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Related Experiment Videos

Codeine kinetics as determined by radioimmunoassay

J W Findlay, R F Butz, R M Welch

    Clinical Pharmacology and Therapeutics
    |October 1, 1977
    PubMed
    Summary

    This study determined codeine bioavailability using radioimmunoassay (RIA). Oral codeine bioavailability was 53% compared to intramuscular injection, with different peak plasma concentrations observed.

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    Area of Science:

    • Pharmacology
    • Pharmacokinetics
    • Analytical Chemistry

    Background:

    • Codeine is a widely used analgesic.
    • Understanding its pharmacokinetic profile is crucial for effective dosing.
    • Bioavailability influences drug efficacy and safety.

    Purpose of the Study:

    • To determine pharmacokinetic parameters of codeine in humans.
    • To compare the relative bioavailability of oral versus intramuscular codeine administration.
    • To establish codeine plasma concentrations over time.

    Main Methods:

    • A crossover study design was employed with 6 healthy male volunteers.
    • Codeine phosphate (65 mg) was administered orally (in combination with other analgesics) and intramuscularly.
    • Plasma codeine concentrations were measured using a specific radioimmunoassay (RIA) technique.

    Main Results:

    • Peak plasma codeine concentrations were higher and achieved slightly faster after intramuscular injection (194-340 ng/ml at 0.25-1 hr) compared to oral administration (102-140 ng/ml at 0.75-1 hr).
    • Mean plasma half-life (t1/2) and volume of distribution following intramuscular injection were 3.32 hr and 5.1 L/kg, respectively.
    • Oral relative to intramuscular bioavailability of codeine averaged 53% (range 42%-71%).

    Conclusions:

    • Codeine exhibits moderate oral bioavailability, significantly lower than intramuscular administration.
    • The pharmacokinetic differences suggest altered absorption or first-pass metabolism for oral codeine.
    • RIA provides a sensitive method for quantifying codeine in pharmacokinetic studies.

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