Autoinduction of carbamazepine metabolism in children examined by a stable isotope technique

• Published in: Clinical pharmacology and therapeutics Vol. 27; no. 1; p. 83
• Main Authors: Bertilsson, L, Höjer, B, Tybring, G, Osterloh, J, Rane, A
• Format: Journal Article
• Language: English
• Published: United States 01-01-1980
• Subjects: Adolescent; Carbamazepine - blood; Carbamazepine - metabolism; Carbamazepine - therapeutic use; Child; Deuterium - metabolism; Epilepsy - drug therapy; Female; Humans; Kinetics; Male
• ISSN: 0009-9236
• DOI: 10.1038/clpt.1980.13

Autoinduction of carbamazepine (CBZ) metabolism was investigated in 3 children (10 to 13 yr old) using tetradeuterium-labeled CBZ (CBZ-D4). Prior to treatment, CBZ and CBZ-D4 given as a mixture had almost identical kinetics in each patient. During maintenance therapy with CBZ, part of the CBZ was exchanged for CBZ-D4 on 3 occasions. The clearance of CBZ-D4 given on the second day of therapy was 0.036 +/- 0.003 1 . kg-1 . hr-1, whereas it had been 0.028 +/- 0.003 before treatment. After 17 to 32 days of treatment, clearance doubled (0.056 +/- 0.010) but during the next 4 mo there was no further increase, indicating that the autoinduction was complete within 1 mo. As a corollary there was a decrease in steady-state plasma levels.