Summary
The metabolism of pentobarbitone has been investigated in two healthy volunteers, and the urinary excretion of unchanged drug, and the products of ω and (ω1)-oxidation, quantified for four days after each of three doses to each volunteer. The rates of excretion are discussed in terms which include enzyme induction effects.
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References
Maynert E.W. and Dawson J.M. (1952): 5-Ethyl-5-(3′-hydroxy-1’-methylbutyl) barbituric acids as metabolites of pentobarbital, J. biol. Chem.,195, 389–395.
Dickert Y.J., Shea P.J. and McCarty L.P. (1966): The synthesis and pharmacological activity of 5-ethyl-5-(3′-hydroxy-1′-methylbutyl)barbituric acid, J. med. Chem.,9, 249.
Maynert E.W. (1969): A racemic form of 5-ethyl-5-(3-hydroxy-1′-methylbutyl) barbituric acid as a metabolite of pentobarbital, J. med. Chem.,12, 180–181.
Carrol F.I. and Mitchell G.N. (1975): Synthesis and absolute stereochemistry of 5-alkyl-5-(3′-hydroxy-1′-methylbutyl)barbituric acid and 5-alkyl-5-(3′-hydroxy-1′-methylbutyl)-2-thiobarbituric acids, J. med. Chem.,18, 37–41.
Carroll F.I. and Philip A. (1971): Synthesis and alkaline decomposition of 5-alkyl-5-(1′-methyl-3′-oxobutyl)barbituric and 2-thiobarbituric acid derivatives, J. med. Chem.,14, 394–396.
Wood H.B. and Horning E.C. (1953): 5-Ethyl-5-(1-methyl-3′-carboxypropyl) barbituric acid and its 2-thio analog. Metabolites from pentobarbital and thiopental, J. Amer. Chem. Soc.,75, 5511–5513.
Ehrnebo M. (1974): Pharmacokinetics and distribution properties of pentobarbital in humans following oral and intravenous administration. J. pharm. Sci.,63, 1114–1118.
Reidenberg M.M., Lowenthal D.T., Briggs W. and Gasparo M. (1976): Pentobarbital elimination in patients with poor renal function. Clin. Pharmac. Ther.,20, 67–71.
Gilbert J.N.T. and Powell J.W. (1976): Enzyme induction effects in the human metabolism of butobarbitone, Eur. J. Drug Metab. Pharmacokin.,1, 188–193.
Baldeo W.C., Gilbert J.N.T. and Powell J.W. (1979): A multi-dose study on the human metabolism of amylobarbitone, Xenobiotica,9, 205–208.
Gilbert J.N.T., Hetherington W.L., Powell J.W. and Whalley W.B. (1975): Metabolism of quinalbarbitone, J. Pharm. Pharmac.,27, 343–347.
Maynert E.W., Foreman R.L. and Watabe T. (1970): Epoxides as obligatory intermediates in the metabolism of olefins to glycols, J. biol. Chem.,245, 5234–5238.
Levin W., Sematinger E., Jacobson M. and Kuntzman R. (1972): Destruction of cytochrome P450 by secobarbital and other barbiturates containing allyl groups. Science,176, 1341–1343.
Cretcher L.H., Koch J.A. and Pittenger W.H. (1925): The synthesis of 5-β-hydroxyethyl-barbituric acid and its alkyl derivatives. J. Amer. Chem. Soc.,47, 3083–3085.
Tang B.K., Inaba T. and Kalow W. (1977): N-Hydroxylation of pentobarbital in man, Drug Metab. Disposition,5, 71–74.
Gilbert J.N.T., Nelmes P.T.J., Powell J.W. and Murray S. (1978): N-Hydroxy-amylobarbitone — a metabolite of amylobarbitone? J. Pharm. Pharmac.,30, 595.
Goldbaum L.R. and Smith P.K. (1954): The interaction of barbiturates with serum albumin and its possible relation to their disposition and pharmacological actions, J. Pharmac. exp. Ther.,111, 197–209.
Pelkonen O. and Kärki N.T. (1973): Effect of physicochemical and pharmacokinetic pronerties of barbiturates on the induction of drug metabolism. Chem. Biol. Interactions,7, 93–99.
Alvan G., Piafsky K., Lind M. and von Bahr C. (1977): Effect of pentobarbital on the disposition of alprenolol. Clin. Pharmac. Ther.,22, 316–321.
Paigen B., Gurtoo H.L., Minowad J. and Paigen K. (1977): Aryl hydrocarbon hydroxylase in cultured human lymphocytes, in Microsomes and Drug Oxidations, ed. Ullrich et al., 418–425, Pergamon Press, Oxford.
Smith R.G., Daves G.D., Lynn R.K. and Gerber N. (1977): Hydantoin ring glucuronidation: characterisation of a new metabolite of 5,5-diphenyl-hydantoin in man and the rat, Biomed. Mass. Spec.,4, 275–279.
Kalow W., Tang B.K., Kadar D. and Inaba T. (1974): Distinctive patterns of amobarbital metabolites. Clin. Pharmac. Ther.,24, 576–582.
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Baldeo, W.C., Gilbert, J.N.T. & Powell, J.W. Multidose studies in the human metabolism of pentobarbitone. European Journal of Drug Metabolism and Pharmacokinetics 5, 75–80 (1980). https://doi.org/10.1007/BF03189449
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DOI: https://doi.org/10.1007/BF03189449