Stable isotopes in human drug metabolism studies

  • G. H. Draffan


The resurgence of interest in the stable isotopes of hydrogen, carbon, nitrogen and oxygen in biomedical research is mainly attributable to the development of increasingly refined technology for their determination. As a result, new areas of application have opened up, and this is particularly the case in pharmaceutical research. The purpose of this paper is to consider the rôles for stable isotope labelling in the conduct of drug metabolism studies in man, and Scheme 3.1 summarises a number of these applications. At present, the largest area of activity concerns the use of labelled drugs as standards in quantitative measurement following administration of the unlabelled substance. However, administration of the stable-isotope-labelled drug can also provide valuable information and, in other cases, complements the use of a radiotracer.


Stable Isotope Isotope Ratio Mass Spectrometer Label Drug Stable Isotope Labelling Stable Isotope Dilution 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. Beckinsale, R. D., Freeman, N. J., Jackson, M. C., Powell, R. E. and Young, W. A. P. Ion Phys., 12, 299Google Scholar
  2. Bending, M. R., Bennett, P. N., Rowland, M. and Steiner, J. (1976). Proceedings of the British Pharmacological Society Meeting, July, 1976, Abstract No. C25Google Scholar
  3. Blake, M. I., Crespi, H. L. and Katz, J. J. (1975). J. Pharm. Sci., 64, 367CrossRefGoogle Scholar
  4. Boyes, R. N. and Keenaghan, J. B. (1971). Lidocaine in the Treatment of Ventricular Arrhythmias (ed. D. B. Scott and D. G. Julian), Livingston, Edinburgh, p. 140Google Scholar
  5. Boyes, R. N., Scott, D. B., Jebson, P. J., Goodman, M. J. and Julian, D. G. (1971). Clin. Pharmacol. Ther., 12, 105Google Scholar
  6. Brash, A. R., Baillie, T. A., Clare, R. A. and Draffan, G. H. (1976). Biochem. Med., 16, 77CrossRefGoogle Scholar
  7. Davies, D. S., Wing, L. M. H., Reid, J. L., Neill, E., Tippett, P. and Dollery, C. T. (1977). Clin. Pharmacol. Ther., 21, 593Google Scholar
  8. Draffan, G. H., Bellward, G. D., Clare, R. A., Dargie, H. J., Dollery, C. T., Murray, S., Reid, J. L., Wing, L. M. H. and Davies, D. S. (1975). Proceedings of the Second International Conference on Stable Isotopes (ed. E. R. Klein and P. D. Klein), US Department of Commerce, Springfield, Virginia. Document code CONF-75 1027, p. 149Google Scholar
  9. Draffan, G. H., Clare, R. A., Goodwin, B. L., Ruthven, C. R. J. and Sandler, M. (1974). Adv. Mass Spectrom., 6, 245Google Scholar
  10. Draffan, G. H., Clare, R. A., Murray, S., Bellward, G. D., Davies, D. S. and Dollery, C. T. (1976). Advances in Mass Spectrometry in Biochemistry and Medicine, Vol. 2 (ed. A. Frigerio), Spectrum Publications, New York, p. 389Google Scholar
  11. Draffan, G. H., Gilbert, J. D. and McGregor, J. S. (1977). Unpublished observationsGoogle Scholar
  12. Falkner, F. C., Sweetman, B. J. and Watson, J. T. (1975). Appl. Spectrosc. Rev., 10, 51CrossRefGoogle Scholar
  13. Garland, W. A., Trager, W. F. and Nelson, S. D. (1974). Biomed. Mass Spectrom., 1, 124CrossRefGoogle Scholar
  14. Hammar, C.-G., Holmstedt, B. and Ryhage, R. (1968). Anal. Biochem., 25, 337CrossRefGoogle Scholar
  15. Inaba, T., Tang, B. K. and Kalow, W. (1976). Proceedings of the Second International Conference on Stable Isotopes (ed. E. R. Klein and P. D. Klein), National Technical Information Service, US Department of Commerce, Springfield, Virginia. Document code CONF-75 1027, p. 163Google Scholar
  16. Knapp, D. R., Gaffney, T. E. and McMahon, R. E. (1972). Biochem. Pharmacol., 21, 425CrossRefGoogle Scholar
  17. Kropp, H., Kahan, F. M. and Woodruff, H. B. (1975). Abstracts of 15th International Science Conference on Antimicrobial Agents and Chemotherapy, Washington DCGoogle Scholar
  18. Lawson, A. M. and Draffan, G. H. (1975). Prog. Med. Chem., 12, 1CrossRefGoogle Scholar
  19. McMahon, R. E., Sullivan, H. R., Due, S. L. and Marshall, F. J. (1973). Life Sci., 12, 463CrossRefGoogle Scholar
  20. Nelson, D. S., Pohl, L. R. and Trager, W. F. (1975). J. Med. Chem., 18, 1062CrossRefGoogle Scholar
  21. Prescott, L. F., Adjepon-Yamoah, K. K. and Talbot, R. G. (1976). Brit. Med. J., 1, 939CrossRefGoogle Scholar
  22. Rehbinder, D. (1970). Catapres in Hypertension (ed. M. E. Conolly), Butterworths, London, p. 227Google Scholar
  23. Roncucci, R., Simon, M.-J., Jacques, G. and Lambelin, G. (1976). Eur. J. Drug Metab. Pharmacokin., 1, 9CrossRefGoogle Scholar
  24. Sano, M., Yotsui, Y., Abe, H. and Sasaki, S. (1976). Biomed. Mass Spectrom., 3, 1CrossRefGoogle Scholar
  25. Schoeller, D. A. and Hayes, J. M. (1975). Anal. Chem., 47, 408CrossRefGoogle Scholar
  26. Strong, J. M. and Atkinson, A. J. (1972). Anal. Chem., 44, 2287CrossRefGoogle Scholar
  27. Strong, J. M., Dutcher, J. S., Lee, W.-K. and Atkinson, A. J. (1975). Clin. Pharmacol. Ther., 18, 613Google Scholar
  28. Sullivan, H. R., Wood, P. G. and McMahon, R. E. (1976). Biomed. Mass Spectrom., 3, 212CrossRefGoogle Scholar
  29. von Unruh, G. E., Hauber, D. J., Schoeller, D. A. and Hayes, J. M. (1974). Biomed. Mass Spectrom., 1, 345CrossRefGoogle Scholar

Copyright information

© The Contributors 1978

Authors and Affiliations

  • G. H. Draffan
    • 1
  1. 1.Inveresk Research InternationalEdinburghUK

Personalised recommendations