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Indications

BEERS REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN)

GI: constipation, drooling, dysphagia, vomiting

Metab: appetite

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

Resp: cough

Misc:

physical dependence

,

psychological dependence

Interactions

Drug-drug:

Availability

(Generic available)

Route/Dosage

Hepatic Impairment

Hepatic Impairment

US Brand Names

Onfi, Sympazan

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.

Classifications

Therapeutic Classification: anticonvulsants

Pharmacologic Classification: benzodiazepines

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 as active as the parent compound and is further metabolized by the CYP2C19 isoenzyme. The CYP2C19 isoenzyme exhibits genetic polymorphism (2% of White patients, 4% of Black patients, and 14% of Asian patients 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.

Contr. Subst. Schedule

Schedule IV (C-IV)

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
POunknown0.5–4 hr12–24 hr

Patient/Family Teaching

Pronunciation

KLOE-ba-zam

Code

NDC Code