Benzodiazepines

Cards (11)

  • Examples:
    • Diazepam
    • Temazepam
    • Lorazepam
    • Chlordiazepoxide
  • MOA:
    • Increase affinity of GABA to bind to the GABA receptor
    • This causes post-synaptic chloride ions channels to open
    • GABA is an inhibitory neurotransmitter
  • Route of delivery:
    • PO
    • IM
    • IV - resuscitation facilities must be available
    • Buccal
    • Rectal
  • Indications:
    • Short-term treatment for severe, distressing or disabling anxiety
    • Treatment of seizures and status epilepticus
    • Short-term treatment for insomnia
    • Alcohol withdrawal - chlordiazepoxide
    • Tetanus, muscle spasm, acute drug-induced dystonia - diazepam
  • Contraindications:
    • Respiratory depression, respiratory failure and neuromuscular conditions e.g. unstable myasthenia gravis - benzodiazepines can cause loss of airway reflexes
    • Cautions - avoid in liver failure due to risk of hepatic encephalopathy, consider lower doses in elderly patients (more susceptible to side effects)
  • Interactions:
    • CYP450 inhibitors - azoles (antifungals), some antibiotics, omeprazole, sodium valproate, grapefruit
    • Alcohol and opioids - increased sedative effects
    • Clozapine - increased CNS depression
    • Anti-hypertensive mediation - increased hypotensive effects
  • Common side effects:
    • Amnesia, confusion, drowsiness
    • Muscle weakness and ataxia
    • Dependence
  • Benzodiazepines are sometimes used for severely agitated patients but a rare side effect is rebound agitation
  • Counselling:
    • For short term use only - no more than 4 weeks and should not be taken every day
    • Impairment of normal activities - driving, operating heavy machinery
    • Withdrawal effects - very addictive and can cause withdrawal symptoms when stopped
    • Stop alcohol consumption whilst on chlordiazepoxide
  • Withdrawal of a benzodiazepine should be gradual because abrupt withdrawal may produce confusion, toxic psychosis, convulsions, or a condition resembling delirium tremens.
  • Benzodiazepine withdrawal syndrome:
    • Insomnia
    • Anxiety
    • Anorexia
    • Tremor
    • Perspiration
    • Tinnitus
    • Perceptual disturbances