Abstract
Camazepam (7-chloro-3-N,N-dimethylcarbamoyloxy-s-phenyl-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one) has the pharmacological profile of an anxiolytic agent with a clear separation between anxiolytic action and sedative-depressive side effects. Studies of the metabolism of camazepam indicate that the compound is excreted in the urine of several animal species, partly free and partly as N-methyl-oxazepam and oxazepam glucuronides. N-Methyl-oxazepam and oxazepam are pharmacologically active metabolites and may be considered possible contributors to the central nervous system activity of the parent compound. This hypothesis was investigated in the present experiments by comparing brain concentrations of N-methyl-oxazepam and oxazepam after administration of the two metabolites or of camazepam at doses effective against leptazol (pentetrazole) induced convulsions. These findings indicate that the anti-leptazol activity of oral camazepam in the rat is dependent more on the brain concentrations of active metabolites than on the parent compound. However, these conclusions only concern the antileptazol activity of camazepam in the rat. Further studies are needed to see how much the metabolites contribute to other pharmacological effects of camazepam.
| Original language | English |
|---|---|
| Pages (from-to) | 185-187 |
| Number of pages | 3 |
| Journal | Journal of Pharmacy and Pharmacology |
| Volume | 33 |
| Issue number | 3 |
| Publication status | Published - 1981 |
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ASJC Scopus subject areas
- Pharmaceutical Science
- Pharmacology
Cite this
Relationship between camazepam, N-methyl-oxazepam brain concentrations and antileptazol effect in the rat. / Caccia, S.; Ballabio, M.; Garattini, S.
In: Journal of Pharmacy and Pharmacology, Vol. 33, No. 3, 1981, p. 185-187.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Relationship between camazepam, N-methyl-oxazepam brain concentrations and antileptazol effect in the rat
AU - Caccia, S.
AU - Ballabio, M.
AU - Garattini, S.
PY - 1981
Y1 - 1981
N2 - Camazepam (7-chloro-3-N,N-dimethylcarbamoyloxy-s-phenyl-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one) has the pharmacological profile of an anxiolytic agent with a clear separation between anxiolytic action and sedative-depressive side effects. Studies of the metabolism of camazepam indicate that the compound is excreted in the urine of several animal species, partly free and partly as N-methyl-oxazepam and oxazepam glucuronides. N-Methyl-oxazepam and oxazepam are pharmacologically active metabolites and may be considered possible contributors to the central nervous system activity of the parent compound. This hypothesis was investigated in the present experiments by comparing brain concentrations of N-methyl-oxazepam and oxazepam after administration of the two metabolites or of camazepam at doses effective against leptazol (pentetrazole) induced convulsions. These findings indicate that the anti-leptazol activity of oral camazepam in the rat is dependent more on the brain concentrations of active metabolites than on the parent compound. However, these conclusions only concern the antileptazol activity of camazepam in the rat. Further studies are needed to see how much the metabolites contribute to other pharmacological effects of camazepam.
AB - Camazepam (7-chloro-3-N,N-dimethylcarbamoyloxy-s-phenyl-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one) has the pharmacological profile of an anxiolytic agent with a clear separation between anxiolytic action and sedative-depressive side effects. Studies of the metabolism of camazepam indicate that the compound is excreted in the urine of several animal species, partly free and partly as N-methyl-oxazepam and oxazepam glucuronides. N-Methyl-oxazepam and oxazepam are pharmacologically active metabolites and may be considered possible contributors to the central nervous system activity of the parent compound. This hypothesis was investigated in the present experiments by comparing brain concentrations of N-methyl-oxazepam and oxazepam after administration of the two metabolites or of camazepam at doses effective against leptazol (pentetrazole) induced convulsions. These findings indicate that the anti-leptazol activity of oral camazepam in the rat is dependent more on the brain concentrations of active metabolites than on the parent compound. However, these conclusions only concern the antileptazol activity of camazepam in the rat. Further studies are needed to see how much the metabolites contribute to other pharmacological effects of camazepam.
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M3 - Article
C2 - 6116765
AN - SCOPUS:0019429360
VL - 33
SP - 185
EP - 187
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
SN - 0022-3573
IS - 3
ER -