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The influence of aging on the stereoselective pharmacokinetics of propranolol in the rat

(1992) CHIRALITY. 4(2). p.73-79
Author
Organization
Abstract
The influence of aging on the pharmacokinetics and the tissue distribution of (R)- and of (S)-propranolol was studied in 3-, 12-, and 24-month-old rats. After both iv and oral administration of rac-propranolol, the plasma concentrations were higher for the (R)- than for the (S)-enantiomer. For the tissue concentrations, the reverse was true. The free fraction of (S)-propranolol in plasma was about 4 times larger than that of (R)-propranolol, and this is the main factor responsible for the differences in kinetics between the two enantiomers. There was a suggestion for a difference in tissue binding between the two enantiomers. With aging, the plasma and tissue concentrations of both enantiomers increase, probably due to a decrease in blood clearance. Tissue binding did not change much with aging. Notwithstanding the marked differences between the kinetics of the propranolol enantiomers, the changes which occur with aging affect both enantiomers to the same degree.
Keywords
PROTEIN BINDING, TISSUE CONCENTRATIONS, PROPRANOLOL, BETA-ADRENERGIC BLOCKING AGENT, STEREOSELECTIVE PHARMACOKINETICS, PSEUDORACEMIC MIXTURES, ENANTIOMERS, (S)-PROPRANOLOL, ALBUMIN, AGE, (R)-PROPRANOLOL, DISPOSITION, CLEARANCE, TISSUE BINDING, ENANTIOMERS, AGING, PLASMA-PROTEIN BINDING, ALPHA-1-ACID GLYCOPROTEIN

Citation

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Chicago
Vermeulen, An, Frans Belpaire, Emmanuel Moerman, Frits De Smet, and Marcus Bogaert. 1992. “The Influence of Aging on the Stereoselective Pharmacokinetics of Propranolol in the Rat.” Chirality 4 (2): 73–79.
APA
Vermeulen, An, Belpaire, F., Moerman, E., De Smet, F., & Bogaert, M. (1992). The influence of aging on the stereoselective pharmacokinetics of propranolol in the rat. CHIRALITY, 4(2), 73–79.
Vancouver
1.
Vermeulen A, Belpaire F, Moerman E, De Smet F, Bogaert M. The influence of aging on the stereoselective pharmacokinetics of propranolol in the rat. CHIRALITY. 1992;4(2):73–9.
MLA
Vermeulen, An, Frans Belpaire, Emmanuel Moerman, et al. “The Influence of Aging on the Stereoselective Pharmacokinetics of Propranolol in the Rat.” CHIRALITY 4.2 (1992): 73–79. Print.
@article{204979,
  abstract     = {The influence of aging on the pharmacokinetics and the tissue distribution of (R)- and of (S)-propranolol was studied in 3-, 12-, and 24-month-old rats. After both iv and oral administration of rac-propranolol, the plasma concentrations were higher for the (R)- than for the (S)-enantiomer. For the tissue concentrations, the reverse was true. The free fraction of (S)-propranolol in plasma was about 4 times larger than that of (R)-propranolol, and this is the main factor responsible for the differences in kinetics between the two enantiomers. There was a suggestion for a difference in tissue binding between the two enantiomers. With aging, the plasma and tissue concentrations of both enantiomers increase, probably due to a decrease in blood clearance. Tissue binding did not change much with aging. Notwithstanding the marked differences between the kinetics of the propranolol enantiomers, the changes which occur with aging affect both enantiomers to the same degree.},
  author       = {Vermeulen, An and Belpaire, Frans and Moerman, Emmanuel and De Smet, Frits and Bogaert, Marcus},
  issn         = {0899-0042},
  journal      = {CHIRALITY},
  keyword      = {PROTEIN BINDING,TISSUE CONCENTRATIONS,PROPRANOLOL,BETA-ADRENERGIC BLOCKING AGENT,STEREOSELECTIVE PHARMACOKINETICS,PSEUDORACEMIC MIXTURES,ENANTIOMERS,(S)-PROPRANOLOL,ALBUMIN,AGE,(R)-PROPRANOLOL,DISPOSITION,CLEARANCE,TISSUE BINDING,ENANTIOMERS,AGING,PLASMA-PROTEIN BINDING,ALPHA-1-ACID GLYCOPROTEIN},
  language     = {eng},
  number       = {2},
  pages        = {73--79},
  title        = {The influence of aging on the stereoselective pharmacokinetics of propranolol in the rat},
  url          = {http://dx.doi.org/10.1002/chir.530040202},
  volume       = {4},
  year         = {1992},
}

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