Paper I
2013 September (Supplementary) (2010 Scheme) · 40 marks · 120 min

Question

Diazepam

Q73 marksShort Notes

Answer

Diazepam is a long-acting benzodiazepine.

Mechanism of action

  • Binds to a specific benzodiazepine site on the GABA-A receptor
  • Increases the frequency of chloride channel opening in response to GABA → enhances GABA-mediated (inhibitory) neurotransmission → CNS depression

Uses

  • Anxiety disorders
  • Status epilepticus (drug of choice, IV)
  • Skeletal muscle spasm/spasticity
  • Alcohol withdrawal syndrome
  • Premedication before anaesthesia/procedural sedation
  • Muscle relaxant in tetanus

Adverse effects

  • Sedation, drowsiness, ataxia
  • Dependence and tolerance with prolonged use
  • Withdrawal syndrome on abrupt discontinuation
  • Respiratory depression (especially with other CNS depressants/IV use)
  • Anterograde amnesia

Antidote: Flumazenil (competitive benzodiazepine receptor antagonist)

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