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Human spinal fluid methadone levels.

R B Rubenstein, M J Kreek, N Mbawa

    Drug and Alcohol Dependence
    |March 1, 1978
    PubMed
    Summary
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    Methadone levels in cerebrospinal fluid (CSF) were measured in patients undergoing lumbar punctures. CSF methadone concentrations were a fraction of serum levels, appearing 3-8 hours after administration.

    Area of Science:

    • Pharmacology
    • Neuroscience
    • Clinical Medicine

    Background:

    • Methadone is a widely used opioid agonist for pain management and opioid use disorder treatment.
    • Understanding methadone's distribution into the central nervous system is crucial for optimizing therapy and managing side effects.

    Purpose of the Study:

    • To quantify methadone concentrations in cerebrospinal fluid (CSF) relative to serum levels.
    • To determine the time course of methadone appearance in the CSF.

    Main Methods:

    • CSF and serum methadone levels were measured in nine patients undergoing lumbar punctures for medical or surgical reasons.
    • Patients were receiving methadone maintenance therapy.

    Main Results:

    • CSF methadone concentrations were consistently lower than serum levels, representing 2% to 73% of concurrent serum concentrations.

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  • Measured CSF methadone levels ranged from 0.010 to 0.097 ng%.
  • Peak methadone concentrations in CSF were observed approximately 3 to 8 hours post-administration.

    • Conclusions:

    • Methadone penetration into the central nervous system is limited and variable.
    • The observed time lag suggests a delayed distribution of methadone into the CSF.
    • These findings have implications for understanding methadone's central effects and informing dosing strategies.