Abstract
1. The single dose pharmacokinetics of N-desmethylclobazam (NDMC) and clobazam were studied in eight healthy male volunteers. 2. Steady-state pharmacokinetic data are described from four healthy male volunteers and eight epileptic patients taking NDMC. 3. A single 30 mg dose of NDMC produced a greater Cmax (P less than 0.001) and AUC0-infinity (P less than 0.005) and a shorter tmax (P less than 0.05) and t1/2 (P less than 0.01) for NDMC than did 30 mg clobazam. 4. Mean steady-state NDMC concentrations were greater in male patients than in female patients and also in male patients compared with male volunteers. The differences between patients and volunteers might be explained by concomitant antiepileptic medication.
Full text
PDFSelected References
These references are in PubMed. This may not be the complete list of references from this article.
- Aranko K., Mattila M. J., Seppälä T., Aranko S. The contribution of the active metabolites to the tolerance developing to diazepam in man: relationship to bioassayed serum benzodiazepine levels. Med Biol. 1984;62(5):277–284. [PubMed] [Google Scholar]
- Callaghan N., Goggin T. Clobazam as adjunctive treatment in drug resistant epilepsy--report on an open prospective study. Ir Med J. 1984 Aug;77(8):240–244. [PubMed] [Google Scholar]
- Frey H. H., Philippin H. P., Scheuler W. Development of tolerance to the anticonvulsant effect of diazepam in dogs. Eur J Pharmacol. 1984 Sep 3;104(1-2):27–38. doi: 10.1016/0014-2999(84)90365-0. [DOI] [PubMed] [Google Scholar]
- Greenblatt D. J., Divoll M., Abernethy D. R., Ochs H. R., Shader R. I. Clinical pharmacokinetics of the newer benzodiazepines. Clin Pharmacokinet. 1983 May-Jun;8(3):233–252. doi: 10.2165/00003088-198308030-00003. [DOI] [PubMed] [Google Scholar]
- Haigh J. R., Pullar T., Gent J. P., Dailley C., Feely M. N-desmethylclobazam: a possible alternative to clobazam in the treatment of refractory epilepsy? Br J Clin Pharmacol. 1987 Feb;23(2):213–218. doi: 10.1111/j.1365-2125.1987.tb03032.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Jawad S., Richens A., Oxley J. Single dose pharmacokinetic study of clobazam in normal volunteers and epileptic patients. Br J Clin Pharmacol. 1984 Dec;18(6):873–877. doi: 10.1111/j.1365-2125.1984.tb02558.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Pullar T., Edwards D., Haigh J. R., Peaker S., Feely M. P. The effect of cimetidine on the single dose pharmacokinetics of oral clobazam and N-desmethylclobazam. Br J Clin Pharmacol. 1987 Mar;23(3):317–321. doi: 10.1111/j.1365-2125.1987.tb03051.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ratnaraj N., Goldberg V., Lascelles P. T. Determination of clobazam and desmethylclobazam in serum using high-performance liquid chromatography. Analyst. 1984 Jul;109(7):813–815. doi: 10.1039/an9840900813. [DOI] [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]