Camazepam is a benzodiazepine which is a dimethyl carbamate ester of tamzepam, a metabolite of diazepam. Similarly to other drugs in its class, it has antxiolytic, anticonvulsant, hypnotic, and skeletal muscle relaxant properties. However, unlike other benzodiapeines camazepam is predominantly anxiolytic and is relatively weak as an anticonvulsant, hypnotic and skeletal muscle relaxant. [Wikipedia]
Camazepam also has less side effects, such as impaired cognition and reaction times, compared to other benzodiazepines. However, impairment of cognition and disrupted sleep patterns will occur at doses higher than 40mg of carazepam. [Wikipedia] Camazepam is also believed to increase attention, and is associated with skin disorders.
In the United States camazepam is regulated as a Schedule IV controlled substance.
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|Weight||Average: 371.818 |
|Description||This compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.|
|Super Class||Organoheterocyclic compounds|
|Molecular Framework||Aromatic heteropolycyclic compounds|
|External Descriptors||Not Available|
|Indication||Camazepam has been used in placebo controlled studies for the treatment of patients suffering from anxiety and depression.|
|Mechanism of action||Camazepam has been shown to bind competitively to benzodiazepine receptors in the brain with a relatively low affinity in animal models. This binding of benzodiazepine receptors by camazepam and its active metabolites is responsible for its anticonvulsant effects. Notably, only three metabolites were shown to exert anticonvulsant activity, temazepam, oxazepam, and hydroxy camazepam. The anxiolytic properties of camazepam are also attributed to their ability to bind benzodiazepine receptors, also known as GABA receptors. When benzodiazepines bind to GABA receptors they increase the efficiency with which the inhibitory neurotransmitter GABA binds.|
|Absorption||Almost completely absorbed into the bloodstream after oral administration. 90% bioavailability can be achieved in humans.|
|Volume of distribution||Not Available|
|Protein binding||Not Available|
Metabolized by the liver into more than 10 metabolites, some of which are also active and posses anticonvulsant properties.  One active metabolite of note is temazepam which has roughly equal in effectiveness as an anxiolytic, but is less anticonvulsant, sedating, and motor-impairing. Camazepam undergoes enantioselective metabolism by human liver microsomes. 
|Route of elimination||Renally eliminated.|
|Half life||Not Available|
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|Mass Spec (NIST)||Not Available|
Ferrari, G. and Casagrande, C.; U.S. Patent 3,799,920; March 26,1974; assigned to Siphar SA.
1. Lu, Xiang-Lin, and Shen K. Yang. “Enantiomer resolution of camazepam and its derivatives and enantioselective metabolism of camazepam by human liver microsomes.” Journal of Chromatography A 666.1 (1994): 249-257.
2. Morino, Akira, et al. “Receptor-mediated model relating anticonvulsant effect to brain levels of camazepam in the presence of its active metabolites.” Journal of pharmacokinetics and biopharmaceutics 14.3 (1986): 309-321.
3. Morino, A. K. I. R. A., and M. A. K. O. T. O. Sugiyama. “Relation between time courses of pharmacological effects and of plasma levels of camazepam and its active metabolites in rats.” Journal of pharmacobio-dynamics 8.8 (1985): 597.
|AHFS Codes||Not Available|
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