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Regional pharmacokinetics. II. Experimental methods.

R N Upton1, W B Runciman, L E Mather

  • 1Department of Anaesthesia and Intensive Care, University of Adelaide, Australia.

Biopharmaceutics & Drug Disposition
|December 1, 1990
PubMed
Summary
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Regional pharmacokinetics investigates drug levels in specific body areas, offering deeper insights than systemic blood analysis. This review covers experimental methods, applications, and limitations for understanding drug disposition.

Area of Science:

  • Pharmacokinetics
  • Drug Metabolism
  • Toxicology

Background:

  • Regional pharmacokinetics provides detailed drug disposition insights beyond systemic blood concentrations.
  • Understanding drug distribution in specific tissues is crucial for efficacy and safety.

Purpose of the Study:

  • To review experimental methods in regional pharmacokinetics.
  • To discuss the applications and limitations of these methods.
  • To enhance understanding of drug disposition mechanisms.

Main Methods:

  • Post-mortem tissue biopsies for regional drug concentrations.
  • Serial tissue biopsies for time-course analysis in individual animals.
  • In vivo regional blood sampling with catheterization and blood flow measurement.

Related Experiment Videos

  • Artificially perfused regions for controlled studies.
  • Ex vivo methods: tissue slices, cell cultures, and tissue homogenates.

    • Main Results:

    • Post-mortem biopsies offer high specificity but require many animals.
    • Serial biopsies provide time-course data but have limited applications.
    • In vivo regional blood sampling allows repeated measurements.
    • Artificially perfused regions offer control but less in vivo relevance.
    • Ex vivo methods assess uptake, metabolism, and binding.

    Conclusions:

    • Various experimental methods exist for regional pharmacokinetics, each with unique advantages and limitations.
    • The choice of method depends on the specific research question regarding drug disposition.
    • Further research can refine these techniques for more accurate in vivo modeling.