The use of caffeine as a metabolic probe for human drug metabolizing enzymes

General Pharmacology

Volumn 27, Issue 2, 1996, Pages 245-249

  Miners, John O ^a   Birkett, Donald J ^a  

^a FLINDERS MEDICAL CENTRE   (Australia)

Author keywords

caffeine; cytochrome P450; metabolic ratio; methylxanthines; N acetyltransferase; xanthine oxidase

Indexed keywords

1 METHYLURIC ACID; 1 METHYLXANTHINE; 5 ACETAMIDO 6 FORMYLAMINO 3 METHYLURACIL; ACYLTRANSFERASE; CAFFEINE; CYTOCHROME P450 ISOENZYME; DRUG METABOLITE; DRUG METABOLIZING ENZYME; PARAXANTHINE; THEOBROMINE; THEOPHYLLINE; XANTHINE OXIDASE;

BIOTRANSFORMATION; DEMETHYLATION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EXCRETION; DRUG METABOLISM; DRUG URINE LEVEL; ENZYME ACTIVITY; ENZYME SUBSTRATE; HUMAN; PHENOTYPE; POPULATION RESEARCH; PRIORITY JOURNAL; REVIEW; SCREENING; XENOBIOTIC METABOLISM;

EID: 0029981725     PISSN: 03063623     EISSN: None     Source Type: Journal    
DOI: 10.1016/0306-3623(95)02014-4     Document Type: Article

References (34)

1. Arnaud M. J. (1993) Metabolism of caffeine and other components of coffee. In Caffeine, Coffee and Health (Edited by Garattini S.), pp. 43-95. Raven Press, New York.
2. Birkett D. J., Miners J. O. and Attwood J. (1983) Secondary metabolism of theophylline biotransformation products in man - Route of formation of 1-methyluric acid. B. J. Clin. Pharmac. 15, 117-119.
3. Birkett D. J. and Miners J. O. (1991) Caffeine renal clearance and urine caffeine concentrations during steady state dosing. Implications for monitoring caffeine intake during sports events. Br. J. Clin. Pharmac. 31, 405-408.
4. Birkett D. J., Miners J. O. and Day R. O. (1991) 1-Methylxanthine derived from theophylline as an in vivo biochemical probe of allopurinol effect. Br. J. Clin. Pharmac. 32, 238-241.
5. Butler M. A., Iwasaki M., Guengerich F. P. and Kadlubar F. F. (1989) Human cytochrome P450PA (P-4501A2), the phenacetin O-deethylase, is primarily responsible for the hepatic 3-demethylation of caffeine and N-oxidation of carcinogenic arylamines. Proc. Natl. Acad. Sci. USA 86, 7696-7700.
6. Butler M. A., Lang N. P., Young J. F., Caporaso N. E., Vineis P., Hayes R. B., Teitel C. H., Massengill, J. P., Lawsen M. F. and Kadlubar F. F. (1992) Determination of CYP1A2 and NAT2 phenotypes in human populations by analysis of caffeine urinary metabolites. Pharmacogenetics 2, 116-127.
7. Campbell M. E., Grant D. M., Inaba T. and Kalow W. (1987a) Biotransformation of caffeine, paraxanthine, theophylline and theobromine by polycyclic aromatic hydrocarbon-inducible cytochromes P-450 in human liver microsomes. Drug Metabl. Disp. 15, 237-249.
8. Campbell M. E., Spielberg S. P. and Kalow W. (1987b) A urinary metabolite ratio that reflects systemic caffeine clearance. Clin. Pharmac. Ther. 42, 157-165.
9. Day R. O., Miners J. O., Birkett D. J., Graham G. G. and Whitehead A. (1988a) Relationship between plasma oxipurinol concentrations and xanthine oxidase activity involunteers dosed with allopurinol. Br. J. Clin. Pharmac. 26, 429-434.
10. Day R. O., Miners J. O., Birkett D. J., Whitehead A., Naidoo D., Hayes J. and Savdie E. (1988b) Allopurinol dosage selection: relationships between plasma oxipurinol and urate concentrations and urinary urate excretion. Br. J. Clin. Pharmac. 26, 423-428.
11. Fuhr U., Doehmer J., Battula N., Wolfel C., Kudla C., Keita Y. and Staib A. H. (1992) Biotransformation of caffeine and theophylline in mammalian cell lines genetically engineered for expressin of single cytochrome P450 isoforms. Biochem. Pharmac. 43, 225-235.
12. Fuhr U. and Rost K. L. (1994) Simple and reliable CYP1A2 phenotyping by the paraxanthine/caffeine ratio in plasma and in saliva. Pharmacogenetics 4, 109-116.
13. Grant D. M., Tang B. K., Campbell M. E. and Kalow W. (1986) Effect of allopurinol on caffeine disposition in man. Br. J. Clin. Pharmac. 21, 454-458.
14. Grygiel J. J., Wing L. M. H., Farkas J. and Birkett D. J. (1979) Effects of allopurinol on theophylline metabolism and clearance. Clin. Pharmac. Ther. 26, 660-667.
15. Gu L., Gonzalez F. J., Kalow W. and Tang B. K. (1992) Biotransformation of caffeine, paraxanthine, theobromine and theophylline by cDNA-expressed human CYP1A2 and CYP2E1. Pharmacognetics 2, 73-77.
16. James J. E. (1991) Caffeine and Health. Academic Press, London.
17. Kalow, W. and Tang, B. K. (1991a) Use of caffeine metabolite ratios to explore CYP1A2 and xanthine oxidase activities. Clin Pharmac. Ther. 50, 508-519.
18. Kalow W. and Tang B. K. (1991b) Caffeine as a metabolic probe: exploration of the enzyme-inducing effect of cigarette smoking. Clin. Pharmac. Ther. 49, 44-48.
19. Kalow W. and Tang B. K. (1994) The use of caffeine for enzyme assays: a critical appraisal. Clin. Pharmac. Ther. 53, 503-514.
20. Kilbane A. J., Silbart A. K., Manis M., Beitnis I. Z. and Weber W. W. (1990) Human N-actylation genotyping determination with urinary caffeine metabolites. Clin. Pharmac. Ther. 47, 470-476.
21. Lelo A., Birkett D. J., Robson R. A. and Miners J. O. (1986a) Comparative pharmacokinetics of caffeine and its primary demethylated metabolites in man. Br. J. Clin. Pharmac. 22, 177-182.
22. Lelo A., Miners J. O., Robson R. A. and Birkett D. J. (1986b) Quantitative assessment of caffeine partial clearances in man. Br. J. Clin. Pharmac. 22, 183-186.
23. Lelo A., Kjellen G., Birkett D. J. and Miners J. O. (1989) Paraxanthine metabolism in humans: determination of metablic partial clearances and effects of allopurinol and cimetidine. J. Pharmac. Exp. Ther. 248, 315-319.
24. Lelo A., Birkeett D. J. and Miners J. O. (1990) Mechanism of formation of 6-amino-5-(N-methylformylamino)-1-methyluracil and 3,7-dimethyluric acid from theobromine in the rat in vitro. Xenobiotica 20, 823-833.
25. Miners J. O., Attwood J. and Birkett D. J. (1982) Theobromine metabolism in man. Drug Metab. Disp. 10, 672-676.
26. Miners J. O., Attwood J., Wing L. M. H. and Birkett D. J. (1985) Influence of cimetidine, sulfinpyrazone and cigarette smoking on theobromine metabolism in man. Drug. Metab. Disp. 13, 598-601.
27. Notarianni L. J., Oliver S. E., Bennet P. N. and Silverman B. W. (1995) Caffeine as a metabolic probe: A comparison of the metabolic ratios used to assess CYP1A2 activity. Br. J. Clin. Pharmac. 39, 65-69.
28. Parsons W. D. and Neims A. H. (1978) Effects of smoking on caffeine clearance. Clin. Pharmac. Ther. 24, 40-45.
29. Robson R. A., Miners J. O., Matthews A. P., Stupans, I., Meller D., McManus M. E. and Birkett D. J. (1988) Characterization of theophylline metabolism by human liver microsomes. Biochem. Pharmac. 37, 1651-1659.
30. Tang B. K., Kadar D., Qian L., Iriah J., Yip J. and Kalow W. (1991) Caffeine as a metabolic probe: validation of its use for acetylater phenotyping. Clin. Pharmac. Ther. 49, 648-657.
31. Tang B. K., Zhou Y., Kadar D. and Kalow W. (1994) Caffeine as a probe for CYP1A2 activity: potential influence of renal factors on urinary phenotypic trait measurements. Pharmacogenetics 4, 117-124.
32. Tarrus E., Cami J., Roberts D. J., Spickett R. G. W., Celdran E. and Segura J. (1987) Accumulation of caffeine in healthy volunteers treated with furafylline. Br. J. Clin. Pharmac. 23, 9-18.
33. Tassaneeyakul W., Mohamed Z., Birkett D. J., McManus M. E., Veronese M. E., Tukey R. H., Gonzalez F. and Miners J. O. (1992) Caffeine as a probe for human cytochromes P450: validation using cDNA-expression, imunoinhibition and microsomal kinetic techniques. Pharmacogenetics 2, 173-183.
34. Tassaneeyakul W., Birkett D. J., McManus M. E., Veronese M. E., Andersson T., Tukey R. H. and Miners J. O. (1994) Caffeine metabolism by human hepatic cytochromes P450: contributions of 1A2, 2E1 and 3A isoforms. Biochem. Pharmac. 47, 1767-1773.