Diazepam

Azepam is indicated for the short-term treatment of mild to moderate anxiety, excitation, agitation, fear, aggressiveness, etc. Anxiety reactions caused by stressed conditions, anxiety states with somatic expression, acute alcohol withdrawal, status epilepticus, premedication for surgical procedures
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Azepam is indicated for the short-term treatment of mild to moderate anxiety, excitation, agitation, fear, aggressiveness, etc. Anxiety reactions caused by stressed conditions, anxiety states with somatic expression, acute alcohol withdrawal, status epilepticus, premedication for surgical procedures, febrile convulsions, insomnia of hospitalized patients.
Azepam nasal spray is indicated for the acute treatment of intermittent, stereotypic episodes of frequent seizure activity (i.e., seizure clusters, acute repetitive seizures) that are distinct from a patient’s usual seizure pattern in patients with epilepsy 6 years of age and older.

Oral
:
Anxiety: 2 mg thrice daily, increased if necessary to 15-30 mg daily in divided doses. Elderly (or debilitated), half of the adult dose.
Insomnia associated with anxiety: 5-15 mg at bedtime.
Night terrors and somnambulism in Child: 1-5 mg at bedtime.
Injection
(large vein, a rate below 5 mg/minute):
For severe acute anxiety, control of acute panic attacks, and acute alcohol withdrawal: 10 mg repeated if necessary after not less than 4 hours.
Febrile convulsion in children: Slow IV in a dose of 250 mcg/kg.
Rectal
: In case of children- A dose of 500 mcg/kg (maximum 10 mg), repeated if necessary.
Nasal spray
: The recommended dose of Diazepam nasal spray is 0.2 mg/kg or 0.3 mg/kg, depending on the patient’s age and weight. A second dose, when required, may be administered after at least 4 hours after the initial dose. Do not use more than 2 doses to treat a single episode. It is recommended that Diazepam nasal spray be used to treat no more than one episode every five days and no more than five episodes per month.

Azepam is generally well tolerated. Higher doses may cause somnolence, dizziness, light headedness, confusion and ataxia.

Diazepam attaches to the specific site on the GABA receptor and potentiates the effect of GABA, which acts by opening chloride ion channels into cells.
Diazepam is absorbed rapidly and completely after oral administration. Peak Plasma concentration reaches within 15-90 minutes. Mean plasma half-life is 30 hours. Plasma protein binding is 98-99%. Diazepam is metabolized in the liver with only traces of the unchanged drug excreted in urine. A very small proportion of the metabolites is excreted through the bile into the intestine and eliminated with the feces. After rectal administration in suppository form diazepam is significantly absorbed and peak concentration reaches within 1.5-2 hours.