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Nadolol binding to human serum proteins.

L Patel, A Johnson, P Turner

    The Journal of Pharmacy and Pharmacology
    |June 1, 1984
    PubMed
    Summary
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    Nadolol protein binding in healthy individuals ranged from 4-27%, averaging 14%. While a slight correlation with alpha-1-acid glycoprotein was noted, clinical effects from protein binding variations are improbable.

    Area of Science:

    • Pharmacology
    • Biochemistry
    • Clinical Chemistry

    Background:

    • Understanding drug protein binding is crucial for predicting pharmacokinetics and pharmacodynamics.
    • Nadolol, a beta-adrenergic blocker, exhibits variable protein binding.
    • Serum protein concentrations, particularly alpha-1-acid glycoprotein, can influence drug binding.

    Purpose of the Study:

    • To quantify the extent of nadolol protein binding in a cohort of healthy subjects.
    • To investigate the relationship between nadolol binding and serum alpha-1-acid glycoprotein levels.
    • To assess the potential clinical significance of variations in nadolol protein binding.

    Main Methods:

    • Serum samples were collected from 95 healthy individuals.
    • Nadolol protein binding was determined using established laboratory assays.

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  • Serum concentrations of alpha-1-acid glycoprotein were measured.
  • Main Results:

    • Nadolol protein binding varied significantly, ranging from 4% to 27%.
    • The mean protein binding of nadolol was 14% (± 4% s.d.).
    • A statistically significant, albeit small, positive correlation was observed between nadolol binding and serum alpha-1-acid glycoprotein concentration.

    Conclusions:

    • Serum protein binding of nadolol exhibits considerable inter-individual variability.
    • Alpha-1-acid glycoprotein is a minor determinant of nadolol protein binding in healthy subjects.
    • Observed variations in nadolol protein binding are unlikely to cause adverse clinical outcomes.