European Journal of Clinical Pharmacology

, Volume 29, Issue 1, pp 67–71 | Cite as

Plasma protein binding of dipyrone metabolites in man

  • E. Zylber-Katz
  • L. Granit
  • M. Levy
Originals

Summary

Four metabolites of dipyrone, 4-methyl-aminoantipyrine (MAA), 4-aminoantipyrine (AA), 4-formylaminoantipyrine (FAA) and 4-acetylamino-antipyrine (AAA) can be identified in human plasma after its oral administration. The plasma protein binding of the metabolites in samples from 20 healthy volunteers was determined by ultrafiltration. None of the metabolites were found to be extensively bound to plasma proteins. The binding of MAA and AA was relatively higher than of FAA and AAA, as expected from their chemical structure. The mean percentage plasma protein binding was 57.6% for MAA, 47.9 for AA, 17.8 for FAA and 14.2% for AAA. The correlation between the unbound concentration in plasma and the total concentrations of MAA, AA, FAA and AAA was linear. No association was evident between the total protein plasma concentration and the extent of binding. The possible therapeutic implications related to protein binding of several analgesic and non-steroidal anti-inflammatory drugs are discussed.

Key words

dipyrone dipyrone metabolites human protein binding analgesic antipyretic drugs healthy volunteers 

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Copyright information

© Springer-Verlag 1985

Authors and Affiliations

  • E. Zylber-Katz
    • 1
  • L. Granit
    • 1
  • M. Levy
    • 1
  1. 1.Clinical Pharmacology Unit, Department of Medicine AHadassah University HospitalJerusalemIsrael

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