renovascular hypertension. Arch Fam Med 1996 Jul-Aug; 5 (7): 413-6.
245. Plendil (felodipine) tablets: summary of product char- acteristics. AstraZeneca UK Ltd. Updated 11/03/2010 [online]. Available from URL: http://www.medicines.org. uk/EMC/medicine/191/SPC/Plendil+2.5mg%2c+Plendil+ 5mg+and+Plendil+10mg [Accessed 2010 Jul 22].
246. Stearns RA, Chakravarty PK, Chen R, et al. Bio- transformation of losartan to its active carboxylic acid metabolite in human liver microsomes: role of cyto-chrome P4502C and 3A subfamily members. Drug Metab Dispos 1995 Feb; 23 (2): 207-15.
247. Kaukonen KM, Olkkola KT, Neuvonen PJ. Fluconazole but not itraconazole decreases the metabolism of losartan to E-3174. Eur J Clin Pharmacol 1998 Feb; 53 (6): 445-9.
248. Zaidenstein R, Soback S, Gips M, et al. Effect of grapefruit juice on the pharmacokinetics of losartan and its active metabolite E3174 in healthy volunteers. Ther Drug Monit 2001 Aug; 23 (4): 369-73.
249. Varis T, Kaukonen KM, Kivisto KT, et al. Plasma con- centrations and effects of oral methylprednisolone are considerably increased by itraconazole. Clin Pharmacol Ther 1998 Oct; 64 (4): 363-8.
250. Varis T, Kivisto KT, Neuvonen PJ. Grapefruit juice can increase the plasma concentrations of oral methylpredni-solone. Eur J Clin Pharmacol 2000 Sep; 56 (6-7): 489-93.
251. Varis T, Kivisto KT, Backman JT, et al. The cytochrome P450 3A4 inhibitor itraconazole markedly increases the plasma concentrations of dexamethasone and enhances its adrenal-suppressant effect. Clin Pharmacol Ther 2000 Nov; 68 (5): 487-94.
252. Raaska K, Niemi M, Neuvonen M, et al. Plasma con- centrations of inhaled budesonide and its effects on plasma cortisol are increased by the cytochrome P4503A4 inhibitor itraconazole. Clin Pharmacol Ther 2002 Oct; 72 (4): 362-9.
253. Hande K, Messenger M, Wagner J, et al. Inter- and intra- patient variability in etoposide kinetics with oral and intravenous drug administration. Clin Cancer Res 1999 Oct; 5 (10): 2742-7.
254. Reif S, Nicolson MC, Bisset D, et al. Effect of grapefruit juice intake on etoposide bioavailability. Eur J Clin Pharmacol 2002 Oct; 58 (7): 491-4.
255. Goldbart A, Press J, Sofer S, et al. Near fatal acute col- chicine intoxication in a child: a case report. Eur J Pediatr 2000 Dec; 159 (12): 895-7.
256. Fujiwara K, Adachi H, Nishio T, et al. Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology 2001 May; 142 (5): 2005-12.
257. Kassem NA, Deane R, Segal MB, et al. Thyroxine (T4) transfer from CSF to choroid plexus and ventricular brain regions in rabbit: contributory role of P-glycoprotein and organic anion transporting polypeptides. Brain Res 2007 Nov 21; 1181: 44-50.
258. Lilja JJ, Laitinen K, Neuvonen PJ. Effects of grapefruit juice on the absorption of levothyroxine. Br J Clin Pharmacol 2005 Sep; 60 (3): 337-41.
259. Schubert W, Cullberg G, Edgar B, et al. Inhibition of 17 beta-estradiol metabolism by grapefruit juice in ovar-iectomized women. Maturitas 1994 Dec; 20 (2-3): 155-63.
260. Weber A, Jager R, Borner A, et al. Can grapefruit juice influence ethinylestradiol bioavailability? Contraception 1996 Jan; 53 (1): 41-7.
261. Grande LA, Mendez RD, Krug RT, et al. Attention: grapefruit! Lancet 2009 Apr 4; 373 (9670): 1222.
262. Wang JS, DeVane CL. Involvement of CYP3A4, CYP2C8, and CYP2D6 in the metabolism of (R)- and (S)-methadone in vitro. Drug Metab Dispos 2003 Jun; 31 (6): 742-7.
263. Benmebarek M, Devaud C, Gex-Fabry M, et al. Effects of grapefruit juice on the pharmacokinetics of the en-antiomers of methadone. Clin Pharmacol Ther 2004 Jul; 76 (1): 55-63.
264. Methadone solution for injection: summary of product char- acteristics. Wockhardt UK Ltd. Updated 02/09/
265. Boolell M, Allen MJ, Ballard SA, et al. Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. Int J Impot Res 1996 Jun; 8 (2): 47-52.
266. Ballard TL, Halaweish FT, Stevermer CL, et al. Naringin does not alter caffeine pharmacokinetics, energy ex- penditure, or cardiovascular haemodynamics in humans following caffeine consumption. Clin Exp Pharmacol Physiol 2006 Apr; 33 (4): 310-4.
267. Strauch K, Lutz U, Bittner N, et al. Dose-response re- lationship for the pharmacokinetic interaction of grapefruit juice with dextromethorphan investigated by human urinary metabolite profiles. Food Chem Toxicol 2009 Aug; 47 (8): 1928-35.
268. Di Marco MP, Edwards DJ, Wainer IW, et al. The effect of grapefruit juice and seville orange juice on the pharma-cokinetics of dextromethorphan: the role of gut CYP3A and P-glycoprotein. Life Sci 2002 Jul 26; 71 (10): 1149-60.
269. Hukkanen J, Jacob 3rd P, Benowitz NL. Effect of grape- fruit juice on cytochrome P450 2A6 and nicotine renal clearance. Clin Pharmacol Ther 2006 Nov; 80 (5): 522-30.
270. Martin J, editor. British national formulary. 58th ed. London: RPS Publishing, 2009: 720-803, 932-46.
271. Grapefruit diet: 12-day grapefruit diet plan [online]. Avail- able from URL: http://www.grapefruit-diet.org [Accessed 2010 Feb 3].
272. Dallas C, Gerbi A, Tenca G, et al. Lipolytic effect of a polyphenolic citrus dry extract of red orange, grapefruit, orange (SINETROL) in human body fat adipocytes: mechanism of action by inhibition of cAMP-phosphodiesterase (PDE). Phytomedicine 2008 Oct; 15 (10): 783-92.
273. Greenblatt DJ. Analysis of drug interactions involving fruit beverages and organic anion-transporting polypeptides. J Clin Pharmacol 2009 Dec; 49 (12): 1403-7.
274. Inspra (eplerenone) tablets: summary of product char- acteristics. Pfizer Limited. Updated 19/11/ 2009 [online]. Available from URL: http://www. medicines.org.uk/EMC/ medicine/16746/SPC/Inspra+25mg+%26+50+mg+film-coat ed+tablets/#tableOfContents [Accessed 2010 Sep 28].
275. Xarelto (rivaroxaban) 10mg tablets: summary of product characteristics. Bayer plc. Updated 30/06/2010 [online]. Available from URL: http://www. medicines.org.uk/EMC/ medicine/21265/SPC/Xarelto+10+mg+film-coated+tablets/ #tableOfContents [Accessed 2010 Sep 28]