CSF concentrations and serum protein binding of carbamazepine and carbamazepine-10,11-epoxide in epileptic patients.
Serum and CSF samples of patients receiving chronic carbamazepine treatment were analysed. Daily fluctuations in serum levels of carbamazepine and carbamazepine-10,11-epoxide did not appear to be related to the dosage schedule, but some patients tended to have lower fluctuations when the carbamazepine was given more frequently. The epoxide/carbamazepine serum ratios varied greatly from patient to patient, and also fluctuated during the day for the same patient. Carbamazepine and carbamazepine-10,11-epoxide were present in CSF in concentrations ranging from 19 to 34% and 26 to 71% of the serum concentrations, respectively. There was a significant relationship between the free fraction of both drugs evaluated in vivo and the CSF/serum ratios. The need for a careful evaluation of the possible clinical effect of the epoxide is stressed.
National Hospital for Epilepsy, 1300 Sandvika, Norway.
S I
SI
Johannessen
M
M
Gerna
J
J
Bakke
R E
RE
Strandjord
P L
PL
Morselli
D000293:Adolescent; D000328:Adult; D001798:Blood Proteins / Q000378:metabolism*; D002220:Carbamazepine / Q000031:analogs & derivatives* / Q000097:blood / Q000134:cerebrospinal fluid*; D004827:Epilepsy / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D008297:Male; D011485:Protein Binding; D055815:Young Adult
D001798:Blood Proteins; D002220:Carbamazepine; C012227:carbamazepine epoxide