Literature DB >> 6103027

Species differences in clobazam metabolism and antileptazol effect.

S Caccia, G Guiso, R Samanin, S Garattini.   

Abstract

The antileptazol effect of clobazam lasts longer in the mouse than in the rat. After intraperitoneal injection of clobazam (10 mg kg-1) plasma and brain concentrations of the drug and its rate of disappearance were similar in both species, whereas the metabolite N-demethylclobazam was present at higher concentrations and for longer in the mouse than in the rat. Although the exact contribution of the N-desmethylclobazam to the anticonvulsant effect of clobazam cannot be assessed, the longer duration in mice than in rats seems to be associated with different brain accumulations of the metabolite.

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Year:  1980        PMID: 6103027     DOI: 10.1111/j.2042-7158.1980.tb12861.x

Source DB:  PubMed          Journal:  J Pharm Pharmacol        ISSN: 0022-3573            Impact factor:   3.765


  5 in total

Review 1.  Formation of active metabolites of psychotropic drugs. An updated review of their significance.

Authors:  S Caccia; S Garattini
Journal:  Clin Pharmacokinet       Date:  1990-06       Impact factor: 6.447

Review 2.  Disposition of anticonvulsants in childhood.

Authors:  J I Morrow; A Richens
Journal:  Clin Pharmacokinet       Date:  1989       Impact factor: 6.447

3.  Antileptazol activity and kinetic of CP 1414 S (7-nitro-2-amino-5-phenyl-3-H-,1,5-benzodiazepine-4-one) in the rat and mouse.

Authors:  S Caccia; M Ballabio; M G Zanini; S Garattini; R Samanin
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1982       Impact factor: 2.441

4.  Species differences in phenazepam kinetics and metabolism.

Authors:  V P Zherdev; S Caccia; S Garattini; A L Ekonomov
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1982       Impact factor: 2.441

5.  Receptor-mediated model relating anticonvulsant effect to brain levels of camazepam in the presence of its active metabolites.

Authors:  A Morino; H Sasaki; H Mukai; M Sugiyama
Journal:  J Pharmacokinet Biopharm       Date:  1986-06
  5 in total

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