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Chemical
name7-Chloro-1-methyl-5-phenyl-H-1, 5-
benzodiazepine-2, 4(3H, 5H)-dione.
CategoryAntianxiey agent, Antiepileptic agent.
Mechanism of
action
It is believed that benzodiazepines enhance or facilitate
the inhibitory neurotransmitter action of gamma - aminobutyric acid
(GABA), which is one of the major inhibitory neurotransmitters in the
brain and mediates both pre - and post - synaptic inhibition in all
regions of the CNS, following interaction between the benzodiazepine and
specific neuronal membrane receptor. Antianxiety agent; sedative -
hypnotic - Believed to stimulate GABA receptors in the ascending reticular
activating system. Since GABA is inhibitory, receptor simulation increases
inhibition and blocks both cortical and limbic arousal following
stimulation of the brain stem reticular formation.
Indications
- Primary anxiety. Double - blind comparisons of Clobazam 20 to 80mg
daily with diazepam 10 to 40mg daily have generally not demonstrated any
significant difference between the anti - anxiety effect of the two
benzodiazepines.
- Anxiety associated with psychosomatic disorders.
- Anxiety states in psychotic disorders.
- Adjuvant therapy in epilepsy clobazam is active against partial and
generalized seizures in epilepsy of widely differing aetiology in
patients of all ages but is usually only indicated for adjunctive
therapy.
- The relief of acute anxiety and related insomnia caused by, for
example, fear of surgery and as adjunct therapy for epilepsy in children
aged more than 3 years.
- Use as an hypnotic.
Precautions to
considerRisk - Benefit
should be considered when the following medical problems exist: Alcohol
intoxication, acute, with depressed vital signs (additive CNS depression)
- Drug abuse or dependence, history of (patients predisposed to
habituation and dependence) - Glaucoma, angle - Closure, acute or
predisposition to (benzodiazepines may have anticholinergic effect) -
Hepatic and renal function impairment (elimination half - life may be
prolonged) - Hyperkinesis (paradoxical reactions may occur) -
Hypoalbuminemia - mental depression, sever - myasthenia gravis - Organic
brain disorders - Porphyria - Psychoses - Sensitivity to benzodiazepines -
Sleep apnea.
Pregnancy / Breast -
feeding
Clobazam may appear in the breast milk of nursing mothers
and breast - feeding is probably best avoided. Clobazam should not be used
in pregnancy, particularly during the first trimester.
Drug
interactions
The administration of alcohol resulted in significantly
higher serum concentration of clobazam. The concurrent administration of
hypnotics or antidepressants with sedative activity may cause an increase
in side effects, particularly tiredness or drowsiness. Carbamazepine
and phenytion increased N - dealkylation of clobazam, whereas valporic
acid and phenobarbital increased clobazam plasma concentrations.
Side / Adverse
effects
Drowsiness, vertigo, confusion, paradoxical excitation,
mental depression headache, visual disturbances, nausea, vomiting,
respiratory depression, mental and physical dependance.
Administration and
dosage
The usual dose for the shortterm treatment of anxiety is
20 to 30mg daily given in divided doses or as a single dose at night; in
severe conditions up to 60mg daily has been given. Similar daily doses
have been given as adjunctive therapy in the management of epilepsy.
How
suppliedTablets: Box of 100
Coated tablet. Each coated tablet contains 10mg clobazam.
StorageStore below 30° C , protect from light and
moisture.
References
- Martindale, the complete drug reference 32nd edition.
- Therapeutic drugs, 2nd Edition.
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