Pharmacokinetics of 1,4-butanediol in rats: Bioactivation to γ-hydroxybutyric acid, interaction with ethanol, and oral bioavailability

AAPS Journal

Volumn 10, Issue 1, 2008, Pages 56-69

  Fung, Ho Leung ^a   Tsou, Pei Suen ^a   Bulitta, Jurgen B ^a   Tran, Doanh C ^a   Page, Nathaniel A ^a   Soda, David ^a   Mi Fung, Sun ^a  

^a UNIVERSITY AT BUFFALO   (United States)

Author keywords

1,4 butanediol; Drugs of abuse; Ethanol; GHB; Metabolic inhibition; Population pharmacokinetics

Indexed keywords

1,4 BUTANEDIOL; 4 HYDROXYBUTYRIC ACID; ALCOHOL; ALDEHYDE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BIOTRANSFORMATION; COMPARTMENT MODEL; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG ALCOHOL INTERACTION; DRUG BIOAVAILABILITY; DRUG DOSE COMPARISON; DRUG ELIMINATION; DRUG MEGADOSE; IN VITRO STUDY; LOW DRUG DOSE; MALE; METABOLIC ACTIVATION; METABOLIC INHIBITION; NONHUMAN; PHARMACODYNAMICS; RAT; REFLEX DISORDER; RIGHTING REFLEX; TOXICOKINETICS;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BUTYLENE GLYCOLS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; ETHANOL; MALE; RATS; RATS, SPRAGUE-DAWLEY; SODIUM OXYBATE;

EID: 51249111276     PISSN: 15507416     EISSN: None     Source Type: Journal    
DOI: 10.1208/s12248-007-9006-3     Document Type: Article

References (19)

1. A. Camacho, S. C. Matthews, B. Murray, and J. E. Dimsdale. Use of GHB compounds among college students. Am. J. Drug Alcohol Abuse 31(4):601-607 (2005).
2. J. Lettieri, and H. L. Fung. Absorption and first-pass metabolism of 14C-gamma-hydroxybutyric acid. Res. Commun. Chem. Pathol. Pharmacol. 13(3):425-437 (1976).
3. J. Lettieri, and H. L. Fung. Improved pharmacological activity via pro-drug modification: Comparative pharmacokinetics of sodium gamma-hydroxybutyrate and gamma-butyrolactone. Res. Commun. Chem. Pathol. Pharmacol. 22(1):107-118 (1978).
4. J. T. Lettieri, and H. L. Fung. Dose-dependent pharmacokinetics and hypnotic effects of sodium gamma-hydroxybutyrate in the rat. J. Pharmacol. Exp. Ther. 208(1):7-11 (1979).
5. R. D. Irwin. NTP summary report on the metabolism, disposition, and toxicity of 1,4-butanediol (CAS No. 110-63-4). Toxic. Rep. Ser. 54:1-28, A21-28, B21-25 (1996).
6. O. H. Lowry, N. J. Rosebrough, A. L. Farr, and R. J. Randall. Protein measurement with the Folin phenol reagent. J. Biol. Chem. 193(1):265-275 (1951).
7. K. M. Boje, and H. L. Fung. Characterization of the pharmacokinetic interaction between nifedipine and ethanol in the rat. J. Pharmacol. Exp. Ther. 249(2):567-571 (1989).
8. S. L. Beal, L. B. Sheiner, A. J. Boechmann (eds.). NONMEM Users Guides. Version 6, Icon Development Solutions, Ellicott City, 1989-2006.
9. H. L. Fung, E. Haas, J. Raybon, J. Xu, and S. M. Fung. Liquid chromatographic-mass spectrometric determination of endogenous gamma-hydroxybutyrate concentrations in rat brain regions and plasma. J. Chromatogr. B Anal. Technol. Biomed. Life Sci. 807(2):287-291 (2004).
10. D. K. Van Sassenbroeck, P. De Paepe, F. M. Belpaire, and W. A. Buylaert. Characterization of the pharmacokinetic and pharmacodynamic interaction between gamma-hydroxybutyrate and ethanol in the rat. Toxicol. Sci. 73(2):270-278 (2003).
11. H. Matsumoto, T. Fujimiya, and Y. Fukui. Role of alcohol dehydrogenase in rat ethanol elimination kinetics. Alcohol Alcohol Suppl. 29(1):15-20 (1994).
12. J. Shimada, T. Miyahara, S. Otsubo, N. Yoshimatsu, T. Oguma, and T. Matsubara. Effects of alcohol-metabolizing enzyme inhibitors and beta-lactam antibiotics on ethanol elimination in rats. Jpn. J. Pharmacol. 45(4):533-544 (1987).
13. M. S. Mumenthaler, J. L. Taylor, and J. A. Yesavage. Ethanol pharmacokinetics in white women: Nonlinear model fitting versus zero-order elimination analyses. Alcohol Clin. Exp. Res. 24(9):1353-1362 (2000).
14. H. Matsumoto, Y. Minowa, Y. Nishitani, and Y. Fukui. An allometric model for predicting blood ethanol elimination in mammals. Biochem. Pharmacol. 57(2):219-223 (1999).
15. J. G. Wagner, P. K. Wilkinson, and D. A. Ganes. Parameters Vm' and Km for elimination of alcohol in young male subjects following low doses of alcohol. Alcohol Alcohol 24(6):555-564 (1989).
16. F. Poldrugo, and O. C. Snead 3rd. 1,4-Butanediol and ethanol compete for degradation in rat brain and liver in vitro. Alcohol 3(6):367-370 (1986).
17. F. Poldrugo, S. Barker, M. Basa, F. Mallardi, and O. C. Snead. Ethanol potentiates the toxic effects of 1,4-butanediol. Alcohol Clin. Exp. Res. 9(6):493-497 (1985).
18. F. Poldrugo, and O. C. Snead 3rd. Effect of ethanol and acetaldehyde on gamma-hydroxybutyric acid in rat brain and liver. Subst. Alcohol Actions Misuse 5(5):263-271 (1984).
19. W. J. Jusko, J. R. Koup, and G. Alvan. Nonlinear assessment of phenytoin bioavailability. J. Pharmacokinet. Biopharm. 4(4):327-336 (1976).