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Lidocaine plasma protein binding

P A Routledge, A Barchowsky, T D Bjornsson

    Clinical Pharmacology and Therapeutics
    |March 1, 1980
    PubMed
    Summary
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    Plasma protein binding of lidocaine, particularly alpha 1-acid glycoprotein (AAG), significantly influences its unbound fraction. AAG concentration is a key predictor of lidocaine binding variability in healthy individuals.

    Area of Science:

    • Pharmacology
    • Biochemistry
    • Clinical Chemistry

    Background:

    • Lidocaine is a widely used local anesthetic and antiarrhythmic drug.
    • The unbound fraction of a drug in plasma is generally considered pharmacologically active.
    • Plasma protein binding influences drug distribution, efficacy, and toxicity.

    Purpose of the Study:

    • To investigate the relationship between plasma protein concentrations and the unbound fraction of lidocaine.
    • To determine the role of alpha 1-acid glycoprotein (AAG) and albumin in lidocaine binding.
    • To assess interindividual and intraindividual variability in lidocaine plasma binding.

    Main Methods:

    • Equilibrium dialysis was used to measure the percentage of unbound lidocaine in plasma from 24 healthy subjects.

    Related Experiment Videos

  • C14-labeled lidocaine hydrochloride was added to plasma samples.
  • Concentrations of alpha 1-acid glycoprotein (AAG) and albumin were measured.

    • Main Results:

    • The percentage of unbound lidocaine was inversely related to plasma AAG concentration (r = -0.931, p < 0.001).
    • Lidocaine binding ratio strongly correlated with AAG concentration (r = 0.960, p < 0.001).
    • Albumin concentration showed no significant relationship with lidocaine binding.

    Conclusions:

    • Alpha 1-acid glycoprotein is the primary determinant of lidocaine plasma protein binding in healthy subjects.
    • Significant interindividual and intraindividual variations in lidocaine binding exist.
    • Plasma AAG concentration can predict the extent of lidocaine plasma binding.