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Morphine binding to human plasma proteins.

G D Olsen

    Clinical Pharmacology and Therapeutics
    |January 1, 1975
    PubMed
    Summary
    This summary is machine-generated.

    Morphine primarily binds to human albumin in plasma, with about 34-37% protein binding. This interaction is influenced by protein concentration, impacting drug distribution.

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    Area of Science:

    • Pharmacology
    • Biochemistry
    • Drug Metabolism

    Background:

    • Plasma protein binding influences drug efficacy and distribution.
    • Understanding morphine's protein interactions is crucial for therapeutic management.
    • Previous studies have explored drug-protein binding, necessitating further investigation into morphine.

    Purpose of the Study:

    • To investigate the binding of (N-methyl-14C) morphine to human plasma proteins, including albumin and gamma globulin.
    • To determine the extent of morphine binding to human plasma in the therapeutic concentration range.
    • To compare morphine's protein binding characteristics with those of methadone.

    Main Methods:

    • Equilibrium dialysis was employed to study the interaction of radiolabeled morphine with purified human albumin, gamma globulin, and whole human plasma.

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  • Protein and drug concentrations were varied to assess their impact on morphine binding.
  • Binding percentages were calculated based on the distribution of radiolabeled morphine.

    • Main Results:

    • Morphine demonstrates significant binding to human albumin and, to a lesser extent, to gamma globulin.
    • Plasma lipoproteins likely do not bind morphine.
    • In the therapeutic range, 34.0% to 37.5% of morphine is bound to human plasma proteins, primarily albumin.
    • Morphine binding is dependent on protein concentration but independent of drug concentration.

    Conclusions:

    • Morphine's primary binding site in human plasma is albumin.
    • The lower lipid solubility of morphine compared to methadone may explain its reduced affinity for plasma proteins.
    • These findings contribute to understanding morphine's pharmacokinetics and its interactions within the body.