section name header

Pronunciation

KLOE-ba-zam

Classifications

Therapeutic Classification: anticonvulsants

Pharmacologic Classification: benzodiazepines

Indications

BEERS REMS


Action

  • Facilitates neurotransmission mediated by gamma-amino butyric acid (GABA) by binding to the benzodiazepine site of the GABAAreceptor.
Therapeutic effects:
  • Decreased incidence and severity of seizures associated with Lennox-Gestaut syndrome.

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Rapidly distributes throughout the body.

Metabolism/Excretion: Primarily metabolized in the liver by the CYP3A4 isoenzyme, with some metabolism by the CYP2C19 and CYP2B6 isoenzymes. Major circulating metabolite, desmethylclobazam, is 1/5 as active as the parent compound and is further metabolized by the CYP2C19 isoenzyme. The CYP2C19 enzyme system exhibits genetic polymorphism (2% of Whites, 4% of Blacks, and 14% of Asians may be poor metabolizers and may have significantly desmethylclobazam concentrations and an risk of adverse effects).2% excreted unchanged in urine, 1% in feces.

Half-Life: Clobazam: 36–42 hr; desmethylclobazam: 71–82 hr.

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
POunknown0.5–4 hr12–24 hr



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Derm: STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS

GI: constipation, drooling, dysphagia, vomiting

Metab: appetite

Neuro: sedation, somnolence, aggression, ataxia, dizziness, dysarthria, fatigue, insomnia, irritability, lethargy

Resp: cough

Interactions

Drug-drug:

Route/Dosage

Hepatic Impairment

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Onfi, Sympazan

Contr. Subst. Schedule

Schedule IV (C-IV)

Code

NDC Code