Validation of the five‐drug “Pittsburgh cocktail” approach for assessment of selective regulation of drug‐metabolizing enzymes

To determine whether the probe drugs caffeine, chlorzoxazone, dapsone, debrisoquin (INN, debrisoquine), and mephenytoin can be simultaneously administered as a metabolic cocktail to estimate in vivo cytochrome P450 (CYP) and N‐acetyltransferase enzyme activities.

[1]  G. Wilkinson,et al.  Mephenytoin hydroxylation deficiency in Caucasians: Frequency of a new oxidative drug metabolism polymorphism , 1984, Clinical pharmacology and therapeutics.

[2]  M. Hippius,et al.  Lack of pharmacokinetic interaction between dextromethorphan, coumarin and mephenytoin in man after simultaneous administration. , 1996, Die Pharmazie.

[3]  A. Conney,et al.  Intraindividual variation in drug disposition , 1979, Clinical pharmacology and therapeutics.

[4]  D. Breimer Interindividual Variations in Drug Disposition , 1983, Clinical pharmacokinetics.

[5]  H. Yamazaki,et al.  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. , 1994, The Journal of pharmacology and experimental therapeutics.

[6]  R. Branch,et al.  The ability to 4-hydroxylate debrisoquine is related to recurrence of bladder cancer. , 1992, Pharmacogenetics.

[7]  P. Beaune,et al.  Hydroxylation of chlorzoxazone as a specific probe for human liver cytochrome P-450IIE1. , 1991, Chemical research in toxicology.

[8]  D. Breimer,et al.  Influence of enzyme induction and inhibition on the oxidation of nifedipine, sparteine, mephenytoin and antipyrine in humans as assessed by a "cocktail" study design. , 1989, The Journal of pharmacology and experimental therapeutics.

[9]  A. Janssens,et al.  Relationship between the metabolism of antipyrine, hexobarbital and theophylline in patients with liver disease as assessed by a ‘cocktail’ approach , 1989, European journal of clinical investigation.

[10]  E. Kharasch,et al.  Single‐dose disulfiram inhibition of chlorzoxazone metabolism: A clinical probe for P450 2E1 , 1993, Clinical pharmacology and therapeutics.

[11]  T. Lesnick,et al.  The procarcinogen hypothesis for bladder cancer: activities of individual drug metabolizing enzymes as risk factors. , 1995, Pharmacogenetics.

[12]  D. Breimer,et al.  Differential effects of quinidine on the disposition of nifedipine, sparteine, and mephenytoin in humans , 1991, Clinical pharmacology and therapeutics.

[13]  R. Branch,et al.  Genetic polymorphism of S-mephenytoin hydroxylation. , 1989, Pharmacology & therapeutics.

[14]  G. Wilkinson,et al.  Activity of oxidative routes of metabolism of debrisoquin, mephenytoin, and dapsone is unrelated to the pathogenesis of vinyl chloride–induced disease , 1992, Clinical pharmacology and therapeutics.

[15]  F. Berthou,et al.  High-performance liquid chromatographic determination of chlorzoxazone and 6-hydroxychlorzoxazone in serum: a tool for indirect evaluation of cytochrome P4502E1 activity in humans. , 1993, Journal of chromatography.

[16]  T. Inaba,et al.  Quinidine: potent inhibition of sparteine and debrisoquine oxidation in vivo. , 1986, British journal of clinical pharmacology.

[17]  E. Hispard,et al.  Assessment of cytochrome P4502E1 induction in alcoholic patients by chlorzoxazone pharmacokinetics. , 1994, Biochemical pharmacology.

[18]  F. Berthou,et al.  Interaction between two probes used for phenotyping cytochromes P4501A2 (caffeine) and P4502E1 (chlorzoxazone) in humans. , 1995, Pharmacogenetics.

[19]  E. Kharasch,et al.  Metabolism of dapsone to its hydroxylamine by CYP2E1 in vitro and in vivo , 1995, Clinical pharmacology and therapeutics.

[20]  R. Frye,et al.  Determination of chlorzoxazone and 6-hydroxychlorzoxazone in human plasma and urine by high-performance liquid chromatography. , 1996, Journal of chromatography. B, Biomedical applications.

[21]  R. Branch,et al.  Human liver microsomal N-hydroxylation of dapsone by cytochrome P-4503A4. , 1992, Molecular pharmacology.

[22]  R. Branch,et al.  Improved high-performance liquid chromatographic determination of debrisoquine and 4-hydroxydebrisoquine in human urine following direct injection. , 1996, Journal of chromatography. B, Biomedical applications.

[23]  S. Loft,et al.  Metronidazole and antipyrine as probes for the study of foreign compound metabolism. , 1990, Pharmacology & toxicology.

[24]  Y. Iwasaki,et al.  A simple useful method for the determination of hepatic function in patients with liver cirrhosis using caffeine and its three major dimethylmetabolites. , 1992, International journal of clinical pharmacology, therapy, and toxicology.

[25]  S. Santos,et al.  Influence of renal failure on cytochrome P450 activity in hypertensive patients using a “cocktail” of antipyrine and nifedipine , 1996, European Journal of Clinical Pharmacology.

[26]  C. McClain,et al.  Endotoxin administration to humans inhibits hepatic cytochrome P450-mediated drug metabolism. , 1994, The Journal of clinical investigation.

[27]  M. Danhof,et al.  Relationship between the metabolism of antipyrine, hexobarbitone and theophylline in man as assessed by a 'cocktail' approach. , 1988, British journal of clinical pharmacology.

[28]  M. J. Coon,et al.  Cytochrome P-450 : multiplicity of isoforms, substrates, and catalytic and regulatory mechanisms , 1991 .

[29]  J. A. Porter,et al.  The contribution of N‐hydroxylation and acetylation to dapsone pharmacokinetics in normal subjects , 1990, Clinical pharmacology and therapeutics.

[30]  M. Butler,et al.  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. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[31]  R. Branch,et al.  The disposition of dapsone in cirrhosis , 1992, Clinical pharmacology and therapeutics.

[32]  R. Skoda,et al.  The genetic polymorphism of debrisoquine/sparteine metabolism-molecular mechanisms. , 1990, Pharmacology & therapeutics.

[33]  G. Wilkinson,et al.  Frequency distribution of dapsone N‐hydroxylase, a putative probe for P4503A4 activity, in a white population , 1994, Clinical pharmacology and therapeutics.

[34]  D. Breimer,et al.  A 'cocktail' strategy to assess in vivo oxidative drug metabolism in humans. , 1990, Trends in pharmacological sciences.

[35]  T. Blaschke,et al.  Effects of ketoconazole on the polymorphic 4-hydroxylations of S-mephenytoin and debrisoquine. , 1989, British journal of clinical pharmacology.

[36]  U. Klotz,et al.  Influence of Diet and Nutritional Status on Drug Metabolism , 1996, Clinical pharmacokinetics.

[37]  Shih-Ling Chang,et al.  Simplified Phenotyping with Dextromethorphan by Thin‐Layer Chromatography: Application to Clinical Laboratory Screening for Deficiencies in Oxidative Drug Metabolism , 1988, Therapeutic drug monitoring.

[38]  L. D. de Leede,et al.  Correlation between antipyrine metabolite formation and theophylline metabolism in humans after simultaneous single-dose administration and at steady state. , 1985, The Journal of pharmacology and experimental therapeutics.

[39]  G. Cantelli-forti,et al.  Cocktail Strategy: Complications and Limitations , 1993, Journal of clinical pharmacology.

[40]  R. Branch,et al.  Genetic predisposition to bladder cancer: ability to hydroxylate debrisoquine and mephenytoin as risk factors. , 1987, Cancer research.

[41]  M. Horan,et al.  The Relationship between Phenazone (Antipyrine) Metabolite Formation and Theophylline Metabolism in Healthy and Frail Elderly Women , 1993, Clinical pharmacokinetics.

[42]  C. Alm,et al.  S‐mephenytoin hydroxylation phenotypes in a Swedish population determined after coadministration with debrisoquin , 1989, Clinical pharmacology and therapeutics.

[43]  D. Strandness,et al.  Liver blood flow, antipyrine clearance, and antipyrine metabolite formation clearance in patients with chronic active hepatitis and alcoholic cirrhosis. , 1994, British journal of clinical pharmacology.

[44]  K. Chiba,et al.  Dapsone N‐acetylation, metoprolol α‐hydroxylation, and S‐mephenytoin 4‐hydroxylation polymorphisms in an Indonesian population: A cocktail and extended phenotyping assessment trial , 1994, Clinical pharmacology and therapeutics.

[45]  P. Beaune,et al.  Hydroxylation of chlorzoxazone as a specific probe for human liver cytochrome P-450IIE1 , 1990 .

[46]  M. Relling,et al.  Dextromethorphan and caffeine as probes for simultaneous determination of debrisoquin‐oxidation and N‐acetylation phenotypes in children , 1989, Clinical pharmacology and therapeutics.

[47]  S. Loft,et al.  Metronidazole clearance: A one‐sample method and influencing factors , 1988, Clinical pharmacology and therapeutics.

[48]  R. Blouin,et al.  Rapid screening for polymorphisms in dextromethorphan and mephenytoin metabolism. , 1990, British journal of clinical pharmacology.

[49]  D. Breimer,et al.  Lack of pharmacokinetic interaction between nifedipine, sparteine and phenytoin in man. , 1991, British journal of clinical pharmacology.

[50]  R. Blouin,et al.  Effects of interferon-alpha monotherapy on hepatic drug metabolism in cancer patients. , 1993, British journal of clinical pharmacology.

[51]  U. Fuhr,et al.  Simple and reliable CYP1A2 phenotyping by the paraxanthine/caffeine ratio in plasma and in saliva. , 1994, Pharmacogenetics.

[52]  B. K. Park,et al.  N-Hydroxylation of dapsone by multiple enzymes of cytochrome P450: implications for inhibition of haemotoxicity. , 1995, British journal of clinical pharmacology.

[53]  R. Branch,et al.  Scleroderma is associated with differences in individual routes of drug metabolism: A study with dapsone, debrisoquin, and mephenytoin , 1990, Clinical pharmacology and therapeutics.