In vitro approaches to predicting drug interactions in vivo

Biochemical Pharmacology

Volumn 55, Issue 2, 1998, Pages 113-122

  Von Moltke, L L ^a   Greenblatt, D J ^a   Schmider, J ^a   Wright, C E ^a   Harmatz, J S ^a   Shader, R I ^a  

^a TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Chemical inhibition; Cytochromes P450; Drug interactions; In vitro metabolism; Scaling

Indexed keywords

ALPRAZOLAM; ALPRENOLOL; AMIODARONE; AMITRIPTYLINE; ANTIFUNGAL AGENT; BENZODIAZEPINE DERIVATIVE; CYCLOSPORIN; CYTOCHROME P450; DESIPRAMINE; ERYTHROMYCIN; FLUOXETINE; FLUPHENAZINE; FLUVOXAMINE; IMIPRAMINE; ITRACONAZOLE; KETOCONAZOLE; MIDAZOLAM; NEUROLEPTIC AGENT; NIFEDIPINE; NORFLUOXETINE; NORSERTRALINE; NORTRIPTYLINE; PAROXETINE; SEROTONIN UPTAKE INHIBITOR; SERTRALINE; TERFENADINE; TRIAZOLAM;

ANIMAL TISSUE; DRUG INTERACTION; DRUG METABOLISM; HUMAN; HUMAN TISSUE; IN VITRO STUDY; LIVER MICROSOME METABOLISM; MODEL; MOUSE; PLASMA PROTEIN BINDING; PREDICTION; PRIORITY JOURNAL; RAT; REVIEW;

EID: 0031974059     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(97)00239-6     Document Type: Article

References (107)

1. PH Beaune FP Guengerich Human drug metabolism in vitro Pharmacol Ther 37 1988 193 211
2. DJ Birkett PI Mackenzie ME Veronese JO Miners In vitro approaches can predict human drug metabolism Trends Pharmacol Sci 14 1993 292 294
3. K Brøsen Recent developments in hepatic drug oxidation Implications for clinical pharmacokinetics Clin Pharmacokinet 18 1990 220 239
4. FJ Gonzalez Human cytochromes P450 Problems and prospects Trends Pharmacol Sci 13 1992 346 352
5. FP Guengerich Human cytochrome P-450 enzymes Life Sci 50 1992 1471 1478
6. TA Ketter DA Flockhart RM Post KD Denicoff PJ Pazzaglia LB Marangell MS George AM Callahan The emerging role of cytochrome P450 3A in psychopharmacology J Clin Psychopharmacol 15 1995 387 398
7. M Murray P450 enzymes Inhibition mechanisms, genetic regulation and effects of liver disease Clin Pharmacokinet 23 1992 132 146
8. A Parkinson An overview of current cytochrome P450 technology for assessing the safety and efficacy of new materials Toxicol Pathol 24 1996 45 57
9. AD Rodrigues Use of in vitro human metabolism studies in drug development Biochem Pharmacol 48 1994 2147 2156
10. PB Watkins Role of cytochrome P450 in drug metabolism and hepatotoxicity Semin Liver Dis 10 1990 235 250
11. SA Wrighton JC Stevens The human hepatic cytochromes P450 involved in drug metabolism Crit Rev Toxicol 22 1992 1 21
12. PK Honig DC Wortham K Zamani DP Conner JC Mullin LR Cantilena Terfenadine–ketoconazole interaction Pharmacokinetic and electrocardiographic consequences J Am Med Assoc 269 1993 1513 1518
13. TD Leemann P Dayer Quantitative prediction of in vivo drug metabolism and interactions from in vitro data GM Pacifici GN Fracchia Advances in Drug Metabolism in Man 1995 The European Commission Luxembourg 783 830
14. AR Boobis Prediction of inhibitory drug–drug interactions by studies in vitro GM Pacifici GN Fracchia Advances in Drug Metabolism in Man 1995 The European Commission Luxembourg 513 539
15. GT Tucker The rational selection of drug interaction studies Implications of recent advances in drug metabolism Int J Clin Pharmacol Ther Toxicol 30 1992 550 553
16. Segel IH, Enzyme Kinetics . Wiley, New York, 1975.
17. K Brøsen E Skjelbo BB Rasmussen HE Poulsen S Loft Fluvoxamine is a potent inhibitor of cytochrome P4501A2 Biochem. Pharmacol 45 1993 1211 1214
18. LL von Moltke DJ Greenblatt SX Duan J Schmider L Kudchadker SM Fogelman JS Harmatz RI Shader Phenacetin O -deethylation by human liver microsomes in vitro Inhibition by chemical probes, SSRI antidepressants, nefazodone and venlafaxine Psychopharmacology 128 1996 398 407
19. Y-F Ueng T Kuwabara Y-J Chun FP Guengerich Cooperativity in oxidations catalyzed by cytochrome P450-3A4 Biochemistry 36 1997 370 381
20. M Shou J Grogan JA Mancewicz KW Krausz FJ Gonzalez HV Gelboin KR Korzekwa Activation of CYP3A4 Evidence for the simultaneous binding of two substrates in a cytochrome P450 active site Biochemistry 33 1994 6450 6455
21. J Schmider DJ Greenblatt JS Harmatz RI Shader Enzyme kinetic modelling as a tool to analyse the behaviour of cytochrome P450 catalysed reactions Application to amitriptyline N-demethylation Br J Clin Pharmacol 41 1996 593 604
22. J Schmider DJ Greenblatt LL von Moltke JS Harmatz RI Shader N-Demethylation of amitriptyline in vitro Role of cytochrome P-450 3A (CYP3A) isoforms and effect of metabolic inhibitors J Pharmacol Exp Ther 275 1995 592 597
23. T Andersson JO Miners ME Veronese DJ Birkett Diazepam metabolism by human liver microsomes is mediated by both S -mephenytoin hydroxylase and CYP3A isoforms Br J Clin Pharmacol 38 1994 131 137
24. LL von Moltke DJ Greenblatt J Schmider SX Duan CE Wright JS Harmatz RI Shader Midazolam hydroxylation by human liver microsomes in vitro Inhibition by fluoxetine, norfluoxetine, and by azole antifungal agents J Clin Pharmacol 36 1996 783 791
25. A Ghosal H Satoh PE Thomas E Bush D Moore Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cDNA-expressed human cytochrome P450 Drug Metab Dispos 24 1996 940 947
26. T Kronbach D Mathys M Umeno FJ Gonzalez UA Meyer Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4 Mol Pharmacol 36 1989 89 96
27. JB Houston Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance Biochem Pharmacol 47 1994 1469 1479
28. DJ Back JF Tjia Comparative effects of the antimycotic drugs ketoconazole, fluconazole, itraconazole and terbinafine on the metabolism of cyclosporin by human liver microsomes Br J Clin Pharmacol 32 1991 624 626
29. JS Harmatz DJ Greenblatt Falling off the straight line Some hazards of correlation and regression J Clin Psychopharmacol 12 1992 75 78
30. RB Barlow Effects of ‘rogue’ points on non-linear fitting Trends Pharmacol Sci 14 1993 399 403
31. JR Halpert Structural basis of selective cytochrome P450 inhibition Annu Rev Pharmacol Toxicol 35 1995 29 53
32. RB Silverman Mechanism-based enzyme inactivators Methods Enzymol 249 1992 241 282
33. von Moltke LL, Greenblatt DJ, Schmider J, Harmatz JS and Shader RI, Metabolism of drugs by cytochrome P450 3A isoforms. Clin Pharmacokinet 29 (Suppl 1) : 33–44, 1995.
34. GR Wilkinson Clearance approaches in pharmacology Pharmacol Rev 39 1987 1 47
35. GR Wilkinson DG Shand A physiological approach to hepatic drug clearance Clin Pharmacol Ther 18 1975 377 390
36. SA Wrighton BJ Ring Inhibition of human CYP3A catalyzed 1′-hydroxy midazolam formation by ketoconazole, nifedipine, erythromycin, cimetidine, and nizatidine Pharm Res 11 1994 921 924
37. KT Olkkola K Aranko H Luurila A Hiller L Saarnivaara J-J Himberg PJ Neuvonen A potentially hazardous interaction between erythromycin and midazolam Clin Pharmacol Ther 53 1993 298 305
38. H Echizen H Kawasaki K Chiba M Tani T Ishizaki A potent inhibitory effect of erythromycin and other macrolide antibiotics on the mono-N-dealkylation metabolism of disopyramide with human liver microsomes J Pharmacol Exp Ther 264 1993 1425 1431
39. KS Pang M Rowland TN Tozer In vivo evaluation of Michaelis–Menten constants of hepatic drug-eliminating systems Drug Metab Dispos 6 1978 197 200
40. AK Mitra KE Thummel TF Kalhorn ED Kharasch JD Unadkat JT Slattery Inhibition of sulfamethoxazole hydroxylamine formation by fluconazole in human liver microsomes and healthy volunteers Clin Pharmacol Ther 59 1996 332 340
41. KL Kunze WF Trager Warfarin–fluconazole III. A rational approach to management of a metabolically based drug interaction Drug Metab Dispos 24 1996 429 435
42. CM Ervine DE Matthew B Brennan JB Houston Comparison of ketoconazole and fluconazole as cytochrome P450 inhibitors Drug Metab Dispos 24 1996 211 215
43. BJ Ring SN Binkley L Roskos SA Wrighton Effect of fluoxetine, norfluoxetine, sertraline and desmethyl sertraline on human CYP3A catalyzed 1′-hydroxy midazolam formation in vitro J Pharmacol Exp Ther 275 1995 1131 1135
44. GM Pacifici A Viani Methods of determining plasma and tissue binding of drugs Pharmacokinetic consequences Clin Pharmacokinet 23 1992 449 468
45. H Kurz B Fichtl Binding of drugs to tissues Drug Metab Rev 14 1983 467 510
46. M Tsuru RR Erickson JL Holtzman The metabolism of phenytoin by isolated hepatocytes and hepatic microsomes from male rats J Pharmacol Exp Ther 222 1982 658 661
47. MA Bogeyevitch EMJ Gillam PEB Reilly DJ Winzor Physical partitioning as the major source of metoprolol uptake by hepatic microsomes Biochem Pharmacol 36 1987 4167 4168
48. S Miyauchi Y Sawada T Iga M Hanano Y Sugiyama Comparison of the hepatic uptake clearances of fifteen drugs with a wide range of membrane permeabilities in isolated rat hepatocytes and perfused rat livers Pharm Res 10 1993 434 440
49. C-H Chou AM Evans G Fornasini M Rowland Relationship between lipophilicity and hepatic dispersion and distribution for a homologous series of barbiturates in the isolated perfused in situ rat liver Drug Metab Dispos 21 1993 933 938
50. G Schuhmann B Fichtl H Kurz Prediction of drug distribution in vivo on the basis of in vitro binding data Biopharm Drug Dispos 8 1987 73 86
51. p,f) of quinidine in rats J Pharm Pharmacol 36 1984 340 342
52. JH Lin Y Sugiyama S Awazu M Hanano In vitro and in vivo evaluation of the tissue-to-blood partition coefficient for physiological pharmacokinetic models J Pharmacokinet Biopharm 10 1982 637 647
53. DJ Greenblatt LL von Moltke J Schmider JS Harmatz RI Shader Inhibition of human cytochrome P450-3A isoforms by fluoxetine and norfluoxetine In vitro and in vivo studies J Clin Pharmacol 36 1996 792 798
54. M Aravagiri SR Marder A Yuwiler KK Midha NS Kula RJ Baldessarini Distribution of fluphenazine and its metabolites in brain regions and other tissues of the rat Neuropsychopharmacology 13 1995 235 247
55. JM Scavone H Friedman DJ Greenblatt RI Shader Effect of age, body composition, and lipid solubility on benzodiazepine tissue distribution in rats Arzeneimittelforschung 37 1987 2 6
56. X Xie SH Steiner MH Bickel Kinetics of distribution and adipose tissue storage as a function of lipophilicity and chemical structure II. Benzodiazepines Drug Metab Dispos 19 1991 15 19
57. KE Ferslew AN Hagardorn WF McCormick Postmortem determination of the biological distribution of sufentanil and midazolam after an acute intoxication J Forensic Sci 34 1989 249 257
58. SA Jortani JC Valentour A Poklis Thioridazine enantiomers in human tissues Forensic Sci Int 64 1994 165 170
59. BS Levine S-C Wu BA Goldberger YH Caplan Two fatalities involving haloperidol J Anal Toxicol 15 1991 282 284
60. H Friedman HR Ochs DJ Greenblatt RI Shader Tissue distribution of diazepam and its metabolite desmethyldiazepam A human autopsy study J Clin Pharmacol 25 1985 613 615
61. RJ Wong The determination of the trizolobenzodiazepine triazolam in post mortem samples J Anal Toxicol 8 1984 10 13
62. B Levine AJ Jenkins JE Smialek Distribution of sertraline in postmortem cases J Anal Toxicol 18 1994 272 274
63. DN Bailey RF Shaw Interpretation of blood and tissue concentrations in fatal self-ingested overdose involving amitriptyline An update (1978–1979) J Anal Toxicol 4 1980 232 236
64. K Worm B Kringsholm A Steentoft Clozapine cases with fatal, toxic or therapeutic concentrations Int J Legal Med 106 1993 115 118
65. AD Fraser AF Isner RA Perry Distribution of trimipramine and its major metabolites in a fatal overdose case J Anal Toxicol 11 1987 168 170
66. T Hilberg J Morland A Bjorneboe Postmortem release of amitriptyline from the lungs; a mechanism of postmortem drug redistribution Forensic Sci Int 64 1994 47 55
67. GR Jones DJ Pounder Site dependence of drug concentrations in postmortem blood—A case study J Anal Toxicol 11 1987 186 190
68. T Hilberg A Bugge K-M Beylich J Ingum A Bjørneboe J Mørland An animal model of postmortem amitriptyline redistribution J Forensic Sci 38 1993 81 90
69. T Hilberg A Bugge K-M Beylich J Mørland A Bjørneboe Diffusion as a mechanism of postmortem drug redistribution An experimental study in rats Int J Legal Med 105 1992 87 91
70. DJ Morgan RA Smallwood Clinical significance of pharmacokinetic models of hepatic elimination Clin Pharmacokinet 18 1990 61 76
71. SM Pond TN Tozer First-pass elimination Basic concepts and clinical consequences Clin Pharmacokinet 9 1984 1 25
72. JC Kolars P Schmiedlin-Ren JD Schuetz C Fang PB Watkins Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes J Clin Invest 90 1992 1871 1878
73. KS Lown JC Kolars KE Thummel JL Barnett KL Kunze SA Wrighton PB Watkins Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel Lack of prediction by the erythromycin breath test Drug Metab Dispos 22 1994 947 955
74. MF Paine DD Shen KL Kunze JD Perkins CL Marsh JP McVicar DM Barr BS Gillies KE Thummel First-pass metabolism of midazolam by the human intestine Clin Pharmacol Ther 60 1996 14 24
75. KE Thummel D O’Shea MF Paine DD Shen KL Kunze JD Perkins GR Wilkinson Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism Clin Pharmacol Ther 59 1996 491 502
76. MF Hebert JP Roberts T Pruesksaritanont LZ Benet Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction Clin Pharmacol Ther 52 1992 453 457
77. DY Gomez VJ Wacher SJ Tomlanovich MF Hebert LZ Benet The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine Clin Pharmacol Ther 58 1995 15 19
78. JA Como WE Dismukes Oral azole drugs as systemic antifungal therapy N Engl J Med 330 1994 263 272
79. J Heykants M Michiels W Meuldermans J Monbaliu K Lavrijsen A Van Peer JC Levron R Woestenborghs G Cauwenbergh The pharmacokinetics of itraconazole in animals and man An overview RA Fromtling Recent Trends in the Discovery, Development and Evaluation of Antifungal Agents 1987 J. R. Prous Science Publishers, S. A Barcelona 223 249
80. CM Riley MO James Determination of ketoconazole in the plasma, liver, lung, and adrenal of the rat by high-performance liquid chromatography J Chromatogr 377 1986 287 294
81. D Matthew B Brennan K Zomorodi JB Houston Disposition of azole antifungal agents. I. Nonlinearities in ketoconazole clearance and binding in rat liver Pharm Res 10 1993 418 422
82. LL von Moltke DJ Greenblatt JS Harmatz SX Duan LM Harrel MM Cotreau-Bibbo GA Pritchard CE Wright RI Shader Triazolam biotransformation by human liver microsomes in vitro Effects of metabolic inhibitors and clinical confirmation of a predicted interaction with ketoconazole J Pharmacol Exp Ther 276 1996 370 379
83. KT Olkkola JT Backman PJ Neuvonen Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole Clin Pharmacol Ther 55 1994 481 485
84. A Varhe KT Olkkola PJ Neuvonen Oral triazolam is potentially hazardous to patients receiving systemic antimycotics ketoconazole or itraconazole Clin Pharmacol Ther 56 1994 601 607
85. LL von Moltke DJ Greenblatt SX Duan JS Harmatz RI Shader In vitro prediction of the terfenadine–ketoconazole pharmacokinetic interaction J Clin Pharmacol 34 1994 1222 1227
86. LL von Moltke DJ Greenblatt MM Cotreau-Bibbo JS Harmatz RI Shader Inhibitors of alprazolam metabolism in vitro Effect of serotonin-reuptake-inhibitor antidepressants, ketoconazole and quinidine Br J Clin Pharmacol 38 1994 23 31
87. CE Wright DJ Greenblatt LL von Moltke BL Ehrenberg JS Harmatz K Corbett RI Shader Ketoconazole inhibition of triazolam and alprazolam clearance Differential kinetic and dynamic consequences Clin Pharmacol Ther 61 1997 183
88. K-M Lin JK Lau R Smith P Phillips E Antal RE Poland Comparison of alprazolam plasma levels in normal Asian and Caucasian male volunteers Psychopharmacology 96 1988 365 369
89. RB Smith PD Kroboth JT Vanderlugt JP Phillips RP Juhl Pharmacokinetics and pharmacodynamics of alprazolam after oral and IV administration Psychopharmacology 84 1984 452 456
90. J Ahonen KT Olkkola PJ Neuvonen Effect of itraconazole and terbinafine on the pharmacokinetics and pharmacodynamics of midazolam in healthy volunteers Br J Clin Pharmacol 40 1995 270 272
91. KT Olkkola J Ahonen PJ Neuvonen The effect of the systemic antimycotics, itraconazole and fluconazole, on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam Anesth Analg 82 1996 511 516
92. C von Bahr E Spina C Birgersson Ö Ericsson M Göransson T Henthorn F Sjöqvist Inhibition of desmethylimipramine 2-hydroxylation by drugs in human liver microsomes Biochem Pharmacol 34 1985 2501 2505
93. S Ohmori S Takeda T Rikihisa M Kiuchi Y Kanakubo M Kitada Studies on cytochrome P450 responsible for oxidative metabolism of imipramine in human liver microsomes Biol Pharm Bull 16 1993 571 575
94. LL von Moltke DJ Greenblatt MM Cotreau-Bibbo SX Duan JS Harmatz RI Shader Inhibition of desipramine hydroxylation in vitro by serotonin-reuptake-inhibitor antidepressants, and by quinidine and ketoconazole A model system to predict drug interactions in vivo J Pharmacol Exp Ther 268 1994 1278 1283
95. LL von Moltke DJ Greenblatt MH Court SX Duan JS Harmatz RI Shader Inhibition of alprazolam and desipramine hydroxylation in vitro by paroxetine and fluvoxamine Comparison with other selective serotonin reuptake inhibitor antidepressants J Clin Psychopharmacol 15 1995 125 131
96. RI Shader LL von Moltke J Schmider JS Harmatz DJ Greenblatt The clinician and drug interactions—An update J Clin Psychopharmacol 16 1996 197 201
97. RF Bergstrom AL Peyton L Lemberger Quantification and mechanism of the fluoxetine and tricyclic antidepressant interaction Clin Pharmacol Ther 51 1992 239 248
98. SH Preskorn J Alderman M Chung W Harrison M Messig S Harris Pharmacokinetics of desipramine coadministered with sertraline or fluoxetine J Clin Psychopharmacol 14 1994 90 97
99. J Alderman SH Preskorn DJ Greenblatt W Harrison D Penenberg J Allison M Chung Desipramine pharmacokinetics when coadministered with paroxetine or sertraline in extensive metabolizers J Clin Psychopharmacol 17 1997 284 291
100. K Brøsen JG Hansen KK Nielsen SH Sindrup LF Gram Inhibition by paroxetine of desipramine metabolism in extensive but not in poor metabolizers of sparteine Eur J Clin Pharmacol 44 1993 349 355
101. TA Lasher JC Fleishaker RC Steenwyk EJ Antal Pharmacokinetic pharmacodynamic evaluation of the combined administration of alprazolam and fluoxetine Psychopharmacology 104 1991 323 327
102. DJ Greenblatt SH Preskorn MM Cotreau WD Horst JS Harmatz Fluoxetine impairs clearance of alprazolam but not of clonazepam Clin Pharmacol Ther 52 1992 479 486
103. JC Fleishaker LK Hulst A pharmacokinetic and pharmacodynamic evaluation of the combined administration of alprazolam and fluvoxamine Eur J Clin Pharmacol 46 1994 35 39
104. LL von Moltke DJ Greenblatt SX Duan JS Harmatz CE Wright RI Shader Inhibition of terfenadine metabolism in vitro by azole antifungal agents and by selective serotonin reuptake inhibitor antidepressants Relation to pharmacokinetic interactions in vivo J Clin Psychopharmacol 16 1996 104 112
105. DE Martin B Zussman DE Everitt LJ Benincosa R Etheredge DK Jorkasky No effect of paroxetine (P) on the cardiac safety and PK of terfenadine (T) J Clin Pharmacol 36 1996 849
106. CE Wright TA Lasher-Sisson RC Steenwyk CN Swanson A pharmacokinetic evaluation of the combined administration of triazolam and fluoxetine Pharmacotherapy 12 1992 103 106
107. BB Rasmussen J Mäenpää O Pelkonen S Loft HE Poulsen JL Lykkesfeldt K Brøsen Selective serotonin reuptake inhibitors and theophylline metabolism in human liver microsomes Potent inhibition by fluvoxamine Br J Clin Pharmacol 39 1995 151 159