Diazepam is indicated for the short-term treatment of mild to moderate anxiety, excitation, agitation, fear, and aggressiveness. It is also used in anxiety reactions caused by stress, anxiety states with somatic symptoms, acute alcohol withdrawal, status epilepticus, premedication for surgical procedures, febrile convulsions, and insomnia in hospitalized patients.

Diazepam is a benzodiazepine derivative and a safe tranquillizer with anxiolytic, anticonvulsant, and central muscle relaxant properties. Intravenous diazepam is widely used in obstetric practice and in the management of status epilepticus.

Diazepam binds to specific sites on the GABA receptor and enhances the effect of GABA, which works by opening chloride ion channels into cells, producing inhibitory effects in the central nervous system.

Diazepam is rapidly and completely absorbed after oral administration. Peak plasma concentration is reached within 15–90 minutes. Mean plasma half-life is approximately 30 hours. Plasma protein binding is about 98–99%. It is metabolized in the liver, with only trace amounts of unchanged drug excreted in urine. A small portion of metabolites is excreted via bile into the intestine and eliminated in feces. After rectal administration in suppository form, diazepam is significantly absorbed, with peak plasma concentration occurring within 1.5–2 hours.

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.

IM/slow IV 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.

Concomitant use of alcohol is not recommended. Sedation may be enhanced when Diazepam is used together with neuroleptics (antipsychotics), hypnotics, sedating antihistamines, and other CNS depressants such as general anaesthetics, narcotic analgesics, or antidepressants. Diazepam clearance is increased when used with phenobarbital, and decreased when used with cimetidine. Omeprazole and isoniazid may inhibit diazepam metabolism.

Diazepam is contraindicated in myasthenia gravis, pulmonary insufficiency, respiratory depression, and hypersensitivity to benzodiazepines.

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

Diazepam and its active metabolites cross the placental barrier and are excreted into breast milk. Therefore, its use should be avoided during pregnancy and lactation if possible. US FDA Pregnancy Category D.

Prolonged use and abrupt withdrawal should be avoided. Diazepam should be used with caution in patients with respiratory disease, muscle weakness, history of drug or alcohol abuse, and in hepatic or renal impairment.

Symptoms may include sedation, muscle weakness, deep sleep, or paradoxical excitation. In severe cases, ataxia, hypotonia, hypotension, respiratory depression, and rarely coma or death may occur.

Benzodiazepine sedatives, centrally acting skeletal muscle relaxants, primary anti-epileptic drugs.

Store in a cool (below 25°C) and dry place, protected from light.