Kinetics of epsilon-aminocaproic acid distribution, elimination, and antifibrinolytic effects in normal subjects

Marilynn C. Frederiksen, Dennis J. Bowsher, Tsuen Ih Ruo, Thomas K. Henthorn, Chung Hsin Ts'ao, David Green, Arthur J. Atkinson*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

Abstract

The kinetics of ε{lunate}-aminocaproic acid (EACH) distribution and elimination were studied in six normal subjects after a single 10-gm iv dose. Steady-state distribution volume averaged 30.0 l or 0.39 l/kg. Mean elimination t sol1 2 was 294 min and the elimination clearance was 0.19 1/min. Renal excretion of unchanged EACA accounted for 68% of its elimination and renal EACA clearance averaged 115% of creatinine clearance. EACA antifibrinolytic effect kinetics were also characterized in five of the subjects by the monitoring of clot lysis times in whole blood and platelet-rich plasma. Peak antifibrinolytic effects were observed 15 to 60 min after peak EACA plasma concentrations were attained. A model of maximal fibrinolysis inhibition (Emax) was used to estimate a half-maximal inhibition (IC50) of 63 ± 19.7 μg/ml. This agrees with the value of 0.55mM or 72 μg/ml that has been reported for the dissociation constant of the EACA-plasminogen complex and is consistent with the proposed biochemical mechanism of EACA action.

Original languageEnglish (US)
Pages (from-to)387-393
Number of pages7
JournalClinical pharmacology and therapeutics
Volume35
Issue number3
DOIs
StatePublished - Mar 1984

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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