A mechanism-based integrated pharmacokinetic enzyme model describing the time course and magnitude of phenobarbital-mediated enzyme induction in the rat

Pharmaceutical Research

Volumn 23, Issue 3, 2006, Pages 521-532

  Magnusson, Mats O ^a   Karlsson, Mats O ^a   Sandström, Rikard ^a  

^a UPPSALA UNIVERSITY   (Sweden)

Author keywords

Induction; Modeling; Nonmem; Phenobarbital; Time course

Indexed keywords

ANDROSTENEDIONE; CYTOCHROME P450 1A2; CYTOCHROME P450 2B1; CYTOCHROME P450 2B2; CYTOCHROME P450 3A1; CYTOCHROME P450 3A2; FENEMAL RECIP; PHENOBARBITAL;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG SPECIFICITY; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME INDUCTION; ENZYME KINETICS; EXPERIMENTAL MODEL; HORMONE SYNTHESIS; IN VITRO STUDY; MALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; ANTICONVULSANTS; ARYL HYDROCARBON HYDROXYLASES; CYTOCHROME P-450 CYP1A2; CYTOCHROME P-450 CYP2B1; CYTOCHROME P-450 ENZYME SYSTEM; CYTOCHROMES; ENZYME INDUCTION; LIVER; MALE; MICROSOMES, LIVER; MODELS, BIOLOGICAL; PHENOBARBITAL; RATS; RATS, SPRAGUE-DAWLEY;

EID: 33644898558     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-005-9571-z     Document Type: Article

References (35)

1. R. H. Levy A. A. Lai M. S. Dumain 1979 Time-dependent kinetics IV: pharmacokinetic theory of enzyme induction J. Pharm. Sci. 68 398 399
2. A. B. Okey 1990 Enzyme induction in the cytochrome P-450 system Pharmacol. Ther. 45 241 298
3. J. Y. Chien K. E. Thummel J. T. Slattery 1997 Pharmacokinetic consequences of induction of CYP2E1 by ligand stabilization Drug Metab. Dispos. 25 1165 1175
4. A. V. Boddy M. Cole A. D. Pearson J. R. Idle 1995 The kinetics of the auto-induction of ifosfamide metabolism during continuous infusion Cancer Chemother. Pharmacol. 36 53 60
5. M. Hassan U. S. Svensson P. Ljungman B. Bjorkstrand H. Olsson M. Bielenstein M. Abdel-Rehim C. Nilsson M. Johansson M. O. Karlsson 1999 A mechanism-based pharmacokinetic-enzyme model for cyclophosphamide autoinduction in breast cancer patients Br. J. Clin. Pharmacol. 48 669 677
6. C. von Bahr E. Steiner Y. Koike J. Gabrielsson 1998 Time course of enzyme induction in humans: effect of pentobarbital on nortriptyline metabolism Clin. Pharmacol. Ther. 64 18 26
7. T. Kerbusch A. D. Huitema J. Ouwerkerk H. J. Keizer R. A. Mathot J. H. Schellens J. H. Beijnen 2000 Evaluation of the autoinduction of ifosfamide metabolism by a population pharmacokinetic approach using nonmem Br. J. Clin. Pharmacol. 49 555 561
8. B. Frame S. L. Beal 1998 Non-steady state population kinetics of intravenous phenytoin Ther. Drug Monit. 20 408 416
9. T. Gordi R. Xie N. V. Huong D. X. Huong M. O. Karlsson M. Ashton 2005 A semiphysiological pharmacokinetic model for artemisinin in healthy subjects incorporating autoinduction of metabolism and saturable first-pass hepatic extraction Br. J. Clin. Pharmacol. 59 189 198
10. E. M. Bomhard U. Schmidt E. Loser 1998 Time course of enzyme induction in liver and kidneys and absorption, distribution and elimination of 1,4-dichlorobenzene in rats Toxicology 131 73 91
11. J. Meijer A. Bergstrand J. W. DePierre 1987 Preparation and characterization of subcellular fractions from the liver of C57B1/6 mice, with special emphasis on their suitability for use in studies of epoxide hydrolase activities Biochem. Pharmacol. 36 1139 1151
12. O. Lowry N. Rosebrough L. Farr R. Randall 1951 Protein measurement with the Folin phenol reagent J. Biol. Chem. 193 265 275
13. K. Kushida K. Chiba T. Ishizaki 1983 Simultaneous liquid chromatographic determination of chloramphenicol and antiepileptic drugs (phenobarbital, phenytoin, carbamazepine, and primidone) in plasma Ther. Drug Monit. 5 127 133
14. I. Leclercq J. P. Desager C. Vandenplas Y. Horsmans 1996 Fast determination of low-level cytochrome P-450 1A1 activity by high-performance liquid chromatography with fluorescence or visible absorbance detection J. Chromatogr., B Biomed. Appl. 681 227 232
15. M. O. Magnusson R. Sandström 2004 Quantitative analysis of eight testosterone metabolites using column switching and liquid chromatography/tandem mass spectrometry Rapid Commun. Mass Spectrom. 18 1089 1094
16. S. L. Bealand and L. S. Sheiner. NONMEM user's guide, NONMEM Project Group, University of California at San Francisco, 1994.
17. E. N. Jonsson M. O. Karlsson 1999 Xpose-an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for nonmem Comput. Methods Programs Biomed. 58 51 64
18. Y. N. Sun D. C. DuBois R. R. Almon N. A. Pyszczynski W. J. Jusko 1998 Dose-dependence and repeated-dose studies for receptor/gene-mediated pharmacodynamics of methylprednisolone on glucocorticoid receptor down-regulation and tyrosine aminotransferase induction in rat liver J. Pharmacokinet. Biopharm. 26 619 648
19. A. D. Rodrigues R. A. Prough 1991 Induction of cytochromes P450IA1 and P450IA2 and measurement of catalytic activities Methods Enzymol. 206 423 431
20. D. J. Waxman 1988 Interactions of hepatic cytochromes P-450 with steroid hormones. Regioselectivity and stereospecificity of steroid metabolism and hormonal regulation of rat P-450 enzyme expression Biochem. Pharmacol. 37 71 84
21. S. Imaoka T. Yamada T. Hiroi K. Hayashi T. Sakaki Y. Yabusaki Y. Funae 1996 Multiple forms of human P450 expressed in Saccharomyces cerevisiae. Systematic characterization and comparison with those of the rat Biochem. Pharmacol. 51 1041 1050
22. A. J. Sonderfan M. P. Arlotto D. R. Dutton S. K. [tmp] McMillen A. Parkinson 1987 Regulation of testosterone hydroxylation by rat liver microsomal cytochrome P-450 Arch. Biochem. Biophys. 255 27 41
23. D. E. Ryan W. Levin 1990 Purification and characterization of hepatic microsomal cytochrome P-450 Pharmacol. Ther. 45 153 239
24. D. J. Waxman A. Ko C. Walsh 1983 Regioselectivity and stereoselectivity of androgen hydroxylations catalyzed by cytochrome P-450 isozymes purified from phenobarbital-induced rat liver J. Biol. Chem. 258 11937 11947
25. A. Parkinson P. E. Thomas D. E. Ryan W. Levin 1983 The in vivo turnover of rat liver microsomal epoxide hydrolase and both the apoprotein and heme moieties of specific cytochrome P-450 isozymes Arch. Biochem. Biophys. 225 216 236
26. A. W. Wood D. C. Swinney P. E. Thomas D. E. Ryan P. F. Hall W. Levin W. A. Garland 1988 Mechanism of androstenedione formation from testosterone and epitestosterone catalyzed by purified cytochrome P-450b J. Biol. Chem. 263 17322 17332
27. K. Kobayashi K. Urashima N. Shimada K. Chiba 2002 Substrate specificity for rat cytochrome P450 (CYP) isoforms: screening with cDNA-expressed systems of the rat Biochem. Pharmacol. 63 889 896
28. W. Levin P. E. Thomas D. E. Ryan A. W. Wood 1987 Isozyme specificity of testosterone 7 alpha-hydroxylation in rat hepatic microsomes: is cytochrome P-450a the sole catalyst? Arch. Biochem. Biophys. 258 630 635
29. D. J. Waxman N. A. Pampori P. A. Ram A. K. Agrawal B. H. hapiro 1991 Interpulse interval in circulating growth hormone patterns regulates sexually dimorphic expression of hepatic cytochrome P450 Proc. Natl. Acad. Sci. USA 88 6868 6872
30. P. Reidenberg P. Glue C. R. Banfield R. D. Colucci J. W. Meehan E. Radwanski P. Mojavarian C. C. Lin J. Nezamis M. Guillaume M. B. Affrime 1995 Effects of felbamate on the pharmacokinetics of phenobarbital Clin. Pharmacol. Ther. 58 279 287
31. R. Riva F. Albani M. Contin A. Baruzzi 1996 Pharmacokinetic interaction between antiepileptic drugs Clin. Pharmacokinet. 31 470 493
32. G. D. Anderson 1998 A mechanistic approach to antiepileptic drug interactions Ann. Pharmacother. 32 554 563
33. S. G. Paibir W. H. Soine D. F. Thomas R. A. Fisher 2004 Phenobarbital N-glucosylation by human liver microsomes Eur. J. Drug Metab. Pharmacokinet. 29 1 51 59
34. P. Bentley F. Oesch 1982 Foreign compound metabolism in the liver Prog. Liver Dis. 7 157 178
35. I. S. Owens 1977 Genetic regulation of UDP-glucuronosyltransferase induction by polycyclic aromatic compounds in mice. Co-segregation with aryl hydrocarbon (benzo(alpha)pyrene) hydroxylase induction J. Biol. Chem. 252 2827 2833