Effect of dexamethasone on the intestinal first-pass metabolism of indinavlr in rats: Evidence of cytochrome P-450 a and P-glycoprotein induction

Drug Metabolism and Disposition

Volumn 27, Issue 10, 1999, Pages 1187-1193

  Lin, Jiunn H ^a   Chiba, Masato ^a   Chen, I Wu ^a   Nishime, Joy A ^a   Deluna, Florencia A ^a   Yamazaki, Masayo ^a   Lin, Yuh J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450; DEXAMETHASONE; GLYCOPROTEIN P; INDINAVIR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BIOAVAILABILITY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG EFFECT; DRUG POTENCY; ENZYME SUBSTRATE; FIRST PASS EFFECT; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; INTESTINE MUCOSA; LIVER METABOLISM; LIVER PARENCHYMA; NONHUMAN; PRIORITY JOURNAL; PROTEIN INDUCTION; RAT;

ANIMALS; ANTI-HIV AGENTS; ARYL HYDROCARBON HYDROXYLASES; BLOTTING, WESTERN; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 ENZYME SYSTEM; DEXAMETHASONE; INDINAVIR; INTESTINES; LIVER; MALE; OXIDOREDUCTASES, N-DEMETHYLATING; P-GLYCOPROTEIN; RATS; RATS, SPRAGUE-DAWLEY;

EID: 0032844759     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (36)

1. Benet LZ, Wu CY, Hebert MF and Wacher VJ (1996) Intestinal drug metabolism and antitransport process: A potential shift in oral drug delivery. J Control Release 39:139-143.
2. Bonn P, Frankhuijzen-Sierevogel A and Noordhoek J (1982) Time and dose dependence of 3-methylcholanthrene-induced metabolism in rat intestinal mucosal cells and microsomes. Biochem Pharmacol 31:3707-3710.
3. Boxenbaum H (1980) Interspecies variation in liver weight, hepatic blood flow and antipyrine intrinsic clearance in extrapolation of data to benzodiazepines and phenytoin. J Pharmacokinet Biopharm 8:165-176
4. Chen I-W, Vastag KJ and Lin JH (1995) High-performance liquid chromatographic determination of a potent and selective HIV protease inhibitor (L-735,524) in rat, dog and monkey plasma. J Chromatogr 672:111-117.
5. Chiba M, Hensleigh M and Lin JH (1997) Hepatic and intestinal metabolism of indinavir, an HIV protease inhibitor, in rat and human microsomes. Biochem Pharmacol 53:1187-1195.
6. Fromm MF, Busse D, Kroemer HK and Eichelbaum M (1996) Differential induction of prehepatic and hepatic metabolism of verapamil by rifampin. Hepatology 24:796-801.
7. Gan L-SL, Moseley A, Khosla B, Augustijns PF, Bradshaw TP, Hendren RW and Thakker DR (1996) CYP3A-like cytochrome P450-mediated metabolism and polarized efflux of cyclosporin A in Caco-2 cells: Interaction between the two biochemical barriers to intestinal transport. Drug Metab Dispos 24:344-349.
8. Gant TW, Silverman JA, Bisgaard HC, Burt RK, Marino PA and Thorgeirsson SS (1991) Regulation of 2-acetylaminofluorene and 3-methylcholanthrene-mediated induction of multi-drug resistance and cytochrome P450 IA gene family expression in primary hepatocyte culture and rat liver. Mol Carcinog 4:499-501.
9. Gerlowski LE and Jain RK (1983) Physiologically based pharmacokinetic modeling: Principles and applications. J Pharm Sci 72:1103-1127.
10. Gillette JR and Pang KS (1977) Theoretic aspects of pharmacokinetic drug interaction. Clin Pharmacol Ther 22:627-638.
11. Holtbecker N, Fromm MF, Kroemer HK, Ohnhms EF and Heidemann H (1996) The nifedipinerifampin interaction: Evidence for induction of gut wall metabolism. Drug Metab Dispos 24:1121-1123.
12. Houston JB (1994) Utility of in vitro drug metabolism data in prediction of in vivo metabolic clearance. Biochem Pharmacol 47:1469-1479.
13. Ilett KF, Tee LBG, Reeves PT and Minchin RF (1990) Metabolism of drugs and other xenobiotics in the gut lumen wall. Pharmacol Ther 46:67-93.
14. Kaminsky LS and Fasco MJ (1992) Small intestinal cytochrome P450. Crit Rev Toxicol 21:407-422.
15. Kessler M, Oreste A, Storelli C, Murer H, Muller M and Semenza G (1978) A modified procedure for the rapid preparation of efficiently transporting vesicles from small intestinal brush border membranes. Biochemica et Biophysica Acta 506:136-154.
16. Kim RB, Fromm MF, Wandel C, Leake B, Wood AJJ, Roden DM and Wilkinson GR (1998) The drug transporter p-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J Clin Invest 101:289-294.
17. Klippert P, Borm P and Noordhoek J (1982) Prediction of intestinal first-pass effect of phenacetin in the rat from enzyme kinetic data - Correlation with in vivo data using mucosal blood flow. Biochem Pharmacol 31:2545-2548.
18. Kobayashi K, Sogame Y, Hara H and Hayashi K (1990) Mechanism of glutathione S-conjugate transport in canalicular and basolateral membrane. J Biol Chem 265:7737-7741.
19. Kolars JC, Lown KS, Schmeidlin-Ren P, Ghosh M, Fang C, Wrighton SA, Merion RM and Watkins PB (1994) CYP3A gene expression in human gut epithelium. Pharmacogenetics 4:247-259.
20. Krishna DR and Klotz U (1994) Extrahepatic metabolism of drugs in humans. Clin Pharmacokinet 26:144-150.
21. Laemmli UK (1970) Cleavage of structural proteins during the assembly of the head of bacteriophage T4. Nature (Lond) 227:680-685.
22. Lin JH, Chiba M and Baillie TA (1999) Is the role of the small intestine in first-pass metabolism overemphasized? Pharmacol Rev 51:135-158.
23. Lin JH, Chiba M, Balani SK, Chen I-W, Kwei GYS, Vastag KJ and Nishime JA (1996) Species differences in the pharmacokinetics and metabolism of indinavir, a potent human immunodeficiency virus protease inhibitor. Drug Metab Dispos 24:1111-1120.
24. Paine MF, Shen DD, Kunze KL, Persins JD, Marsh CL, McVicar JP, Barr DM, Gillies BS and Thummel KE (1996) First-pass metabolism of midazolam by the human intestine. Clin Pharmacol Ther 60:14-24.
25. Raeissi SD, Hidalog IJ, Segura-Aguilar J and Artursson P (1999) Interplay between CYP3A-mediated metabolism and polarized efflux of terfenadine and its metabolites in intestinal epithelial Caco-2 (TC7) cell monolayers. Pharm Res 16:625-632.
26. Renwick AG and George CF (1989) Metabolism of xenobiotics in the gastrointestinal tract, in Intermediary Xenobiotic Metabolism in Animals: Methodology, Mechanisms and Significance (Huston DH, Caldwell J and Paulson GD eds) pp 13-40, Taylor & Francis, London.
27. Rocci ML and Jusko WJ (1983) Lagran program for area and moments in pharmaceutic analysis. Comput Programs Biomed 16:203-216.
28. Salphati L and Benet LZ (1998) Modulation of p-glycoprotein expression by cytochrome P450 3A inducers in male and female rat livers. Biochem Pharmacol 55:387-395.
29. Tallarida RJ and Murray RB (1987) Manual of Pharmacologic Calculation with Computer Programs, 2nd ed., Springer-Verlag, New York.
30. Thummel KE, Kunze KL and Shen DD (1997) Enzyme-catalyzed process of first-pass hepatic and intestinal drug extraction. Advanced Drug Delivery Rev 27:99-127.
31. Towbin H, Staehelin T and Gordon J (1979) Electrophoretic transfer of proteins from polyacrylamide gels to nitrocellulose sheets: Procedure and some applications. Proc Natl Acad Sci USA 76:4350-4354.
32. Wacher VJ, Wu CY and Benet LZ (1995) Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and p-glycoprotein: Implications for drug delivery and activity in cancer chemotherapy. Mol Pharmacol 13:129-134.
33. Watkins PB (1997) The barrier function of CYP3A4 and p-glycoprotein in the small bowel. Advanced Drug Delivery Rev 27:161-170.
34. Watkins PB, Wrighton SA, Schuetz EG, Molowa DT and Guzelian PS (1987) Identification of glucocorticoid cytochrome P450 in the intestinal mucosa of rats and man. J Clin Invest 80:1029-1036.
35. Wilkinson GR (1987) Clearance approaches in pharmacology. Pharmacol Rev 39:1-47.
36. Wu CY, Benet LZ, Hebert MF, Gupta SK, Rowland M, Gomez DY and Wacher VJ (1995) Differentiation of absorption and first-pass gut and hepatic metabolism in humans: Studies with cyclosporine. Clin Pharmacol Ther 58:492-497.