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November 1986

Total and Free Serum Concentrations of Carbamazepine and Carbamazepine-10,11-Epoxide in Children With Epilepsy

Author Affiliations

From the Department of Neurology, The Hospital for Sick Children, London (Drs Agbato and Brett), the Department of Chemical Pathology, The National Hospital for Nervous Diseases, London (Mr Elyas and Drs Patsalos, and Lascelles), and The Chalfont Centre for Epilepsy, Chalfont St Peter, Buckinghamshire (Dr Patsalos).

Arch Neurol. 1986;43(11):1111-1116. doi:10.1001/archneur.1986.00520110011006

• Simultaneous steady-state serum total and free (non-protein-bound) concentrations of carbamazepine and carbamazepine-10,11-epoxide were measured in 68 patients under the age of 21 years with epilepsy (44 males, 24 females; mean age, 11.8 ∓ 4.5 years). Thirty patients were maintained on monotherapy with carbamazepine. Mean serum total carbamazepine and carbamazepine10,11-epoxide concentrations obtained were 7.0 ∓ 2.4 mg/L (29.5 ∓ 10.0 μmol/ L) and 1.5 ∓ 0.6 mg/L (5.9 ∓ 2.6 μmol/ L), respectively. Mean serum-free carbamazepine and carbamazepine-10,11-epoxide concentrations obtained were 1.3 ∓ 0.5 mg/L (5.7 ∓ 2.1 μmol/L) and 0.5 ∓ 0.3 mg/L (2.2 ∓ 1.1 μmol/L), respectively. Binding of carbamazepine and carbamazepine-10,11-epoxide was 81% ∓ 3% and 62% ∓ 10%, respectively. There was no significant difference in binding between male and female patients or those maintained on monotherapy and polytherapy. Age correlated significantly with carbamazepine binding but not with carbamazepine-10,11-epoxide binding. Free concentrations of carbamazepine and carbamazepine-10,11-epoxide correlated significantly with total carbamazepine and total carbamazepine10,11-epoxide concentrations, respectively, indicating that the binding capacities of both carbamazepine and carbamazepine-10,11-epoxide are constant at serum total carbamazepine concentrations within the quoted therapeutic range.