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Chemical name

7-Chloro-1-methyl-5-phenyl-H-1, 5- benzodiazepine-2, 4(3H, 5H)-dione.

Category

Antianxiey 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

  1. 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.
  2. Anxiety associated with psychosomatic disorders.
  3. Anxiety states in psychotic disorders.
  4. 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.
  5. 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.
  6. Use as an hypnotic.

Precautions to consider

Risk - 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 supplied

Tablets: Box of 100 Coated tablet. Each coated tablet contains 10mg clobazam.

Storage

Store below 30° C , protect from light and moisture.

References

  1. Martindale, the complete drug reference 32nd edition.
  2. Therapeutic drugs, 2nd Edition.

   
 

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