Drug information of Clobazam

Mechanism of effect

Binds to the benzodiazepine site of the GABA A receptor and potentiates GABAergic neurotransmission.

Pharmacodynamic

Binds to the benzodiazepine site of the GABA A receptor and potentiates GABAergic neurotransmission.

Pharmacokinetics

Rapidly and extensively absorbed. Bioavailability is approximately 100%. T max is 0.5 to 4 h. Extensively metabolized in the liver by N-demethylation, primarily by CYP3A4 . The half-life is 36 to 42 h. Approximately 82% is excreted in the urine and 11% in the feces.

Drug indications

Adjunctive treatment of seizures associated with Lennox-Gastaut syndrome.

Dosage

Usual Adult Dose for Lennox-Gastaut Syndrome Clobazam should be administered in divided doses twice daily (the 5 mg dose can be administered as a single daily dose). Dose escalation should not proceed more rapidly than every 7 days and dosing within each body weight group should be individualized. Initial total daily dose: Body weight 30 kg or less: 5 mg orally daily Body weight 30 kg or more: 10 mg orally daily Starting day 7 total daily dose: Body weight 30 kg or less: 10 mg orally daily Body weight 30 kg or more: 20 mg orally daily Starting day 14 total daily dose: Body weight 30 kg or less: 20 mg orally daily Body weight 30 kg or more: 40 mg orally daily

Side effects

insomnia , constipation , decreased appetite , vomiting , fatigue , irritability , Blurred vision , rash , Depression , urticaria , thrombocytopenia , leukopenia , anemia , Urinary tract infection , Cough , fever , anxiety , Stevens-Johnson syndrome , somnolence , Upper respiratory tract infection , bronchitis , dysphagia , Increased ALT , Increased AST , agitation , ataxia , pneumonia , lethargy , hallucinations , Diplopia

Interactions

Olopatadine , Drospirenone , Zolpidem , Cetirizine , Medroxyprogesterone , Neostigmine , Aripiprazole , Aminophiline , Acetaminophen+codine , Expectorant codein , Desogestrol , Fluvoxamine , Fluconazole , Midazolam , Ketoconazole , Clozapine , Yohimbine , Bisoprolol , Tapentadol , codeine , Axitinib , Procaine , Entrectinib , Oxymorphone , Ethchlorvynol , Eliglustat , Cannabidiol , Avapritinib

Alerts

1-Monitor patients for somnolence and sedation, particularly with concomitant use of other CNS depressants. 2-Carefully monitor patients with a history of substance abuse because of the predisposition of such patients to habituation and dependence. 3-Monitor patients for the emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior. 4-Safety and efficacy not established in patients younger than 2 y.

Points of recommendation

1-Patients should not engage in hazardous activities requiring mental alertness (eg, operating machinery or motor vehicles) until the effect of clobazam is known. 2-Avoid abrupt discontinuation of clobazam; withdrawal symptoms may occur with abrupt discontinuation, 3-May occur and risk is present even with use at recommended doses over a period of only a few weeks.

Pregnancy level

C

Related drugs

Alprazolam , Midazolam