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Biliary excretion of barbiturates.

C D Klaassen

    British Journal of Pharmacology
    |September 1, 1971
    PubMed
    Summary

    Pentobarbitone and phenobarbitone are significantly excreted into rat bile, with concentrations much higher than in plasma. Probenecid reduces this biliary excretion of barbiturates.

    Area of Science:

    • Pharmacokinetics
    • Drug Metabolism
    • Biliary Excretion

    Background:

    • Pentobarbitone and phenobarbitone are commonly used barbiturates.
    • Understanding their excretion pathways is crucial for drug efficacy and safety.

    Purpose of the Study:

    • To investigate the biliary excretion of pentobarbitone and phenobarbitone in rats.
    • To quantify the extent of excretion and identify the excreted forms.

    Main Methods:

    • Rats were administered pentobarbitone and phenobarbitone.
    • Bile and plasma concentrations of barbiturates and their metabolites were measured.
    • The effect of probenecid on biliary excretion was assessed.

    Main Results:

    • Bile concentrations of pentobarbitone and phenobarbitone (or metabolites) were 22-fold and 10-fold higher than plasma concentrations, respectively.

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  • 28% of pentobarbitone and 18% of phenobarbitone were excreted in bile within 6 hours.
  • The majority of excreted compounds were polar metabolites, not the parent drugs.

    • Conclusions:

    • Pentobarbitone and phenobarbitone are actively excreted into rat bile, primarily as metabolites.
    • Biliary excretion represents a significant elimination route for these barbiturates.
    • Probenecid inhibits the biliary excretion of these drugs.