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Preliminary pharmacokinetic studies of propylthiouracil in humans

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Abstract

Previous analytical procedures for the analysis of propylthiouracil (PTU) in blood and urine samples are questionable on several points. Therefore, a gas-liquid chromatography method has been developed which is both more sensitive and more specific. Application of this procedure confirmed that the drug was rapidly absorbed and eliminated. The mean terminal half-life in euthyroids was found to be 63 min. One hyperthyroid subject showed a far higher plasma clearance than seen with euthyroids, which requires further study.

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References

  1. E. B. Astwood. Treatment of hyperthyroidism with thiourea and thiouracil.J.A.M.A. 122: 78–81 (1943).

    Article  CAS  Google Scholar 

  2. E. B. Astwood. Thyrotoxicosis. InProceedings of an International Symposium, Edinburgh, 1967, I. Irvine, ed., E. & S. Livingstone Ltd. (1967), pp. 85–98.

  3. I. W. Grote. A new color reaction for soluble organic sulfur compounds.J. Biol. Chem. 93: 25–30 (1931).

    CAS  Google Scholar 

  4. L. C. Chesley. A method for determination of thiourea.J. Biol. Chem. 152: 571–578 (1944).

    CAS  Google Scholar 

  5. H. van Genderen, K. L. Van Lier, and J. Debeus. The determination of 4-methyl-2-thiouracil in animal tissues and blood.Biochim. Biophys. Acta 2: 482–486 (1948).

    Article  Google Scholar 

  6. R. H. Williams, B. J. Jandorf, and G. A. Kay. Methods for the determination of thiouracil in tissues and body fluids.J. Lab. Clin. Med. 29: 329–336 (1944).

    CAS  Google Scholar 

  7. K. J. Olson, R. E. Ely, and E. P. Reineke. An improved method for the determination of thiouracil.J. Biol. Chem. 169: 681–687 (1947).

    CAS  PubMed  Google Scholar 

  8. R. H. Williams and G. A. Kay. Thiouracils and thiourea.Arch. Internat. Med. 80: 37–52 (1947).

    Article  CAS  Google Scholar 

  9. D. A. McGinty, E. A. Sharp, W. A. Dill, and R. W. Rawson. Excretion studies on thiouracil and its 6-benzyl-6-n-propyl and 6-methyl-derivatives in man.J. Clin. Endocrinol. 8: 1043–1050 (1948).

    Article  CAS  Google Scholar 

  10. P. Morch. Quantitative determination of 4-methyl-thiouracil in urine.Acta Pharmacol. 1: 106–111 (1945).

    Article  CAS  Google Scholar 

  11. H. N. Christensen. Analytical determination and some properties of several thyroid-inhibiting compounds and of substances related to them.J. Biol. Chem. 162: 27–35 (1946).

    CAS  PubMed  Google Scholar 

  12. W. Doden and R. Kopf. Determination of 2-thiouracil, 4-methyl-2-thiouracil and 4-propyl-2-thiouracil.Arch. Exptl. Pathol. Pharmacol. 213: 51–58 (1951).

    Article  CAS  Google Scholar 

  13. R. A. McAllister. A new color reaction for methyl-thiouracil.Nature 4227: 789 (1950).

    Article  Google Scholar 

  14. R. A. McAllister and K. W. Howells. The colorimetric determination of methyl-thiouracil and propylthiouracil in tablets using 2,6-dichloro-quinone-chlorimide.J. Pharm. Pharmacol. 4: 259–261 (1952).

    Article  CAS  Google Scholar 

  15. W. D. Alexander, V. Evans, A. MacAuley, T. F. Gallagher, Jr., and J. Londono. Metabolism of35S-labelled antithyroid drugs in man.Brit. Med. J. 2: 290–291 (1969).

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  16. A. Fravolini and A. Begliomini. Gas chromatographic determination of thiouracils in feeds.J.A.O.A.C. 48: 908–911 (1965).

    CAS  Google Scholar 

  17. Y. Sasaki and T. Hashizume. Gas chromatography of trimethylsilylated bases and nucleosides.Anal. Biochem. 16: 1–19 (1966).

    Article  CAS  PubMed  Google Scholar 

  18. J. MacGee. Determination of nucleid acid base ratio by gas liquid chromatography.Anal. Biochem. 14: 305–314 (1966).

    Article  CAS  PubMed  Google Scholar 

  19. J. MacGee. Rapid determination of diphenylhydantoin in blood plasma by gas liquid chromatography.Anal. Biochem. 42: 421–422 (1970).

    CAS  Google Scholar 

  20. E. W. Robb and J. J. Westerbrook. Preparation of methyl esters for gas liquid chromatography of acids by pyrolysis of tetramethylammonium salts.Anal. Chem. 35: 1644–1647 (1963).

    Article  CAS  Google Scholar 

  21. E. Brochmann-Hanssen and O. T. Oke. Gas chromatography of barbiturates, phenolic alkaloids and xanthine bases: Flash heater methylation by means of trimethylanilinium hydroxide.J. Pharm. Sci. 58: 370–371 (1969).

    Article  CAS  PubMed  Google Scholar 

  22. R. H. Williams and G. A. Kay. Further studies of the absorption distribution and elimination of thiouracil.J. Clin. Endocrinol. Metab. 4: 385–394 (1944).

    Article  CAS  Google Scholar 

  23. R. H. Williams, G. H. Kay, and B. J. Jandorf. Thiouracil; its absorption, distribution and excretion.J. Clin. Invest. 23: 613–627 (1944).

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  24. K. E. Paschkis, A. Cantarow, A. E. Rakoff, and E. K. Tillson. Thiouracil levels in serum and urine.J. Pharmacol. Exptl. Therap. 83–84: 270–274 (1945).

    Google Scholar 

  25. D. S. Sitar and D. P. Thornhill. Prophylthiouracil: Absorption, metabolism and excretion in the albino rat.J. Pharmacol. Exptl. Therap. 183: 440–448 (1972).

    CAS  Google Scholar 

  26. R. H. Lindsay, B. S. Hulsey, H. Aboul-Eneen, and J. B. Hill. Abstract 840, Fifth International Congress of Pharmacology, San Francisco (July 23–28, 1971).

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Author information

Author notes

  1. D. Schuppan

    Present address: Riker Laboratories, Saint Paul, Minnesota

  2. B. v. Lehmann

    Present address: Institut für Pharmakologie, Berlin, Germany

  3. A. Pilbrant

    Present address: Research Department, Aktiebolaget KABI, Stockholm, Sweden

Authors and Affiliations

  1. Department of Pharmacy, School of Pharmacy and School of Medicine, University of California, 94143, San Francisco, California

    D. Schuppan, S. Riegelman, B. v. Lehmann, A. Pilbrant & C. Becker

Authors
  1. D. Schuppan
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  2. S. Riegelman
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  3. B. v. Lehmann
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  4. A. Pilbrant
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  5. C. Becker
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Additional information

Supported in part by Grant GM 16496 from the National Institutes of Health.

This paper was submitted to a Consulting Editor who served as the Journal Editor during its review process.

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Schuppan, D., Riegelman, S., Lehmann, B.v. et al. Preliminary pharmacokinetic studies of propylthiouracil in humans. Journal of Pharmacokinetics and Biopharmaceutics 1, 307–318 (1973). https://doi.org/10.1007/BF01060038

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  • DOI: https://doi.org/10.1007/BF01060038

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