Abstract
Concentrations of carbamazepine (CBZ) and its 10,11-epoxide metabolite (CBZ-E) were measured in simultaneously collected plasma and mixed saliva samples from 15 children (aged 1-13 years). Saliva concentrations of CBZ and CBZ-E were measured in hourly samples taken from six of these children during dose intervals whilst on different dose or dose-frequency regimens. Saliva and plasma CBZ (r = 0.91; P less than 0.001) and CBZ-E (r = 0.91; P less than 0.001) concentrations were significantly correlated. The mean +/- s.d. steady state CBZ-E/CBZ concentration ratio in the six children was 0.40 +/- 0.21 and was similar at all times within the 12 h dose interval. The mean +/- s.d. percentage fluctuation of the combined CBZ + CBZ-E (103.0 +/-28.9) was significantly less than that of CBZ-E (145.5 +/- 52.8) but not CBZ (109.6 +/- 31.1). If CBZ and CBZ-E have equipotent anticonvulsant activity in man, the contribution of CBZ-E approximates to 30% of total anticonvulsant effect in children taking CBZ alone.
Full text
PDF




Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Astier A., Maury M., Barbizet J. Simultaneous, rapid high-performance liquid chromatographic microanalysis of plasma carbamazepine and its 10,11-epoxide metabolite: applications to pharmacokinetic studies in humans. J Chromatogr. 1979 Oct 11;164(2):235–240. doi: 10.1016/s0378-4347(00)81193-7. [DOI] [PubMed] [Google Scholar]
- Brodie M. J., Forrest G., Rapeport W. G. Carbamazepine 10, 11 epoxide concentrations in epileptics on carbamazepine alone and in combination with other anticonvulsants. Br J Clin Pharmacol. 1983 Dec;16(6):747–749. doi: 10.1111/j.1365-2125.1983.tb02257.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- MacKichan J. J., Duffner P. K., Cohen M. E. Salivary concentrations and plasma protein binding of carbamazepine and carbamazepine 10,11-epoxide in epileptic patients. Br J Clin Pharmacol. 1981 Jul;12(1):31–37. doi: 10.1111/j.1365-2125.1981.tb01851.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Pynnönen S., Sillanpä M., Frey H., Iisalo E. Carbamazepine and its 10,11-epoxide in children and adults with epilepsy. Eur J Clin Pharmacol. 1977 Jan 3;11(2):129–133. doi: 10.1007/BF00562904. [DOI] [PubMed] [Google Scholar]
- Rane A., Höjer B., Wilson J. T. Kinetics of carbamazepine and its 10,11-epoxide metabolite in children. Clin Pharmacol Ther. 1976 Mar;19(3):276–283. doi: 10.1002/cpt1976193276. [DOI] [PubMed] [Google Scholar]
- Rylance G. W., Butcher G. M., Moreland T. Saliva carbamazepine levels in children. Br Med J. 1977 Dec 3;2(6100):1481–1481. doi: 10.1136/bmj.2.6100.1481. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Rylance G. W., Moreland T. A., Butcher G. M. Carbamazepine dose-frequency requirement in children. Arch Dis Child. 1979 Jun;54(6):454–458. doi: 10.1136/adc.54.6.454. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Westenberg H. G., van der Kleijn E., Oei T. T., de Zeeuw R. A. Kinetics of carbamazepine and carbamazepine-epoxide, determined by use of plasma and saliva. Clin Pharmacol Ther. 1978 Mar;23(3):320–328. doi: 10.1002/cpt1978233320. [DOI] [PubMed] [Google Scholar]
