Pig hepatocytes as an in vitro model to study the regulation of human CYP3A4: Prediction of drug-drug interactions with 17α-ethynylestradiol

Chemico-Biological Interactions

Volumn 107, Issue 1-2, 1997, Pages 93-108

  Olsen, Anette K ^a,b   Hansen, Kristian T ^a   Friis, Christian ^b  

^a NOVO NORDISK A S   (Denmark)

^b UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

17 ethynylestradiol; CYP3A; Drug drug interactions; Hepatocytes; Induction; Pig

Indexed keywords

CARBAMAZEPINE; CYTOCHROME P450 ISOENZYME; DEXAMETHASONE; ERYTHROMYCIN; ETHINYLESTRADIOL; NORFLOXACIN; PHENOBARBITAL; PHENYLBUTAZONE; PHENYTOIN; RIFAMPICIN; SPIRAMYCIN; SULFINPYRAZONE; TESTOSTERONE; TROLEANDOMYCIN; VALPROIC ACID;

ANIMAL CELL; CONFERENCE PAPER; CONTROLLED STUDY; DRUG HYDROXYLATION; ENZYME INDUCTION; ENZYME REGULATION; FEMALE; LIVER CELL; LIVER CELL CULTURE; MONOLAYER CULTURE; NONHUMAN; SWINE;

ANIMALS; ANTIBODIES, MONOCLONAL; CELLS, CULTURED; CYTOCHROME P-450 ENZYME SYSTEM; DRUG INTERACTIONS; ENZYME INDUCTION; ESTRADIOL CONGENERS; ETHINYL ESTRADIOL; FEMALE; HUMANS; HYDROXYLATION; IMMUNOHISTOCHEMISTRY; LIVER; MIXED FUNCTION OXYGENASES; PREDICTIVE VALUE OF TESTS; REPRODUCIBILITY OF RESULTS; SWINE; TESTOSTERONE; TIME FACTORS;

ANIMALIA; SUS SCROFA;

EID: 0030722057     PISSN: 00092797     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0009-2797(97)00077-X     Document Type: Conference Paper

References (40)

1. G.T. McInnes, M.J. Brodie, Drug interactions that matter. A critical reappraisal, Drugs 36 (1988) 83-110.
2. Y. Choi, K. Thrasher, E.E. Wer, L.J. Sholiton, C. Olinger, Effect of diphenylhydantoin on cortisol kinetics in humans, Pharmacol. Exp. Ther. 176 (1971) 27-34.
3. N. Haque, K. Thrasher, E.E. Werk, M.C. Knowles, L.J. Sholiton, Studies on dexamethasone metabolism in man: effect of diphenylhydantoin, J. Clin. Endocrinol. Metab. 34 (1972) 44-50.
4. D.M. Edwards, R.J. Courtenay-Evans, J.M. Galley, J. Hunter, A.D. Tait, Changes in cortisol metabolism following rifampicin therapy, Lancet 2 (1974) 549-551.
5. M.R. Stjernholm, F.H. Katz, Effects of diphenylhydantoin, phenobarbital and diazepam on the metabolism of methylprednisolone and its sodium succinate, J. Clin. Endocrinol. Metab. 41 (1975) 196-204.
6. S.J. Wassner, A.J. Pennisi, M.H. Malekzadeh, R.N. Fine, The adverse effect of anticonvulsant therapy on renal allograft survival, J. Paediatr. 88 (1976) 134-137.
7. T.J. Wadhwa, A.J. Schroeder, S.A. Pesce, C.W. Myre, C.W. Clardy, M.R. First, Cyclosporin drug interactions: a review, Ther. Drug Monit. 9 (1987) 399-406.
8. D.J. Back, M.L'E. Orme, Pharmacokinetic drug interactions with oral contraceptives, Clin. Pharmacokinet. 18 (1990) 472-484.
9. F.P. Guengerich, Oxidation of 17α-ethynylestradiol by human liver cytochrome P-450, Mol. Pharmacol. 33 (1988) 500-508.
10. D. Janz, D. Schmidt, Anti-epileptic drugs and failure of oral contraceptives, Lancet 1 (1974) 1113.
11. H.M. Bolt, M. Bolt, H. Kappus, Interactions of rifampicin treatment with pharmacokinetics and metabolism of ethinyloestradiol in man, Acta endocrinol. 85 (1977) 189-197.
12. A.M. Breckenridge, D.J. Back, F.E. Crawford, M. MacIver, M. ĹE Orme, B.K. Park, P.H.Y. Rowe, E. Smith, Drug interactions with contraceptive steroids, in: R.W. Estabrook, E. Lindenlaub (Eds.), The Induction of Drug Metabolism, vol. 14, Schattauer Verlag, New York, 1978, pp. 607-713.
13. M.P. Diamond, J.W. Greene, J.M. Thompson, J.E. Vanttooydonk, A. Wentz, Interaction of anticonvulsants and oral contraceptives in epileptic adolescents, Contraception 31 (1985) 623-632.
14. P. Crawford, D.J. Chadwick, C. Martin, J. Tjia, D.J. Back, M. Orme, The interaction of phenytoin and carbamazepine with combined oral contraceptives, Br. J. Clin. Pharmacol. 30 (1990) 892-896.
15. H.M. Bolt, H. Kappus, M. Bolt, Effect of rimapicin treatment on the metabolism of oestradiol and 17α-ethinyloestradiol by human liver microsomes, Eur. J. Clin. Pharmacol. 8 (1975) 301-307.
16. 3H]17α-ethynylestradiol in women, Xenobiotica 13 (7) (1983) 421-431.
17. B.K. Park, J.L. Maggs, Interindividual variation in the metabolism of ethynylestradiol, Prog. Clin. Biol. Res. 214 (1986) 289-302.
18. L. Pichard, I. Fabre, G. Fabre, J. Domergue, B.S. Aubert, G. Mourad, P. Maurel, Cyclosporin A drug interactions: screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes. Drug Metab. Dispos. 18 (5) (1990) 595-606.
19. M.T. Donato, J.V. Castell, M.J. Gómez-Lechón, Effect of model inducers on cytochrome P450 activities of human hepatocytes in primary culture, Drug Metab. Dispos. 23 (5) (1995) 553-558.
20. T.A. Kocarek, E.G. Schuetz, S. Strom, R.A. Fisher, P.S. Guzelian, Comparative analysis of cytochrome P450 3A induction in primary cultures of rat, rabbit, and human hepatocytes, Drug Metab. Dispos. 23 (3) (1995) 415-421.
21. S.A. Wrighton, E.G. Shuetz, P.B. Watkins, P. Maurel, J. Barwick, B.S. Bailey, H. Hartle, B. Young, P. Guzelian, Demonstration in multiple species of inducible hepatic cytochrome P-450 and their mRNAs related to the glucocorticoid-inducible cytochrome P-450 of the rat, Mol. Pharmacol. 28 (1985) 312-321.
22. A.K. Olsen, C. Friis, K.T. Hansen, Identification of the rabbit and pig liver cytochrome P450 enzymes responsible for the formation of the 2-hydroxy metabolite and 17α-ethynylestradiol, Pharmacol. Toxicol. (unpublished).
23. M. Monshouwer, R.F. Witkamp, S.M. Nijmeijer, J.G. van Amsterdam, A.S.J.P.A.A. van Miert, Suppresion of cytochrome P450-and UDP glucuronosyl transferase dependent enzyme activities by pro-inflammatory cytokines and possible role of nitric oxide in primary cultures of pig hepatocytes, Toxicol. Appl. Pharmacol. 137 (1996) 237-244.
24. T. Omura, R. Sato, The carbon monoxide-binding pigment of liver microsomes. II. Solubilization, purification and properties, J. Biol. Chem. 239 (1964) 2379-2385.
25. G.L. Peterson, A simplification of the protein assay method of Lowry et al. which is more generally applicable, Anal. Biochem. 83 (1977) 346-356.
26. 3H]17α-ethynylestradiol and metabolites in rabbits and pigs following rifampicin and β-naphthoflavone, Pharmacol. Toxicol. (unpublished).
27. D. Larrey, C. Funck-Brentano, P. Breil, J. Vitaux, C. Theodore, G. Babany, D. Pessayre, Effects of erythromycin on hepatic drug-metabolizing enzymes in humans, Biochem. Pharmacol. 32 (6) (1983) 1063-1068.
28. P.B. Watkins, S.A. Wrighton, P. Maurel, E.G. Schuetz, G. Mendez-Picon, G.A. Parker, P.S. Guzelian, Identification of an inducible form of cytochrome P-450 in human liver, Proc. Natl. Acad. Sci. USA 82 (1985) 6310-6314.
29. D. Pessayre, V. Descatoire, M. KonstantinovaMitcheve, J.C. Wandsheer, B. Cober, R. Level, J.P. Benhamou, M. Jaouen, D. Mansuy, Selfinduction by triacetyloleandomycin of its own transformation into a metabolite forming a stable 456 nm absorbing complex with cytochrome P450, Biochem. Pharmacol. 30 (1981) 553-558.
30. D. Larrey, M. Tinel, D. Pessayre, Formation of inactive cytochrome P-450 Fe(II)-metabolite complexes with several erythromycin derivatives but not with josamycin and midecamycin in rats, Biochem. Pharmacol. 32 (1983) 1487-1493.
31. J. Combalbert, I. Fabre, G. Fabre, I. Dalet, J. Derancorut, J.P. Cano, P. Maurel, Metabolism of cyclosporin A. IV. Purification and identification of the the rifampicin-inducible human liver cytochrome P-450 (cyclosporin A oxidase) as a product of P-450IIIA gene subfamily, Drug Metab. Dispos. 17 (1989) 197-207.
32. D.J. Birkett, J.O. Miner, J. Attwood, Evidence for a dual action of sulphinpyrazone on drug metabolism in man: theophylline-sulphinpyrazone interaction, Br. J. Clin. Pharmacol. 15 (1983) 567-569.
33. P. Crawford, D. Chadwick, P. Cleland, J. Tjia, A. Cowie, D.J. Bach, M.L'E. Orme, The lack of effect of sodium vasproate on the pharmacokinetics of oral contraceptive steroids, Contraception 33 (1986) 51-59.
34. L. Vernillet, P. Bertault-Peres, Y. Berland, J. Barradas, A. Durand, M. Olmer, Lack of effect of spiramycin on cyclosporin pharmacokinetics, Br. J. Clin. Pharmacol. 27 (1989) 789-794.
35. L. Pichard, I. Fabre, M. Daujat, J. Domergue, J. Joyeux, P. Maurel, Effect of corticosteroids on the expression of cytochromes P450 and on cyclosporin A oxidase activity in primary cultures of human hepatocytes, Mol. Pharmacol. 41 (1992) 1047-1055.
36. E.G. Schuetz, J.D. Schuetz, S.C. Strom, M.T. Thompson, R. Fisher, D.T. Molowa, D. Li, P.S. Guzelian, Regulation of human liver cytochromes P-450 in family 3A in primary and continuous culture of human hepatocytes, Hepatology 18 (1993) 1254-1262.
37. P.B. Watkins, S.A. Murray, L.G. Winkelman, D.M. Heuman, S.A. Wrighton, P.S. Guzelian, Identification of an inducible form of cytochrome P-450 in human liver, Proc. Nat. Acad. Sci. USA 82 (1989) 688-697.
38. B. Saad, H. Thomas, H. Schawalder, F. Waechter, P. Maier, Oxygen tension, insulin, and glucagon affect the preservation and induction of cytochrome P450 isoforms in cultured rat hepatocytes, Toxicol. Appl. Pharmacol. 126 (1994) 372-379.
39. P.C. Lee, S.L. Werlin, The induction of hepatic cytochrome P450 3A in rats: effect of age, Proc. Soc. Exp. Biol. Med. 210 (1995) 134-139.
40. A.P. Li, D.L. Kaminski, A. Rasmussen, Substrates of human hepatic cytochrome P450 3A4, Toxicology 104 (1995) 1-8.