Validation of the five-drug 'Pittsburgh cocktail' approach for assessment of selective regulation of drug-metabolizing enzymes

Clinical Pharmacology and Therapeutics

Volumn 62, Issue 4, 1997, Pages 365-376

  Frye, Reginald F ^a   Matzke, Gary R ^a   Adedoyin, Adedayo ^a   Porter, James A ^a   Branch, Robert A ^a  

^a UNIVERSITY OF PITTSBURGH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLDAPSONE; ACYLTRANSFERASE; CAFFEINE; CHLORZOXAZONE; CYTOCHROME P450; DAPSONE; DEBRISOQUINE; MEPHENYTOIN; N HYDROXYDAPSONE;

ADULT; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG INTERACTION; DRUG METABOLISM; DRUG MIXTURE; ENZYME ACTIVITY; ENZYME REGULATION; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; REGULATORY MECHANISM; VOLUNTEER;

ADULT; ANALYSIS OF VARIANCE; ARYLAMINE N-ACETYLTRANSFERASE; CAFFEINE; CHLORZOXAZONE; CYTOCHROME P-450 ENZYME SYSTEM; DAPSONE; DEBRISOQUIN; DRUG INTERACTIONS; HUMANS; MALE; MEPHENYTOIN; PHENOTYPE; REFERENCE VALUES;

EID: 0030712276     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0009-9236(97)90114-4     Document Type: Article

References (62)

1. Bauer LA, O'Sullivan T, Reiss WG, Horn JR, Opheim K, Strandness DE, et al. Liver blood flow, antipyrine clearance, and antipyrine metabolite formation clearance in patients with chronic active hepatitis and alcoholic cirrhosis. Br J Clin Pharmacol 1994;37:375-81.
2. WalterSack I, Klotz U. Influence of diet and nutritional status on drug metabolism. Clin Pharmacokinet 1996;31:47-64.
3. Porter TD, Coon MJ. Cytochrome P-450: multiplicity of isoforms, substrates and catalytic and regulatory mechanisms. J Biol Chem 1991;266:13469-72.
4. Shimada T, Yamazaki H, Mimura M, Inui Y, Guengerich FP. Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians. J Pharmacol Exp Ther 1994;270:414-23.
5. Brockmoller J, Roots I. Assessment of liver metabolic function: clinical implications. Clin Pharmacokinet 1994;27:216-18.
6. Branch RA, Chern HD, Adedoyin A, Romkes-Sparks M, Lesnick TG, Persad R, et al. The procarcinogen hypothesis for bladder cancer: activities of individual drug-metabolizing enzymes as risk factors. Pharmacogenetics 1995;5:S97-100.
7. Breimer DD, Schellens JH. A "cocktail" strategy to assess in vivo oxidative drug metabolism in humans. Trends Pharmacol Sci 1990;11:223-5.
8. Breimer DD. Interindividual differences in drug disposition: clinical implications and methods of investigation. Clin Pharmacokinet 1983;8:371-7.
9. Butler MA, Iwasaki M, Guengerich FP, Kadlubar FF. Human cytochrome P-450pa (P-450IA2), the phenacetin O-deethylase, is primarily responsible for the hepatic 3-demethylation of caffeine and N-oxidation of carcinogenic arylamines. Biochemistry 1989;86: 7696-700.
10. Fuhr U, Rost KL. Simple and reliable CYP1A2 phenotyping by the paraxanthine/caffeine ratio in plasma and saliva. Pharmacogenetics 1994;4:109-16.
11. Peter R, Bocker R, Beaune PH, Iwasaki M, Guengerich FP, Yang CS. Hydroxylation of chlorzoxazone as a specific probe for human liver cytochrome P-450IIE1. Chem Res Toxicol 1990;3:566-73.
12. Kharasch ED, Thummel KE, Mhyre J, Lillibridge JH. Single-dose disulfiram inhibition of chlorzoxazone metabolism: a clinical probe for P450 2E1. Clin Pharmacol Ther 1993;53:643-50.
13. Fleming CM, Branch RA, Wilkinson GR, Guengerich FP. Human liver microsomal N-hydroxylation of dapsone by cytochrome P-4503A4. Mol Pharmacol 1992; 41:975-80.
14. May DG, Porter J, Wilkinson GR, Branch RA. Frequency distribution of dapsone N-hydroxylase, a putative probe for P4503A4 activity, in a white population. Clin Pharmacol Ther 1994;55:492-500.
15. Meyer UA, Skoda RC, Zanger UM. The genetic polymorphism of debrisoquine/sparteine metabolism: molecular mechanisms. Pharmacol Ther 1990;46:297-308.
16. Wilkinson GR, Guengerich FP, Branch RA. Genetic polymorphism of S-mephenytoin hydroxylation. Pharmacol Ther 1989;43:53-76.
17. May DG, Arns PA, Richards WO, Porter J, Ryder D, Fleming CM, et al. The disposition of dapsone in cirrhosis. Clin Pharmacol Ther 1992;51:689-700.
18. Black C, May G, Csuka ME, Lupoli S, Wilkinson GR, Branch RA. Activity of oxidative routes of metabolism of debrisoquin, mephenytoin, and dapsone is unrelated to the pathogenesis of vinyl chloride-induced disease. Clin Pharmacol Ther 1992;52:659-67.
19. Guttendorf RJ, Wedlund PJ, Blake J, Chang SL. Simplified phenotyping with dextromethorphan by thin-layer chromatography: application to clinical laboratory screening for deficiencies in oxidation drug metabolism. Ther Drug Monit 1988;10:490-8.
20. Fleming CM, Kaisary A, Wilkinson GR, Smith P, Branch RA. The ability to 4-hydroxylate debrisoquine is related to recurrence of bladder cancer. Pharmacogenetics 1992;2:128-34.
21. May DG, Black CM, Olsen NJ, Csuka ME, Tanner SB, Bellino L, et al. Scleroderma is associated with differences in individual routes of drug metabolism: a study with dapsone, debrisoquin, and mephenytoin. Clin Pharmacol Ther 1990;48:286-95.
22. Frye RF, Stiff DD, Matzke GR, Branch RA. A sensitive method for the simultaneous determination of caffeine and its dimethylxanthine metabolites in human serum, saliva, and plasma [abstract]. Pharm Res 1993;10:S43.
23. Frye RF, Stiff DD. Determination of chlorzoxazone and 6-hydroxychlorzoxazone in human plasma and urine by high-performance liquid chromatography. J Chromatogr B Biomed Appl 1996;686:291-6.
24. May DG, Porter JA, Uetrecht JP, Wilkinson GR, Branch RA. The contribution of N-hydroxylation and acetylation to dapsone pharmacokinetics in normal subjects. Clin Pharmacol Ther 1990;48:619-27.
25. Frye RF, Branch RA. Improved high performance liquid chromatographic determination of debrisoquine and 4-hydroxydebrisoquine in human urine following direct injection. J Chromatogr B Biomed Appl 1996;677:178-82.
26. Wedlund PJ, Aslanian WS, McAllister CB, Wilkinson GR, Branch RA. Mephenytoin hydroxylation deficiency in Caucasians: frequency of a new oxidation drug metabolism polymorphism. Clin Pharmacol Ther 1984;36:773-80.
27. Tanaka E, Ishikawa A, Yamamoto Y, Osada A, Tsuji K, Fukao K, et al. A simple useful method of the determination of hepatic function in patients with liver cirrhosis using caffeine and its three major dimethylmetabolites. Int J Clin Pharmacol Ther Toxicol 1992;30:336-41.
28. Girre C, Lucas D, Hispard E, Menez C, Dally S, Menez JF. Assessment of cytochrome P4502E1 induction in alcoholic patients by chlorzoxazone pharmacokinetics. Biochem Pharmacol 1994;47:1503-8.
29. Lucas D, Berthou F, Girre C, Poitrenaud F, Menez JF. High-performance liquid chromatographic determination of chlorzoxazone and 6-hydroxychlorzoxazone in serum: a tool for indirect evaluation of cytochrome P4502E1 activity in humans. J Chromatogr 1993;622:79-86.
30. Kaisary A, Smith P, Jacqz E, McAllister CB, Wilkinson GR, Ray WA, et al. Genetic predisposition to bladder cancer: ability to hydroxylate debrisoquine and mephenytoin as risk factors. Cancer Res 1987;47: 5488-93.
31. Alvares AP, Kappas A, Eiseman JL, Anderson KE, Pantuck CB, Pantuck EJ, et al. Intraindividual variation in drug disposition. Clin Pharmacol Ther 1979; 26:407-19.
32. Frye RF, Stiff DD, Matzke GR, Adedoyin A, Kubisty C, Branch RA. Pharmacokinetics of chlorzoxazone: an in vivo probe of cytochrome P4502E1 activity [abstract]. Pharm Res 1993;10:S388.
33. Mitra AK, Thummel KE, Kalhorn TF, Kharasch ED, Unadkat JD, Slattery JT. Metabolism of dapsone to its hydroxylamine by CYP2E1 in vitro and in vivo. Clin Pharmacol Ther 1995;58:556-66.
34. Gill HJ, Tingle MD, Park BK. N-Hydroxylation of dapsone by multiple enzymes of cytochrome P450: implications for inhibition of haemotoxicity. Br J Clin Pharmacol 1995;40:531-8.
35. Fleming CM, Persad R, Kaisary A, Smith P, Adedoyin A, Porter J, et al. Law activity of dapsone N-hydroxylation as a susceptibility risk factor in aggressive bladder cancer. Pharmacogenetics 1994;4:199-207.
36. Inaba T, Tyndale RE, Mahon WA. Quinidine: potent inhibition of sparteine and debrisoquine oxidation in vivo. Br J Clin Pharmacol 1986;22:199-200.
37. Mikus G, Ha HR, Vozeh S, Zekorn C, Follath F, Eichelbaum M. Pharmacokinetics and metabolism of quinidine in extensive and poor metabolizers of sparteine. Eur J Clin Pharmacol 1986;31:69-72.
38. Berthou F, Goasduff T, Lucas D, Dreano Y, Le Bot MH, Menez JF. Interaction between two probes used for phenotyping cytochromes P4501A2 (caffeine) and P4502E1 (chlorzoxazone) in humans. Pharmacogenetics 1995;5:72-9.
39. Schellens JHM, Janssens AR, Van Der Wart JHF, Van Der Velde EA, Breimer DD. Relationship between the metabolism of antipyrine, hexobarbital, and theophylline in patients with liver disease as assessed by a "cocktail" approach. Eur J Clin Invest 1989;19: 472-9.
40. Schellens JHM, Van Der Wart JHF, Danhof M, Van Der Velde EA, Breimer DD. Relationship between the metabolism of antipyrine, hexobarbital and theophylline in man as assessed by a "cocktail" approach. Br J Clin Pharmacol 1988;26:373-84.
41. Shedlofsky SI, Israel BC, Mcclain CJ, Hill DB, Blouin RA. Endotoxin administration to humans inhibits hepatic cytochrome P450-mediated drug metabolism. J Clin Invest 1994:94:2209-14.
42. Israel BC, Blouin RA, McIntyre W, Shedlofsky SI. Effects of interferon-a monotherapy on hepatic drug metabolism in cancer patients. Br J Clin Pharmacol 1993;36:229-35.
43. Schellens JHM, Van Der Wart JHF, Brugman M, Breimer DD. Influence of enzyme induction and inhibition on the oxidation of nifedipine sparteine, mephenytoin, and antipyrine in humans as assessed by a "cocktail" study design. J Pharmacol Exp Ther 1989; 249:638-45.
44. Loft S, Poulsen HE, Sonne J, Dossing M. Metronidazole clearance: a one-sample method and influencing factors. Clin Pharmacol Ther 1988;43:420-8.
45. Loft S. Metronidazole and antipyrine as probes for the study of foreign compound metabolism. Pharmacol Toxicol 1990;66(suppl 6):1-31.
46. Lanchote VL, Ping WC, Santos SRCJ. Influence of renal failure on cytochrome P-450 activity in hypertensive patients using a "cocktail" of antipyrine and nifedipine. Eur J Clin Pharmacol 1996;50:83-9.
47. Teunissen MWE, De Leede LGJ, Boeijinga JK, Breimer DD. Correlation between antipyrine metabolite formation and theophylline metabolism in humans after simultaneous single-dose administration and at steady state. J Pharmacol Exp Ther 1985;233: 770-5.
48. Groen K, Horan MA, Roberts NA, Gulati RS, Miljkovic B, Jansen EJ, et al. The relationship between phenazone (antipyrine) metabolite formation and theophylline metabolism in healthy and frail elderly women. Clin Pharmacokinet 1993;25:136-44.
49. Back DJ, Tija J, Monig H, Ohnhaus EE, Park BK. Selective inhibition of drug oxidation after simultaneous administration of two probe drugs, antipyrine and tolbutamide. Eur J Clin Pharmacol 1988;34:157-63.
50. Truckenbrodt J, Kraul H, Huster A, Töpfer R, Henschel L, Hoffmann A, et al. Simultaneous administration of various model substances for characterizing in vivo biotransformation in chronic liver diseases. Gastroenterol J 1990;50:179-82.
51. Lautenschlager MT, Viktor S, Muller UA, Hoffmann A. Serum concentrations of caffeine, methimazole, debrisoquine, sulfamethazine and their metabolites in diabetics before and during insulin therapy. Pharmazie 1996;51:750-3.
52. Evans WE, Relling MV, Petros WP, Meyer WH, Mirro J Jr, Crom WR. Dextromethorphan and caffeine as probes for simultaneous determination of debrisoquin-oxidation and N-acetylation phenotypes in children. Clin Pharmacol Ther 1989;45:568-73.
53. Brockmoller J, Roots I. Assessment of liver metabolic function: clinical implications. Clin Pharmacokinet 1994;27:216-48.
54. Tanaka E, Ishikawa A, Yamamoto Y, Osada A, Tsuji K, Fukao K, et al. Comparison of hepatic drug-oxidizing activity after simultaneous administration of two probe drugs, caffeine and trimethadione, to human subjects. Pharmacol Toxicol 1993;72:31-3.
55. Endres HGE, Henschel L, Merkel U, Hippius M, Hoffmann A. Lack of pharmacokinetic interaction between dextromethorphan, coumarin and mephenytoin in man after simultaneous administration. Pharmazie 1996;51:46-51.
56. Setiabudy R, Kusaka M, Chiba K, Darmansjah I, Ishizaki T. Dapsone N-acetylation, metoprolol α-hydroxylation, and S-mephenytoin 4-hydroxylation polymorphisms in an Indonesian population: a cocktail and extended phenotyping assessment trial. Clin Pharmacol Ther 1994;56:142-53.
57. Sanz EJ, Villen T, Alm C, Bertilsson L. S-Mephenytoin hydroxylation phenotypes in a Swedish population determined after coadministration with debrisoquin. Clin Pharmacol Ther 1989;45:495-9.
58. Atiba JO, Blaschke TF, Wilkinson GR. Effects of ketoconazole on the polymorphic 4-hydroxylation of S-mephenytoin and debrisoquine. Br J Clin Pharmacol 1989;28:161-5.
59. Guttendorf RJ, Britto M, Blouin RA, Foster TS, John W, Pittman KA, et al. Rapid screening for polymorphisms in dextromethorphan and mephenytoin metabolism. Br J Clin Pharmacol 1990;29:373-80.
60. Schellens JH, Ghabrial H, van der Wart HH, Bakker EN, Wilkinson GR, Breimer DD. Differential effects of quinidine on the disposition of nifedipine, sparteine, and mephenytoin in humans. Clin Pharmacol Ther 1991;50:520-8.
61. Schellens JH, Soons PA, van der Wart JH, Hoevers JW, Breimer DD. Lack of pharmacokinetic interaction between nifedipine, sparteine, and phenytoin in man. Br J Clin Pharmacol 1991;31:175-8.
62. Paolini M, Biagi GL, Bauer C, Cantelli-Forti G. Cocktail strategy: complications and limitations. J Clin Pharmacol 1993;33:1011-2.