• Medientyp: E-Artikel
  • Titel: Age-related Alteration of Carbamazepine-serum Protein Binding in Man
  • Beteiligte: Koyama, Hikaru; Sugioka, Nobuyuki; Uno, Akira; Mori, Satoru; Nakajima, Kenji
  • Erschienen: Oxford University Press (OUP), 2010
  • Erschienen in: Journal of Pharmacy and Pharmacology
  • Sprache: Englisch
  • DOI: 10.1211/0022357991773474
  • ISSN: 0022-3573; 2042-7158
  • Schlagwörter: Pharmaceutical Science ; Pharmacology
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  • Anmerkungen:
  • Beschreibung: <jats:title>Abstract</jats:title> <jats:p>To determine whether biological maturation influences the kinetics of carbamazepineserum protein binding, the carbamazepine free fraction (%) was investigated in the serum of 66 patients, ranging from 4 to 83 years, with epilepsy or trigeminal neuralgia, treated with carbamazepine alone or carbamazepine in combination with phenytoin, phenobarbital, and/or valproic acid, over a relatively long period.</jats:p> <jats:p>Biochemical parameters such as levels of albumin and non-glycated albumin showed a significant relationship with carbamazepine free fraction (r=-0.521, P &amp;lt; 0.001 for albumin; r=-0.700, P &amp;lt; 0.001 for non-glycated albumin). Non-glycated albumin was more strongly correlated with carbamazepine free fraction. The biochemical parameters showed a significant relationship with age (r=-0.243, P &amp;lt; 0.1 for albumin; r= 0.666, P &amp;lt; 0.001 for glycated albumin; r=-0.459, P &amp;lt; 0.001 for non-glycated albumin; r= 0.640, P &amp;lt; 0.001 for carbamazepine free fraction). Glycated albumin (%), non-glycated albumin and carbamazepine free fraction (%) were strongly correlated with age, whereas albumin showed only a weak correlation with age. To evaluate the effects of ageing on carbamazepine-serum protein binding, the patients were divided into three groups according to age: children, 4–15 years; adults, 16–64 years; elderly, 65–83 years. Albumin and non-glycated albumin were much lower, and glycated albumin (%) and carbamazepine free fraction (%) much higher in the elderly group than in the other two groups.</jats:p> <jats:p>The results of this study showed that the major ligand of carbamazepine in the serum was non-glycated albumin, which decreased with age. These observations suggested that in elderly patients, the elevation of free carbamazepine concentrations in the serum caused by reduced non-glycated albumin levels, induces increases in the sensitivity of the pharmacological effects of carbamazepine and the risk of drug interactions.</jats:p>