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Related Experiment Videos

Plasma protein binding of phencyclidine

H G Giles, W A Corrigall, V Khouw

    Clinical Pharmacology and Therapeutics
    |January 1, 1982
    PubMed
    Summary

    Phencyclidine (PCP) binding in plasma is influenced by alpha 1-acid glycoprotein (alpha 1-AGP), not liver disease. Increased alpha 1-AGP in rats reduced PCP brain concentrations, showing protein binding impacts drug distribution.

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    Area of Science:

    • Pharmacology
    • Biochemistry
    • Toxicology

    Background:

    • Phencyclidine (PCP) is a drug whose distribution is affected by plasma protein binding.
    • Alpha 1-acid glycoprotein (alpha 1-AGP) is an acute-phase reactant known to bind cationic drugs.
    • Alcoholic liver disease can alter plasma protein concentrations, potentially affecting drug binding.

    Purpose of the Study:

    • To investigate the influence of alcoholic liver disease on phencyclidine (PCP) free fraction in male subjects.
    • To determine the role of alpha 1-acid glycoprotein (alpha 1-AGP) in PCP binding.
    • To assess the impact of altered plasma protein binding on PCP distribution in a rat model.

    Main Methods:

    • Measured PCP free fraction in healthy males and males with alcoholic liver disease.
    • Compared PCP binding in plasma versus fatty acid-free human serum albumin (HSA).
    • Assessed PCP binding in alpha 1-AGP solutions.
    • Correlated PCP binding with albumin and alpha 1-AGP concentrations.
    • Administered alpha 1-AGP or saline to rats, followed by 3H-PCP administration and brain concentration measurement.

    Main Results:

    • PCP free fraction was similar in healthy subjects (22.0%) and patients with alcoholic liver disease (23.0%).
    • PCP binding was significantly higher in plasma compared to fatty acid-free HSA.
    • Alpha 1-acid glycoprotein (alpha 1-AGP) significantly contributed to PCP binding, with a free fraction of 36.4% at 75 mg/dl.
    • A regression model showed that albumin and alpha 1-AGP explained half the variance in PCP binding.
    • Rats pretreated with alpha 1-AGP showed an 11% reduction in PCP brain concentrations post-administration.

    Conclusions:

    • Alcoholic liver disease does not significantly alter the free fraction of phencyclidine (PCP) in male subjects.
    • Alpha 1-acid glycoprotein (alpha 1-AGP) plays a crucial role in the plasma protein binding of PCP.
    • Increased plasma protein binding, particularly due to alpha 1-AGP, can reduce the free drug concentration during distribution, affecting drug distribution kinetics.

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