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Influence of age on stereoselective pharmacokinetics and metabolism of hexobarbital in the rat

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Abstract
The influence of age on stereoselective pharmacokinetics and in vitro metabolism of R- and S-hexobarbital was studied in the rat. After intravenous administration of the racemate, the plasma concentrations of S-hexobarbital are markedly lower than those of R-hexobarbital. For S-hexobarbital the half-life is somewhat shorter and the volume of distribution and plasma clearance is higher than for its antipode. For both enantiomers an increase in AUC and half-life, and a decrease in clearance are observed with aging. These changes occur mainly between the 3rd and the 12th month and are slightly more pronounced for R- than for S-hexobarbital, as appears from the SIR ratios. The volume of distribution shows no changes with aging. In vitro disappearance rate in 3-month-old rats is significantly higher for S- than for R-hexobarbital. There is for both enantiomers an increase in disappearance rate in 12-month-old rats as compared to younger or older rats, but this is significant only for the R-enantiomer. There are pronounced differences in the kinetics and metabolism of both hexobarbital enantiomers; changes with aging occur, but are only slightly and not always significantly more important for R- than for S-hexobarbital.
Keywords
STEREOSELECTIVE PHARMACOKINETIC, LIVER, METABOLISM, HEPATOCYTES, ENANTIOMERS, AGING, HEXOBARBITAL, PROPRANOLOL, CLEARANCE

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Chicago
Vermeulen, An, Frans Belpaire, Frits de Smet, Marie Rosseel, and Marcus Bogaert. 1992. “Influence of Age on Stereoselective Pharmacokinetics and Metabolism of Hexobarbital in the Rat.” Mechanisms of Ageing and Development 65 (2-3): 167–175.
APA
Vermeulen, An, Belpaire, F., de Smet, F., Rosseel, M., & Bogaert, M. (1992). Influence of age on stereoselective pharmacokinetics and metabolism of hexobarbital in the rat. MECHANISMS OF AGEING AND DEVELOPMENT, 65(2-3), 167–175.
Vancouver
1.
Vermeulen A, Belpaire F, de Smet F, Rosseel M, Bogaert M. Influence of age on stereoselective pharmacokinetics and metabolism of hexobarbital in the rat. MECHANISMS OF AGEING AND DEVELOPMENT. 1992;65(2-3):167–75.
MLA
Vermeulen, An, Frans Belpaire, Frits de Smet, et al. “Influence of Age on Stereoselective Pharmacokinetics and Metabolism of Hexobarbital in the Rat.” MECHANISMS OF AGEING AND DEVELOPMENT 65.2-3 (1992): 167–175. Print.
@article{206936,
  abstract     = {The influence of age on stereoselective pharmacokinetics and in vitro metabolism of R- and S-hexobarbital was studied in the rat. After intravenous administration of the racemate, the plasma concentrations of S-hexobarbital are markedly lower than those of R-hexobarbital. For S-hexobarbital the half-life is somewhat shorter and the volume of distribution and plasma clearance is higher than for its antipode. For both enantiomers an increase in AUC and half-life, and a decrease in clearance are observed with aging. These changes occur mainly between the 3rd and the 12th month and are slightly more pronounced for R- than for S-hexobarbital, as appears from the SIR ratios. The volume of distribution shows no changes with aging. In vitro disappearance rate in 3-month-old rats is significantly higher for S- than for R-hexobarbital. There is for both enantiomers an increase in disappearance rate in 12-month-old rats as compared to younger or older rats, but this is significant only for the R-enantiomer. There are pronounced differences in the kinetics and metabolism of both hexobarbital enantiomers; changes with aging occur, but are only slightly and not always significantly more important for R- than for S-hexobarbital.},
  author       = {Vermeulen, An and Belpaire, Frans and de Smet, Frits and Rosseel, Marie and Bogaert, Marcus},
  issn         = {0047-6374},
  journal      = {MECHANISMS OF AGEING AND DEVELOPMENT},
  keyword      = {STEREOSELECTIVE PHARMACOKINETIC,LIVER,METABOLISM,HEPATOCYTES,ENANTIOMERS,AGING,HEXOBARBITAL,PROPRANOLOL,CLEARANCE},
  language     = {eng},
  number       = {2-3},
  pages        = {167--175},
  title        = {Influence of age on stereoselective pharmacokinetics and metabolism of hexobarbital in the rat},
  url          = {http://dx.doi.org/10.1016/0047-6374(92)90033-A},
  volume       = {65},
  year         = {1992},
}

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