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Diazepam: Indications, Dosage and Precautions




Diazepam, a benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant and amnesic properties. Its actions are mediated by enhancement of the activity of aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain. On oral administration, diazepam is readily and completely absorbed from the gastrointestinal tract, peak plasma concentration occurring within about 30 to 90 minutes. 
Diazepam, a benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant


It has a biphasic half-life with an initial rapid distribution phase followed by a prolonged terminal elimination phase of 1 or 2 days, its action is further prolonged by the even longer half-life of 2 to 5 days of its principal active metabolite desmethyldiazepam. Diazepam is extensively metabolized in the liver and is excreted in the urine, mainly in the form of its metabolites, either free or in conjugated form.

Indications

Diazepam is used in the treatment of severe anxiety disorders, as hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant particularly in the management of status epilepticus and febrile convulsions, in the control of muscle spasm as in tetanus and in management  of alcohol withdrawal symptoms.



Dosage 

·        Anxiety disorders: 2mg three times daily, increased up to 30 mg daily in divided doses
·        Insomnia associated with anxiety: a single dose of 5mg to 30 mg before retiring to bed
·        Muscle spasm: 2mg to 15 mg daily in divided doses increased in severe spastic disorders, such as cerebral palsy. As an adjunctive in some types of epilepsy up to 60 mg daily in divided doses
·        Management of mild to moderate symptoms of alcohol withdrawal: 5-20 mg, repeated if necessary in 2 to 4 hours or 10 mg 3 to 4 times on the first day reducing to 5 mg 3 to 4 times daily as required. 

      For premedication before dental or minor surgical procedures: a single dose of 5mg to 20 mg

Children
The recommended initial dose of diazepam for children is 0.1 mg to 0.2 mg per kg body weight orally but up to 0.8 mg per kg body weight daily has been given. Dosage recommendation of diazepam for premature infants is not generally given since they may be unable to metabolize the drug.

Precautions, warning and adverse-effects

·        Calm-5 should be avoided in patients with pre-existing CNS depression or coma, acute pulmonary insufficiency or sleep apnoea, and used with caution in those with chronic pulmonary insufficiency, impaired hepatic or renal function and in elderly or debilitated patients
·        Calm-5 are contraindicated in patients with known hypersensitivity to diazepam or other benzodiazepines and in those with chronic psychosis or phobic or obsessional states.
·        The preparation is not recommended for use in pregnant patients during the first trimester or late pregnancy



·        Drug dependence may develop after regular use of diazepam or other benzodiazepines, even in therapeutic doses for short periods.
·        The most frequent adverse effects occasionally associated with diazepam therapy include, drowsiness, sedation and ataxia and other less frequent effects include vertigo, headache, confusion, mental depression, slurred speech or dysarthria, changes in libido, tremor, visual disturbances, urinary incontinence, gastrointestinal disturbances and hypersensitivity reactions.
·    
       It is recommended that withdrawal of diazepam therapy should be gradual as abrupt withdrawal may result in confusion, toxic psychosis, convulsions or a condition resembling delirium tremens

Diazepam: Indications, Dosage and Precautions Diazepam: Indications, Dosage and Precautions Reviewed by gafacom on September 30, 2019 Rating: 5

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