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Urinary excretion of phenobarbitone and its metabolites in chronically treated patients

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Abstract

The elimination of phenobarbitone (PB) was studied in 14 chronically treated epileptic patients under steady state conditions. PB, [S]-PB-N-glucoside ([S]-PB-N-G) and p-hydroxy-PB (p-OH-PB) were assayed in urine by a HPLC method.

Some 57 % of the daily dose was recovered in urine, 14 % as [S]-PB-N-G, 16 % as p-OH-PB (conjugated plus non-conjugated) and 27 % as unaltered PB.

Thus PB-N-G formation contributed significantly to the elimination of PB during long-term administration of the drug, and there was reason to suspect that some of the PB-N-G formed may have already been degraded to untraced products before excretion from the body.

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References

  • Bhargava VO, Garretson LK (1988) Development of phenobarbital glucosidation in the human neonate. Dev Pharmacol Ther 11: 8–13

    Google Scholar 

  • Eadie MJ, Lander CM, Hooper WD, Tyrer JH (1977) Factors influencing plasma phenobarbitone levels in epileptic patients. Br J Clin Pharmacol 4: 541–547

    Google Scholar 

  • Hauptmann A (1912) Luminal bei Epilepsie. Münch Med Wochenschrift 59: 1907–1909

    Google Scholar 

  • Hooper WD, Kunze HE, Eadie MJ (1981) Qualitative and quantitative studies of methylphenobarbital metabolism in man. Drug Metab Disp 9: 381–385

    Google Scholar 

  • Kapetanovic IM, Kupferberg HJ, Porter RJ, Theodore W, Schulman E, Penry JK (1981) Mechanism of valproate-phenobarbital interaction in epileptic patients. Clin Pharmacol Ther 29: 480–486

    Google Scholar 

  • Kunze HE, Hooper WD, Eadie MJ (1980) The metabolism of methylphenobarbitone in man. ASEAN J Clin Sci 1: 115–119

    Google Scholar 

  • Soine WH, Soine PJ, England TM, Welty DF, Wood JH (1990 a) LC determination of the diastereomers of 1-(β-D-glucopyranosyl)phenobarbital in human urine. J Pharm Biomed Anal 8: 365–372

    Google Scholar 

  • Soine WH, Soine PJ, Mongrain SE, England TM (1990 b) Stereochemical characterization of the diastereomers of the phenobarbital N-β-D-glucose conjugate excreted in human urine. Pharm Res 7: 402–406

    Google Scholar 

  • Tang BK (1990) Drug glucosidation. Pharmacol Ther 46: 53–56

    Google Scholar 

  • Tang BK, Kalow W, Grey AA (1979) Metabolic fate of phenobarbital in man. N-glucoside formation. Drug Metab Disp 7: 315–318

    Google Scholar 

  • Treston AM, Philippides A, Jacobsen NW, Eadie MJ, Hooper WD (1987) Identification and synthesis of O-methylcatechol metabolites of phenobarbital and some N-alkyl derivatives. J Pharm Sci 76: 496–501

    Google Scholar 

  • Vest FB, Soine WH, Westkaemper RB, Soine PJ (1989) Stability of phenobarbital N-glucosides: Identification of hydrolysis products and kinetics of decomposition. Pharm Res 6: 458–465

    Google Scholar 

  • Whyte MP, Dekaban AS (1977) Metabolic fate of phenobarbital. A quantitative study of p-hydroxyphenobarbital elimination in man. Drug Metab Disp 5: 63–70

    Google Scholar 

Download references

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Bernus, I., Dickinson, R.G., Hooper, W.D. et al. Urinary excretion of phenobarbitone and its metabolites in chronically treated patients. Eur J Clin Pharmacol 46, 473–475 (1994). https://doi.org/10.1007/BF00191914

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  • DOI: https://doi.org/10.1007/BF00191914

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