Abstract
The pharmacokinetics of clobazam were studied in six healthy volunteers and six age and sex matched enzyme-induced epileptic patients. In the epileptic patients the area under the plasma concentration-time curve for clobazam was significantly smaller and the area under the plasma concentration-time curve for N-desmethylclobazam was significantly greater than in the healthy volunteers. Plasma N-desmethylclobazam concentrations were found to be much higher than those of clobazam in the epileptic patients, raising the possibility that the antiepileptic properties of clobazam are to be attributed more to its metabolite than the parent drug.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Allen J. W., Oxley J., Robertson M. M., Trimble M. R., Richens A., Jawad S. S. Clobazam as adjunctive treatment in refractory epilepsy. Br Med J (Clin Res Ed) 1983 Apr 16;286(6373):1246–1247. doi: 10.1136/bmj.286.6373.1246. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Davies D. S., Thorgeirsson S. S., Breckenridge A., Orme M. Interindividual differences in rates of drug oxidation in man. Drug Metab Dispos. 1973 Jan-Feb;1(1):411–417. [PubMed] [Google Scholar]
- Dhillon S., Richens A. Pharmacokinetics of diazepam in epileptic patients and normal volunteers following intravenous administration. Br J Clin Pharmacol. 1981 Dec;12(6):841–844. doi: 10.1111/j.1365-2125.1981.tb01317.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Divoll M., Greenblatt D. J., Ciraulo D. A., Puri S. K., Ho I., Shader R. I. Clobazam kinetics: intrasubject variability and effect of food on adsorption. J Clin Pharmacol. 1982 Jan;22(1):69–73. doi: 10.1002/j.1552-4604.1982.tb05711.x. [DOI] [PubMed] [Google Scholar]
- Fielding S., Hoffmann I. Pharmacology of anti-anxiety drugs with special reference to clobazam. Br J Clin Pharmacol. 1979;7 (Suppl 1):7S–15S. [PMC free article] [PubMed] [Google Scholar]
- Fraser H. S., Mucklow J. C., Murray S., Davies D. S. Assessment of antipyrine kinetics by measurement in saliva. Br J Clin Pharmacol. 1976 Apr;3(2):321–325. doi: 10.1111/j.1365-2125.1976.tb00610.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Lai A. A., Levy R. H., Cutler R. E. Time-course of interaction between carbamazepine and clonazepam in normal man. Clin Pharmacol Ther. 1978 Sep;24(3):316–323. doi: 10.1002/cpt1978243316. [DOI] [PubMed] [Google Scholar]
- Marcucci F., Fanelli R., Mussini E., Garattini S. Effect of phenobarbital on the in vitro metabolism of diazepam in several animal species. Biochem Pharmacol. 1970 May;19(5):1771–1776. doi: 10.1016/0006-2952(70)90169-3. [DOI] [PubMed] [Google Scholar]
- Ohnhaus E. E., Park B. K., Colombo J. P., Heizmann P. The effect of enzyme induction on diazepam metabolism in man. Br J Clin Pharmacol. 1979 Dec;8(6):557–563. doi: 10.1111/j.1365-2125.1979.tb01044.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Rupp W., Badian M., Christ O., Hajdú P., Kulkarni R. D., Taeuber K., Uihlein M., Bender R., Vanderbeke O. Pharmacokinetics of single and multiple doses of clobazam in humans. Br J Clin Pharmacol. 1979;7 (Suppl 1):51S–57S. doi: 10.1111/j.1365-2125.1979.tb04665.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Tedeschi G., Riva R., Baruzzi A. Clobazam plasma concentrations: pharmacokinetic study in healthy volunteers and data in epileptic patients. Br J Clin Pharmacol. 1981 Jun;11(6):619–622. doi: 10.1111/j.1365-2125.1981.tb01180.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Volz M., Christ O., Kellner H. M., Kuch H., Fehlhaber H. W., Gantz D., Hajdu P., Cavagna F. Kinetics and metabolism of clobazam in animals and man. Br J Clin Pharmacol. 1979;7 (Suppl 1):41S–50S. doi: 10.1111/j.1365-2125.1979.tb04664.x. [DOI] [PMC free article] [PubMed] [Google Scholar]