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Aging and the pharmacokinetics and metabolism of metoprolol enantiomers in the rat

An Vermeulen UGent, Frans Belpaire, Frits De Smet, Isabelle Vercruysse and Marcus Bogaert (1993) JOURNALS OF GERONTOLOGY. 48(3). p.B108-B114
abstract
After i. v. administration of racemic metoprolol in the rat, the plasma concentrations of (R)- and (S)-metoprolol were comparable, and no differences in pharmacokinetic parameters between the two enantiomers were found. From the 3rd to the 12th month, comparable changes were seen for both enantiomers: there was an increase in the area under the plasma concentration-time curve (AUC) and a decrease in blood and plasma clearance. Half-life showed a significant prolongation, volume of distribution decreased between 3 and 12 months and increased between 12 and 24 months. After oral administration of the racemate, AUC and C(max) (maximum plasma concentration) were slightly higher, while oral clearance was slightly lower for (R)-metoprolol than for (S)-metoprolol. With aging, C(max) and AUC increased for both enantiomers, while oral clearance decreased. The change in oral clearance as a function of age is different between (S)- and (R)-metoprolol, and thus enantioselective. In vitro disappearance rate in 3-month-old rats was significantly higher for (S)-metoprolol than for (R)-metoprolol, although the difference was small. With aging, the disappearance rates of both enantiomers increased significantly, but not enantioselectively.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
ATENOLOL, PROPRANOLOL, HEALTHY, PLASMA, YOUNG, AGE
journal title
JOURNALS OF GERONTOLOGY
J. Gerontol.
volume
48
issue
3
pages
B108 - B114
Web of Science type
Article
ISSN
0022-1422
DOI
10.1093/geronj/48.3.B108
language
English
UGent publication?
yes
classification
A1
id
201716
handle
http://hdl.handle.net/1854/LU-201716
date created
2004-01-14 13:42:00
date last changed
2017-10-27 11:22:05
@article{201716,
  abstract     = {After i. v. administration of racemic metoprolol in the rat, the plasma concentrations of (R)- and (S)-metoprolol were comparable, and no differences in pharmacokinetic parameters between the two enantiomers were found. From the 3rd to the 12th month, comparable changes were seen for both enantiomers: there was an increase in the area under the plasma concentration-time curve (AUC) and a decrease in blood and plasma clearance. Half-life showed a significant prolongation, volume of distribution decreased between 3 and 12 months and increased between 12 and 24 months. After oral administration of the racemate, AUC and C(max) (maximum plasma concentration) were slightly higher, while oral clearance was slightly lower for (R)-metoprolol than for (S)-metoprolol. With aging, C(max) and AUC increased for both enantiomers, while oral clearance decreased. The change in oral clearance as a function of age is different between (S)- and (R)-metoprolol, and thus enantioselective. In vitro disappearance rate in 3-month-old rats was significantly higher for (S)-metoprolol than for (R)-metoprolol, although the difference was small. With aging, the disappearance rates of both enantiomers increased significantly, but not enantioselectively.},
  author       = {Vermeulen, An and Belpaire, Frans and De Smet, Frits and Vercruysse, Isabelle and Bogaert, Marcus},
  issn         = {0022-1422},
  journal      = {JOURNALS OF GERONTOLOGY},
  keyword      = {ATENOLOL,PROPRANOLOL,HEALTHY,PLASMA,YOUNG,AGE},
  language     = {eng},
  number       = {3},
  pages        = {B108--B114},
  title        = {Aging and the pharmacokinetics and metabolism of metoprolol enantiomers in the rat},
  url          = {http://dx.doi.org/10.1093/geronj/48.3.B108},
  volume       = {48},
  year         = {1993},
}

Chicago
Vermeulen, An, Frans Belpaire, Frits De Smet, Isabelle Vercruysse, and Marcus Bogaert. 1993. “Aging and the Pharmacokinetics and Metabolism of Metoprolol Enantiomers in the Rat.” Journals of Gerontology 48 (3): B108–B114.
APA
Vermeulen, An, Belpaire, F., De Smet, F., Vercruysse, I., & Bogaert, M. (1993). Aging and the pharmacokinetics and metabolism of metoprolol enantiomers in the rat. JOURNALS OF GERONTOLOGY, 48(3), B108–B114.
Vancouver
1.
Vermeulen A, Belpaire F, De Smet F, Vercruysse I, Bogaert M. Aging and the pharmacokinetics and metabolism of metoprolol enantiomers in the rat. JOURNALS OF GERONTOLOGY. 1993;48(3):B108–B114.
MLA
Vermeulen, An, Frans Belpaire, Frits De Smet, et al. “Aging and the Pharmacokinetics and Metabolism of Metoprolol Enantiomers in the Rat.” JOURNALS OF GERONTOLOGY 48.3 (1993): B108–B114. Print.