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 |