DIAZEPAM

1) Action

• Minor tranquilliser [sedative-hypnotic agent] of the benzodiazepine class

• Antianxiety ; sedative; muscle relaxant; anticonvulsant; amnesic

2) Mechanism

• Acts centrally on CNS in brain; CNS depressant

3) Indications

• Achievement of anaesthesia; premedication to reduce tension and anxiety; produce perioperative amnesia

• Status epilepticus, convulsions

4) Effects on organs—side effects

• Drowsiness, dizziness, ataxia

5) Toxic effects/ precautions with administration

• Prolonging of postoperative recovery

• Increased incidence of postoperative respiratory depression

• [One of the metabolites of diazepam is a CNS depressant, & this accounts for its prolonged duration of action]

• May exacerbate antihypertensive effect of antihypertensives

6) Contraindications

7) Reversal, antagonism or antidote

• Flumazenil: benzodiazepine-receptor antagonist

8) Loading dose, maintenance dose, frequency & method of administration

• 10 mg/ampoule

9) Drug’s metabolism—Drug’s excretion—Half life (pharmacokinetics)

• Metabolised by liver; excreted in faeces & urine

• Elimination half-life: 50-150 hours