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Pharmacokinetics of 10‐OH‐carbazepine, the main metabolite of the antiepileptic oxcarbazepine, from serum and saliva concentrations
Author(s) -
Kristensen O.,
Klitgaard N. A.,
Jönsson B.,
Sindrup S.
Publication year - 1983
Publication title -
acta neurologica scandinavica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.967
H-Index - 95
eISSN - 1600-0404
pISSN - 0001-6314
DOI - 10.1111/j.1600-0404.1983.tb05340.x
Subject(s) - oxcarbazepine , carbamazepine , saliva , pharmacokinetics , metabolite , chemistry , anticonvulsant , free fraction , half life , pharmacology , chromatography , serum concentration , active metabolite , oral administration , endocrinology , medicine , epilepsy , biochemistry , psychiatry
After administration of 600 mg of the antiepileptic oxcarbazepine to 7 healthy volunteers, serum and stimulated saliva samples were collected for the next 72 h. Concentrations of 10‐OH‐carbazepine, the main metabolite of oxcarbazepine, were determined by an HPLC method. The time‐concentration curves showed a median T max of 8 h followed by a plateau until 24 h indicating saturable kinetic processes. Based on the curves, the pharmacokinetic parameters were calculated. The half‐life of 10‐OH‐carbazepine in saliva, 13.8 ± 3.7 (SD) h, was significantly shorter than in serum, 19.3 ± 6.2 (SD) h. The half‐life of 10‐OH‐carbazepine in serum was inversely correlated to the free fraction, estimated by the ratio saliva/serum concentrations. Calculation of the free fraction by this method showed that 53.1 ± 14.4 (SD) % of 10‐OH‐carbazepine is unbound in serum. There was a good correlation ( r = 0.914) between serum and saliva concentrations of 10‐OH‐carbazepine from 8–72 h after administration of oxcarbazepine. This finding indicates that saliva concentrations may prove useful, as has been shown for carbamazepine, in therapeutic monitoring of oxcarbazepine treatment.