Clobazam binds to one or more specific GABA receptors at several sites within the CNS including the limbic system and reticular formation. Increased permeability of neuronal membrane to chloride ions results in GABA’s inhibitory effect leading to hyperpolarisation and stabilisation.

Absorption
Well absorbed from the GI tract (oral); peak plasma concentrations after 1-4 hours.

Distribution
Rapidly crosses the blood-brain barrier. Protein-binding: 85%.

Metabolism
Hepatic by demethylation and hydroxylation.

Excretion
Urine (as unchanged drug and metabolites); 18- 42 hours (elimination half-life).

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Constipation, anorexia, nausea; dizziness, fine tremors; worsening of respiratory symptoms in predisposed individuals; ataxia, drowsiness, headache, confusion; loss of libido, motor dysfunction; dependence; visual disturbances and weight gain.
Potentially Fatal: Respiratory depression.

Overdosage
Drowsiness, mental confusion, lethargy, ataxia, hypotonia, hypotension, respiratory depression, coma and very rarely death. Treatment includes emptying stomach by inducing vomiting (if within 1 hour) or gastric lavage. Activated charcoal may be used to reduce absorption. Monitor respiratory and CV functions. Flumazenil may be given if necessary. Forced diuresis or haemodialysis unlikely to be effective.

May impair ability to perform skilled tasks and hazardous activities; elderly; renal or hepatic impairment; alcoholics; obesity; withdrawal should be gradual.

Increased hepatic clearance of clobazam when administered with phenytoin, phenobarbital or carbamazepine. Cimetidine may increase levels of clobazam.

Potentially Fatal: Concurrent alcohol, hypnotics and sedative antidepressants can potentiate CNS side effects of clobazam.

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Oral
Short-term management of anxiety, Adjunct in epilepsy
Adult: 20-30 mg as a single dose at night or as daily divided doses, increased to 60 mg/day in severe conditions.
Child: 3-12 years: 125 mcg/kg bid increased every 5 days. Usual maintenance dose: 250 mcg/kg bid. Max: 500 mcg/kg bid.
Elderly: or debilitated patients: 10-20 mg daily.

Renal impairment: Dose adjustment may be needed.
Hepatic impairment: Dose adjustment may be needed.

May be taken with or without food

Contraindicated in pregnancy

Contraindicated in lactation

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Hypersensitivity; history of drug dependence; myasthaenia gravis; pregnancy (1st trimester), lactation; serious liver damage; sleep apnoea syndrome; impaired respiratory function.

Oral
Store at 15-30°C.

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