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Pharmacokinetics and bioavailability of tranexamic acid

  • Å. Pilbrant
  • M. Schannong
  • J. Vessman
Originals

Summary

Tranexamic acid 1 g was given intravenously to three healthy volunteers. Plasma concentrations decayed in three monoexponential phases. Most elimination took place during the first eight hours, giving an apparent elimination half-life of approximately two hours. Plasma clearance ranged between 110–116 ml/min. The urinary recovery of tranexamic acid exceeded 95% of the dose. Ten healthy volunteers were given tranexamic acid 2 g orally on an empty stomach, and together with a meal. Food had no influence on the absorption of tranexamic acid, as judged by comparison of the peak plasma concentration, the time required to reach the peak, the AUC from zero to six hours, and the urinary excretion data. The oral bioavailability of tranexamic acid, calculated from 24 h urinary excretion after oral and intravenous administration, was 34% of the dose.

Key words

tranexamic acid pharmacokinetics bioavailability oral absorption influence of food plasma clearance 

References

  1. 1.
    Andersson L, Nilsson IM, Colleen S, Granstrand B, Melander B (1968) Role of urokinase and tissue activator in sustaining bleeding and the management thereof with EACA and AMCA. Ann NY Acad Sci 146: 642–656PubMedGoogle Scholar
  2. 2.
    Boxenbaum HG, Riegelman S, Elashoff RM (1974) Statistical estimations in pharmacokinetics. J Pharmacokinet Biopharm 2: 123–148PubMedCrossRefGoogle Scholar
  3. 3.
    Cormack F, Chakrabarti RR, Jouhar AJ, Fearnley GR (1973) Tranexamic acid in upper gastrointestinal haemmorhage. Lancet 1: 1207–1208PubMedCrossRefGoogle Scholar
  4. 4.
    Eriksson O, Kjellman H, Pilbrant Å, Schannong M (1974) Pharmacokinetics of tranexamic acid after intravenous administration to normal volunteers. Eur J Clin Pharmacol 7: 375–380PubMedCrossRefGoogle Scholar
  5. 5.
    Hedlund PO (1969) Antifibrinolytic therapy with cyklokapron in connection with prostatectomy. A double blind study. Scand J Urol Nephrol 3: 177–182PubMedGoogle Scholar
  6. 6.
    Metzler CM, Elfring GL, McEwen AJ (1974) A users manual for NONLIN and associated programs. Research Biostatics. Upjohn Co, Kalamazoo, MIGoogle Scholar
  7. 7.
    Niazi S (1976) Errors involved in instantaneous intravascular input assumption. J Pharm Sci 65: 750–752PubMedGoogle Scholar
  8. 8.
    Nilsson L, Rybo G (1967) Treatment of menorrhagia with an antifibrinolytic agent, tranexamic acid (AMCA). A double blind investigation. Acta Obstet Gynecol Scand 46: 572–580CrossRefGoogle Scholar
  9. 9.
    Tovi D, Nilsson IM, Thulin C-A (1972) Fibrinolysis and subarachnoid haemmorhage. Inhibitory effect of tranexamic acid. A clinical study. Acta Neurol Scand 48: 393–402PubMedCrossRefGoogle Scholar
  10. 10.
    Tovi D (1973) The use of antifibrinolytic drugs to prevent early recurrent aneurysmal subarachnoid hemmorhage. Acta Neurol Scand 49: 163–175PubMedCrossRefGoogle Scholar
  11. 11.
    Vessman J, Strömberg S (1977) Determination of tranexamic acid in biological material by electron capture gas chromatography after direct derivatization in an aqueous medium. Anal Chem 49: 369–373PubMedCrossRefGoogle Scholar
  12. 12.
    Wagner JG and coworkers (1977) Pharmacokinetic parameters estimated from intravenous data by uniform methods and some of their uses. J Pharmacokinet Biopharm 5: 161–183PubMedCrossRefGoogle Scholar
  13. 13.
    Westlake W (1971) Problems associated with analysis of pharmacokinetic models. J Pharm Sci 60: 882–885PubMedGoogle Scholar
  14. 14.
    Widlund L, Strömberg S, Hallström H, Osanius B (1979) The disposition of tranexamic acid (AMCA) in different animal species and in man after oral dosage. Scientific Report No. 7999047, Kabi AB, StockholmGoogle Scholar

Copyright information

© Springer-Verlag 1981

Authors and Affiliations

  • Å. Pilbrant
    • 1
  • M. Schannong
    • 1
  • J. Vessman
    • 1
  1. 1.Research DepartmentKabi ABStockholmSweden

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