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Chemical
name3 H - 1, 4 -
Benzodiazepin - 2 - amine, 7 - chloro - N - methyl - 5 - phenyl -, 4 -
oxide.
CategoryAntianxiety agent; Sedative - hypnotic;
Antitremor 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 alI regions of the
CNS, following interaction between the benzodiazepine and a specific
neuronal membrane receptor. Antianxiety agent; sedative - hypnotic -
Believed to stimulate GABA receptors in the ascending reticular activating
system. Since GABA is inhibitory, receptor stimulation increases
inhibition and blocks both cortical and limbic arousal following
stimulation of the brain stem reticular formation.
Indications
- Anxiety (treatment) -Chlordiazepoxide is indicated for
the management of anxiety disorders or for the short - term relief of the
symptoms of anxiety and treatment of preoperative apprehension and
anxiety. - Alcohol withdrawal (treatment) - It is indicated for the
relief of acute alcohol withdrawal symptoms such as acute agitation,
tremor, impending or acute delirium tremens, and hallucinosis. -
Headache, tension - Tremors (treatment) - It is used in the treatment of
tension headache, familial, senile, or essential action tremors.
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, severe -
Myasthenia gravis - Organic brain disorders - Porphyria - Psychoses -
Sensitivity to benzodiazepines - Sleep apnea.
Pregnancy / Breast -
feeding
Chlordiazepoxide crosses the placenta and has been
reported to increase the risk of congenital malformations when used during
the first trimester of pregnancy. Chronic usage of benzodiazepines
during pregnancy may cause physical dependence with resulting withdrawal
symptoms in the neonate. Use of benzodiazepine hypnotics during the last
weeks of pregnancy may result in neonatal CNS
depression. Chlordiazepoxide may be distributed into breast milk. Since
neonates metabolize benzodiazepines more slowly than adults and
accumulation of the benzodiazepine and / or its metabolites may occur.
Drug
interactions
Combinations containing any of the following medications,
depending on the amount present, may also interact with this
medication: Alcohol or CNS depression - producing medications;
Antacids; Cimetidine; Clozapine; Hypotension - producing medications;
Levodopa; Zidovudine; Theophyllines; Erythromycin; Contraceptives - oral.
Side / Adverse
effects
Those indicating need for medical attention. Incidence
less frequent: Intolerance to benzodiazepines (confusion); mental
depression. Incidence rare: Allergic reaction; blood dyscrasias;
extrapyramidal effects, dystonic; hepatic dysfunction; hypotension; memory
impairment; muscle weakness ; paradoxical reactions ; phlebitis or venous
thrombosis; behavior problems.
Administration and
dosage
Usual adult dose: Antianxiety agent - Oral, 5
to 25 mg 3 or 4 times a day. Sedative - hypnotic; Alcohol withdrawal -
Oral, 50 to 100 mg initially, repeated as needed, up to 400 mg per day,
the dosage then reduced to maintenance levels. Usual pediatric
dose: Antianxiety agent - Children up to 6 years of age: Safety and
efficacy have not been established. Children 6 years of age and over:
Oral, 5 mg 2 to 4 times a day, the dosage being increased, if necessary,
to 10 mg 2 or 3 times a day. Usual geriatric
dose: Antianxiety agent - Oral, 5 mg 2 to 4 times a day, the dosage
being increased gradually as needed and tolerated.
How
supplied1 - Tablets: Box of
100 coated tablets. Each coated tablet contains 5 mg
chlordiazepoxide. 2 - Tablets: Box of 100 coated tablets. Each coated
tablet contains 10 mg chlordiazepoxide.
StorageStore below 30° C, protect from light and
moisture.
References1 - USP DI (1997) Vol: 1 - Pages: 532 -
540. 2 - Drug facts and comparisons 1994. 3 - USP 23 page: 340.
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