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QuickView for Clobazam (compound)


PubChem
Name: clobazam
PubChem Compound ID: 2789
Molecular formula: C16H13ClN2O2
Molecular weight: 300.739 g/mol
Synonyms:
EINECS 244-908-7; BRN 0758410; Mystan (TN); nchembio747-comp39; H-4723; 1-Phenyl-5-methyl-8-chloro-1,2,4,5-tetrahydro-2,4-dioxo-3H-1, 5-benzodiazepine; Clobazam [USAN:BAN:INN]; Urbanyl; Clobazam; Clobazamum [INN-Latin].
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DrugBank
Identification
Name: clobazam
Name (isomeric): DB00349
Drug Type: small molecule
Brand: Urbadan, Chlorepin, Frisium, Mystan, Urbanyl, Clorepin
Category: Benzodiazepines, Anticonvulsants
CAS number: 22316-47-8
Pharmacology
Indication: For treatment and management of epilepsy and anxiety disorder.
Pharmacology: 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%.
Protein binding: 83%
Biotransformation: 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.
Half Life: 18 hours
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Alcohol increases clobazam absorption by 50%.
Take without regard to meals.
Drug interaction:
TelithromycinTelithromycin may reduce clearance of Clobazam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Clobazam if Telithromycin is initiated, discontinued or dose changed.
KavaKava may increase the effect of the benzodiazepine, clobazam.
VoriconazoleVoriconazole may increase the serum concentration of clobazam by decreasing its metabolism. Monitor for clobazam toxicity if voriconazole is initiated or dose increased.
TipranavirTipranavir may decrease the metabolism and clearance of Clobazam. Consider alternate therapy or monitor for Clobazam toxic effects if Tipranavir is initiated or dose increased.
TiclopidineTiclopidine may decrease the metabolism and clearance of Clobazam. Consider alternate therapy or monitor for adverse/toxic effects of Clobazam if Ticlopidine is initiated, discontinued or dose changed.
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