Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model

British Journal of Clinical Pharmacology

Volumn 49, Issue 1, 2000, Pages 49-58

  Takanaga, Hitomi ^a   Ohnishi, Ayako ^a   Matsuo, Hirotami ^a   Murakami, Hideyasu ^a   Sata, Hiroko ^b   Kuroda, Ken ^b   Urae, Akinori ^a   Higuchi, Shun ^a   Sawada, Yasufumi ^a  

^a KYUSHU UNIVERSITY   (Japan)

^b FUKUOKA UNIVERSITY HOSPITAL   (Japan)

Author keywords

Felodipine; Grapefruit juice; Modelling; Pharmacokinetics

Indexed keywords

CYTOCHROME P450 3A4; FELODIPINE; INTESTINE ENZYME;

AREA UNDER THE CURVE; ARTICLE; CHEMICAL REACTION KINETICS; CONTROLLED STUDY; DRUG CLEARANCE; DRUG ELIMINATION; ENZYME INACTIVATION; FRUIT JUICE; HALF LIFE TIME; HUMAN; MALE; MODEL; NORMAL HUMAN; PRIORITY JOURNAL; REGRESSION ANALYSIS; SLOW RELEASE FORMULATION;

EID: 0033976593     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.2000.00140.x     Document Type: Article

References (44)

1. 1 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: 313-317.
2. 2 Lown KS, Bailey DG, Fontana RJ, et al. Grapefruit juice increases felodipine oral availability in human by decreasing intestinal CYP3A protein expression. J Clin Invest 1997; 99: 2545-2553.
3. 3 Bailey DG, Spence JD, Munoz C, Arnold JMO. Interaction of cirrus juices with felodipine and nifedipine. Lancet 1991; 337: 268-269.
4. 4 Bailey DG, Malcom J, Arnold O, Munoz C, Spence JD. Grapefruit juice-felodipine interaction: mechanism, predictability, and effect of naringin. Clin Pharmacol Ther 1993; 53: 637-642.
5. 5 Lundahl JUE, Regardh CG, Edgar B, Johnsson G. Relation 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: 61-67.
6. 6 Lundahl JUE, Regardh CG, Edgar B, Johnsson G. The interaction effect of grapefruit juice is maximal after the first glass. Eur J Clin Pharmacol 1998; 54: 75-81.
7. 7 Lundahl JUE, Regardh CG, Edgar B, Johnsson G. Effects of grapefruit juice ingestion-pharmacokinetics and haemodynamics of intravenously and orally administered felodipine in healthy men. Eur J Clin Pharmacol 1997; 52: 139-145.
8. 8 Bailey DG, Arnold JMO, 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: 135-140.
9. 9 Bailey DG, Bend JR, Malcom J, Arnold O, Tran LT, Spence JD. Erythromycin-felodipine interaction: magnesium, mechanism, and comparison with grapefruit juice. Clin Pharmacol Ther 1996; 60: 25-33.
10. 10 Rashid TJ, Martin U, Clarke H, Waller DG, Renwick AG, George CF. Factors affecting the absolute bioavailability of nifedipine. Br J Clin Pharmacol 1995; 40: 51-58.
11. 11 Bailey DG, Arnold JMO, Strong HA, et al. Grapefruit juice and naringin on nisoldipine pharmacokinetics. Clin Pharmacol Ther 1993; 54: 589-594.
12. 12 Soons PA, Vogels BA, Roosemalen MC, et al. Grapefruit juice and cimetidine inhibit stereoselective metabolism of nitrendipine in humans. Clin Pharmacol Ther 1991; 50: 394-403.
13. 13 Fhur U, Harder S, Lopez-Rojas P, et al. Increase of verapamil concentrations in steady state by coadministrtion of grapefruit juice. Arch Pharmacol 1994; 349: R134.
14. 14 Benton RE, Honig PK, Zamani K, Cantilena LR, Woosley RL. Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram. Clin Pharmacol Ther 1996; 59: 383-388.
15. 15 Ducharme MP, Provenzano R, Dehoorne-Smith M, Edwards DJ. Trough concentrations of cyclosporine in blood following administration with grapefruit juice. Br J Clin Pharmacol 1993; 36: 457-459.
16. 16 Ducharme MP, Warbasse LH, Edwards DJ. Disposition of intravenous and oral cyclosporine after administration with grapefruit juice. Clin Pharmacol Ther 1995; 57: 485-491.
17. 17 Ozdemir M, Aktan Y, Boydag BS, Cingi MI, Musmul A. Interaction between grapefruit juice and diazepam in human. Eur J Drug Metab Pharmacokin 1998; 23: 55-59.
18. 18 Kupferschmidt HH, Ha HR, Ziegler WH, Meier PJ, Krahenbuhl S. Interaction between grapefruit juice and midazolam in human. Clin Pharmacol Ther 1995; 58: 20-28.
19. 19 Hukkinen SK, Varhe A, Olkkola KT, Neuvonen PJ. Plasma concentrations of triazolam are increased by concomitant ingestion of grapefruit juice. Clin Pharmacol Ther 1995; 58: 127-131.
20. 20 Kupferschmidt HHT, Fattinger KE, Ha HR, Follath F, Krahenbuhl S. Grapefruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man. Br J Clin Pharmacol 1998; 45: 355-359.
21. 21 Weber A, Jager R, Borner A, Klinger G, Vollanth R, Matth K. Can grapefruit juice influence ethinylestradiol bioavailability? Contraception 1996; 53: 41-47.
22. 22 Fuhr U, Klittich K, Atab AH. Inhibitory effect of grapefruit juice and its bitter principal, naringenin, on CYP1A2 dependent metabolism of caffeine in man. Br J Clin Pharmacol 1993; 35: 431-436.
23. 23 Westveer MK, Farquhar ML, George P, Mayers JT. Co-administration of grapefruit juice increases tacrolimus levels in liver transplant recipients. Ann Meet Am Soc Transplant Physicians 1996; 202: P115.
24. 24 Wacher VJ, Wu C-Y, Benet LZ. Overlapping substrate specificities and tissue distribution of cytochrome P450, 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol Carcinogenesis 1995; 13: 129-134.
25. 25 Schmiedlin-Ren P, Edwards DJ, Fitzsimmons ME, et al. Mechanisms of enhanced oral availability of CYP3A4 substrates by grapefruit constituents, decreased enterocyte CYP3A4 concentration and mechanism-based inactivation by furanocoumarins. Drug Metab Dispos 1997; 25: 1228-1233.
26. 26 Takanaga H, Ohnishi A, Matsuo H, Sawada Y. Inhibition of vinblastine efflux mediated by P-glycoprotein by grapefruit juice components in Caco-2 cells. Biol Pharm Bull 1998; 21: 1062-1066.
27. 27 Edwards DJ, Bellevue FH III, Woster PM. Identification of 6′,7′-dihydroxybergamottin, a cytochrome P450 inhibitor, in grapefruit juice. Drug Metab Dispos 1996; 24: 1287-1290.
28. 28 He K, Iyer KR, Hayes RN, Sinz MW, Woolf TF, Hollenberg PF. Inactivation of cytochrome P450 3A4 by bergamottin, a component of grapefruit juice. Chem Res Toxicol 1998; 11: 252-259.
29. 29 Fukuda K, Ohta T, Oshima Y, Ohashi N, Yoshikawa M, Yamazoe Y. Specific CYP3A4 inhibitors in grapefruit juice: furocoumarin dimers as components of drug interaction, Pharmacogenetics 1997; 7: 391-396.
30. 30 Matsuo H, Ohnishi A, Yamada S, et al. Effect of furanocoumarin derivatives in grapefruit juice on the uptake of vinblastin by Caco-2 cells and on the activity of cytochrome P450 3A4. Submitted.
31. 31 Katashima M, Iruno T, Shimojo F, et al. Pharmacokinetics and pharmacodynamics of FK143, a nonsteroid 5α-reductase, in healthy volunteers. Clin Pharmacol Ther 1998; 63: 354-366.
32. 32 Katashima M, Yamamoto K, Gugiuram M, Sawada Y, Iga T. Comparative pharmacokinetic/pharmacodynamic study of proton pump inhibitors, omeprazole and lansoprazole in rats. Drug Metab Dispos 1995; 23: 718-723.
33. 33 Sugiura M, Yamamoto K, Sawada Y, Iga T. Prediction of therapeutic doses based on the pharmacokinetic/pharmacodynamic model of omeprazole, a proton pump inhibitor. Xenobio Metab Dispos 1992; 7: 813-820.
34. 34 Katashima M, Yamamoto K, Tokuma Y, Hata T, Sawada Y, Iga T. Pharmacokinetic and pharmacodynamic study of a new nonsteroidal 5α-reductase inhibitor, 4-[3-[3-[bis (4-isobutylphenyl) methylamino]benzoyl]-1H-indol-1-yl]butyric acid, in rats. J Pharmacol Exp Ther 1998; 284: 914-920.
35. 35 Mapleson WW. An electronic analogue for uptake and exchange of inert gases and other agents. J Appl Physiol 1963; 18: 197.
36. 36 Benowitz N, Forsyth RP, Melmon KL, Rowland M. Lidocaine disposition kinetics in monkey and man I. Prediction by a perfusion model. Clin Pharmacol 1974; 16: 887.
37. 37 Spector WS. (ed). Handbook of Biological Data, pp 163-283. W.B.Saunders, Philadelphia, 1956.
38. 38 Dedrick RL, Zaharko DS, Lutz RJ. Transport binding of methotrexate in vivo. J Pharm Sci 1973; 62: 882.
39. 39 Christensen FN, Davis SS, Hardy JG, Taylor MJ, Whalley DR, Wilson CG. The use of gamma scintigraphy to follow the gastrointestinal transit of pharmaceutícal formulations. J Pharm Pharmacol 1985; 37: 91-95.
40. 40 Yamaoka K, Tanigawara Y, Nakagawa T, Uno T. A pharmacokinetic analysis program (MULTI) for microcomputer. J Pharmacobio-Dyn 1981; 4: 879-885.
41. 41 Shiraki H, Guengerich FP. Turnover of membrane proteins: kinetics of induction and degradation of seven form of rat liver microsomal cytochrome P-450, NADPH-cytochrome P-450 reductase, and epoxide hydrolase. Archiv Biochem Biophys 1984; 2325: 86-96.
42. 42 Edgar B, Bailey DG, Bergstrand R, Johnsson G, Lurje L. Formulation dependent interaction between felodipine and grapefruit juice. Clin Pharmacol Ther 1990; 47 [suppl]: 181.
43. 43 Paine MF, Khalighi M, Fisher JM, et al. Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 1997; 283: 1552-1562.
44. 44 Abrahamsson B, Alpsten M, Hugosson M, et al. Absorption, gastrointestinal transit, and tablet erosion of felodipine extended-release (ER) tablets. Pharm Res 1993; 10: 709-714.