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Interindividual differences of protein binding in man.

H Walther, F P Meyer

    International Journal of Clinical Pharmacology and Biopharmacy
    |October 1, 1979
    PubMed
    Summary
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    Interindividual variability in phenytoin and phenobarbital protein binding is significant. Determining this binding is crucial for evaluating therapeutic effectiveness and adverse effects in patients.

    Area of Science:

    • Pharmacokinetics
    • Clinical Chemistry

    Background:

    • Phenytoin and phenobarbital are commonly prescribed anticonvulsant medications.
    • Accurate therapeutic drug monitoring requires understanding drug disposition, including protein binding.

    Purpose of the Study:

    • To quantify the interindividual variability in serum protein binding for phenytoin and phenobarbital.
    • To highlight the clinical importance of assessing protein binding for optimizing patient therapy.

    Main Methods:

    • Equilibrium dialysis was employed to determine the unbound fractions of phenytoin and phenobarbital in patient serum.
    • Serum samples were analyzed from 390 patients for phenytoin and 220 patients for phenobarbital.

    Main Results:

    • Phenytoin exhibited a wide range of serum protein binding, from 8% to 40%.

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  • Phenobarbital demonstrated even greater variability, with protein binding ranging from 25% to 80%.

    • Conclusions:

    • Significant interindividual variability exists in the protein binding of both phenytoin and phenobarbital.
    • Routine determination of protein binding is essential for accurate therapeutic drug monitoring, preventing treatment failures and adverse drug reactions.