Pharmacology Of Clobazam

Indication For treatment and management of epilepsy and anxiety disorder.
Pharmacodynamics Clobazam is a barbiturate used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain.
Mechanism of action Clobazam binds at a distinct binding site associated with a Cl- ionopore at the GABA-A receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is prolonged as a result.
Absorption Bioavailability is 90%.
Volume of distribution Not Available
Protein binding 83%
Metabolism Hepatic. Clobazam has two major metabolites: N-desmethyl-clobazam and 4'-hydroxyclobazam, the former of which is active. The demethylation is facilitated by CYP2C19, CYP3A4, and CYP2B6 and the 4'-hydroxyclobazam by CYP2C18 and CYP2C19.
Route of elimination Not Available
Half life 18 hours
Clearance Not Available
Toxicity Not Available