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A review of the animal pharmacology of clobazam: An update

Stuart Fielding, Harbans Lal

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Abstract

Clobazam is a 1, 5-benzodiazepine with significant activity in preclinical tests predictive of potential clinical antianxiety activity. Clinical efficacy equivalent to diazepam has been established with minimal effects on psychomotor performance. Clobazam has also been found to have a broad spectrum of anticonvulsant activity with acceptable toxicity and to be active in suppressing aggressive behavior in rodents. This compound appears to have less of an effect on motor coordination, muscle tone, behavioral depression and hyporeflexia than standard reference compounds in various species as well as little or no apparent effect on memory and learning in animals and humans. The major metabolite, desmethylclobazam, is also an anxiolytic candidate approximately 10 times less potent than diazepam and a potent anticonvulsant with a complete lack of sedation. These compounds represent a new classification of pharmaceutical agents in which antianxiety and anticonvulsant effects can be achieved without sedative or depressive side effects.

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Clobazam is a 1, 5-benzodiazepine with significant activity in preclinical tests predictive of potential clinical antianxiety activity. Clinical efficacy equivalent to diazepam has been established with minimal effects on psychomotor performance. Clobazam has also been found to have a broad spectrum of anticonvulsant activity with acceptable toxicity and to be active in suppressing aggressive behavior in rodents. This compound appears to have less of an effect on motor coordination, muscle tone, behavioral depression and hyporeflexia than standard reference compounds in various species as well as little or no apparent effect on memory and learning in animals and humans. The major metabolite, desmethylclobazam, is also an anxiolytic candidate approximately 10 times less potent than diazepam and a potent anticonvulsant with a complete lack of sedation. These compounds represent a new classification of pharmaceutical agents in which antianxiety and anticonvulsant effects can be achieved without sedative or depressive side effects.

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Available abstract

Clobazam is a 1, 5-benzodiazepine with significant activity in preclinical tests predictive of potential clinical antianxiety activity. Clinical efficacy equivalent to diazepam has been established with minimal effects on psychomotor performance. Clobazam has also been found to have a broad spectrum of anticonvulsant activity with acceptable toxicity and to be active in suppressing aggressive behavior in rodents. This compound appears to have less of an effect on motor coordination, muscle tone, behavioral depression and hyporeflexia than standard reference compounds in various species as well as little or no apparent effect on memory and learning in animals and humans. The major metabolite, desmethylclobazam, is also an anxiolytic candidate approximately 10 times less potent than diazepam and a potent anticonvulsant with a complete lack of sedation. These compounds represent a new classification of pharmaceutical agents in which antianxiety and anticonvulsant effects can be achieved without sedative or depressive side effects.

Key concepts: Clobazam, Anxiolytic, Hyporeflexia, Pharmacology, Anticonvulsant, Diazepam, Sedative, Sedation

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