In vivo binding characteristics of carbamazepine and carbamazepine-10,11-epoxide to serum proteins in paediatric patients with epilepsy.
The in vivo serum protein binding characteristics of carbamazepine (CBZ) and carbamazepine-10,11-epoxide (CBZ-E) were assessed in sera from 23 paediatric patients on CBZ monotherapy. We assumed that CBZ and CBZ-E binding to serum proteins comprised specific binding sites on alpha 1-acid glycoprotein (AAG) and non-specific binding sites on serum albumin. Therefore, the binding characteristics of each compound were analysed according to specific and nonspecific binding equations. Association constants for drug-AAG binding were 0.096 l.mumol-1 for CBZ and 0.023 l.mumol-1 for CBZ-E. Within the concentration ranges investigated the specific binding of each compound contributes to the drug-serum protein interactions. Age did not show a significant correlation with the serum unbound fraction of each compound.
Department of Clinical Pharmacy, Oita Medical University, Japan.
Y
Y
Kodama
K
K
Tsutsumi
M
M
Kuranari
H
H
Kodama
I
I
Fujii
M
M
Takeyama
D000293:Adolescent; D000367:Age Factors; D001798:Blood Proteins / Q000378:metabolism*; D002220:Carbamazepine / Q000031:analogs & derivatives* / Q000097:blood* / Q000627:therapeutic use; D002648:Child; D002675:Child, Preschool; D004827:Epilepsy / Q000097:blood* / Q000188:drug therapy; D005260:Female; D006801:Humans; D008297:Male; D011485:Protein Binding
D001798:Blood Proteins; D002220:Carbamazepine; C012227:carbamazepine epoxide