Co-treatment with grapefruit juice inhibits while chronic administration activates intestinal P-glycoprotein-mediated drug efflux

Pharmazie

Volumn 60, Issue 12, 2005, Pages 922-927

  Panchagnula, Ramesch ^a,b   Bansal, T ^a   Varma, M V S ^a   Kaul, C L ^a  

^a NATIONAL INSTITUTE OF PHARMACEUTICAL EDUCATION AND RESEARCH NIPER   (India)

^b UNIVERSITY OF ULSTER   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOPROTEIN P; INDINAVIR; PACLITAXEL; PROPRANOLOL; RIFAMPICIN; VERAPAMIL;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; GRAPEFRUIT JUICE; ILEUM; MALE; MEMBRANE PERMEABILITY; MEMBRANE TRANSPORT; NONHUMAN; PROTEIN EXPRESSION; RAT;

ALGORITHMS; ANIMALS; ANTINEOPLASTIC AGENTS, PHYTOGENIC; ANTITUBERCULAR AGENTS; BEVERAGES; CALCIUM CHANNEL BLOCKERS; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CITRUS PARADISI; DOSE-RESPONSE RELATIONSHIP, DRUG; FOOD-DRUG INTERACTIONS; HIV PROTEASE INHIBITORS; ILEUM; INDINAVIR; INTESTINAL ABSORPTION; MALE; P-GLYCOPROTEIN; PACLITAXEL; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; RATS; RATS, SPRAGUE-DAWLEY; RIFAMPIN; VERAPAMIL;

EID: 29244465111     PISSN: 00317144     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (25)

1. Ambudkar SV, Dey, S, Hrycyna, CA, Ramchandra, M, Pastan, I, Gottesman, MM (1999) Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annu Rev Pharmacol Toxicol 39: 361-398.
2. Bailey D, Spence, J, Munoz, C, Arnold, J (1991) Interaction of citrus juices with felodipine and nifedipine. Lancet 337: 268-269.
3. Chiou WL, Barve, A (1998) Linear correlation of the fraction of oral dose absorbed of 64 drugs between humans and rats. Pharm Res 15: 1792-1795.
4. Edwards DJ, Fitzimmons, ME, Schuetz, EG, Yasuda, K, Ducharme, MP, Warbasse, LH, Woster, PM, Schuetz, JD, Watkins, P (1999) 6′,7′- Dihydroxybergamottin in grapefruit juice and Seville orange juice: Effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein. Clin Pharmacol Ther 65: 237-244.
5. Hanafy A, Langguth, P, Spahn-Langguth, H (2001) Pretreatment with potent P-glycoprotein ligands may increase intestinal secretion in rats. Eur J Pharm Sci 12: 405-415.
6. Kupferschmidt HHT, Fattinger, KE, Ha HR, Follath, F, Krahenbuhl, S (1998) Grapefruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man. Br J Clin Pharmacol 45: 355-359.
7. Langguth HS, Langguth, P (2001) Grapefruit juice enhances intestinal absorption of the P-glycoprotein substrate talinolol. Eur J Pharm Sci 12: 361-367.
8. Lilja JJ, Backman, JT, Laitila J, Luurila H, Neuvonen, PJ (2003) Itraconazole increases but grapefruit juice greatly decreases plasma concentrations of celiprolol. Clin Pharm Ther 73: 192-198.
9. Lin JH (2003) Drug-drug interaction mediated by inhibition and induction of P-glycoprotein. Adv Drug Deliv Rev 55: 53-81.
10. Lown KS, Bailey DG, Fontana RJ, Janardan SK, Adair CH, Fortiage LA, Brown MB, Guo W, Watkins PB (1997) Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. J Clin Invest 99: 2545-2553.
11. Marco MPD, Edwards DJ, Wainer IW, Ducharme MP (2002) The effect of grapefruit juice and seville orange juice on the pharmacokinetics of dextromethorphan: The role of gut CYP3A and P-glycoprotein. Life Sci 71: 1149-1160.
12. Ohnishi A, Matso H, Yamada S, Takanaga H, Morimoto S, Shoyama Y, Ohtana H, Sawada Y (2000) Effect of furanocoumarin derivatives in grapefruit juice on the uptake of vinblastine by Caco-2 cells and on the activity of cytochrome P450 3A4. Br J Pharmacol 130: 1369-1377.
13. Panchagnula R, Bansal T, Varma MV, Kaul CL (2004) Reversed-phase liquid chromatography with ultraviolet detection for simultaneous quantitation of indinavir and propranolol from ex-vivo rat intestinal permeability studies. J Chromatogr B Analyt Technol Biomed Life Sci 806: 277-282.
14. Sandstrom R, Lennernas H (1999) Repeated oral rifampicin decreases the jejunal permeability of R/S-verapamil in rats. Drug Met Disp 27: 951-955.
15. Schmiedlin-Ren P, Edwards DJ, Fitzsimmons ME, He K, Lown KS, Woster PM, Rahman A, Thummel KE, Fisher JM, Hollenberg PF, Watkins PB (1997) Mechanism of enhanced oral availability of CYP3A4 substrates by grapefruit constituents. Decreased enterocyte CYP3A4 concentration and mechanism-based inactivation by furanocoumarins. Drug Met Disp 25: 1228-1234.
16. Sharma P, Chawla HPS, Panchagnula R (2002) LC determination of cephalosporins in in-vitro rat intestinal sac absorption model. J Pharm Biomed Anal 27: 39-50.
17. Soldner A, Christians U, Susanto M, Wacher VJ, Silverman AJ, Benet LZ (1999) Grapefruit juice activates P-glycoprotein-mediated drug transport. Pharm Res 16: 478-485.
18. Sparreboom A, Asperen JV, Mayer U, Schinkel AH, Smit JW, Meijer DKF, Nooijen WJ, Beijnen JH, Tellingen OV (1997) Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc Natl Acad Sci USA 94: 2031-2035.
19. Stephens RH, Hughes JT, Higgs NB, Humphrey M, Warhurst G (2002) Region-dependent modulation of intestinal permeability by drug efflux transporters: in vitro studies in mdr1a(-/-) mouse intestine. J Pharm Exp Ther 303: 1095-1101.
20. Tian R, Koyabu N, Takanaga H, Matsuo H, Ohtani H, Sawada Y (2002) Effects of grapefruit juice and orange juice on the intestinal efflux of P-glycoprotein substances. Pharm Res 19: 802-809.
21. Troutman M, Thakker DR (2003) Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm Res 20: 1210-1223.
22. Varma M, Ashokraj Y, Dey CS, Panchagnula R (2003) P-glycoprotein inhibitors and their screening: a perspective from bioavailability enhancement. Pharmacol Res 48: 347-359.
23. Wang E, Casciano CN, Clement RP, Johnson WW (2001) Inhibition of P-glycoprotein transport function by grapefruit juice psoralen. Pharm Res 18: 432-438.
24. Xu J, Go ML, Lim LY (2003) Modulation of digoxin transport across Caco-2 cell monolayers by citrus fruit juices: lime, lemon, grapefruit, and pummelo. Pharm Res 20: 169-176.
25. Yumoto R, Murakami T, Nakamoto Y, Hasegawa R, Nagai J, Takano M (1999) Transport of rhodamine 123, a P-glycoprotein substrate, across rat intestine and Caco-2 cell monolayers in the presence of cytochrome P-450 3A-related compounds. J Pharmacol Exp Ther 289: 149-155.