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Drug distribution and binding.

S Oie

    Journal of Clinical Pharmacology
    |November 1, 1986
    PubMed
    Summary
    This summary is machine-generated.

    Drug distribution in the body, measured by apparent volume of distribution (V), depends on lipophilicity and protein binding. Extensive tissue distribution influences drug half-life and concentration fluctuations but not average steady-state levels.

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    Area of Science:

    • Pharmacokinetics and Drug Metabolism
    • Physicochemical Properties of Drugs

    Background:

    • Drug distribution is a key pharmacokinetic process influencing therapeutic efficacy and safety.
    • Lipophilicity and protein binding are critical determinants of how drugs distribute within the body.

    Purpose of the Study:

    • To elucidate the factors governing drug distribution in the body.
    • To explain the pharmacokinetic parameter apparent volume of distribution (V) and its implications.

    Main Methods:

    • Review of pharmacokinetic principles related to drug distribution.
    • Analysis of the relationship between drug properties (lipophilicity, protein binding) and V.

    Main Results:

    • Extensive tissue distribution, indicated by high V, is associated with high lipophilicity or high tissue binding/low plasma binding.

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  • The apparent volume of distribution (V) is influenced by drug lipophilicity, plasma protein binding, and tissue binding.
  • In cases of slow drug distribution, V is also dependent on drug clearance.

    • Conclusions:

    • The apparent volume of distribution (V) is a crucial parameter reflecting drug distribution characteristics.
    • Drug distribution significantly impacts drug half-life and concentration variability during multiple dosing regimens.
    • Understanding drug distribution is essential for optimizing dosing strategies and predicting drug behavior in vivo.