Overdose accidental or otherwise. ABCs, monitor O₂ sats and give oxygen. Ensure ability to manage respiratory depression and airways issues. Respiratory and airway support. Flumazenil may be given with caution.
- Long acting Benzodiazepine
- Active metabolites have a half-life of 100 hours
Mode of action
- Binds to a receptor on the GABA(A) receptor-chloride ionophore complex.
- Does not bind to the active site where GABA itself binds
- Enhances the effect of GABA the main inhibitory neurotransmitter in CNS
- GABA(A) receptor are ligand-gated ion channels
- Increases the frequency of Cl- channel opening and potentiating GABA transmission
Indications
- Anticonvulsant, Anxiolytic, Muscle relaxant, Hypnotic for insomnia, Premedication
- Myoclonus, Amnesia - useful for unpleasant procedures, Alcohol withdrawal
Dose
- Anxiety/Sedation : Diazepam 2-5 mg tds up to 30 mg per day in divided doses
- Status Epilepticus: Diazepam 5-10 mg slow iv (Diazemuls is less irritating) which may be repeated. Up to 20 mg.
Contraindications
- Operating machinery, Sleep apnoea syndrome
- Use with other sedation/alcohol
- Respiratory depression, Respiratory muscle weakness
- Myasthenia gravis, muscle weakness
Cautions
- Driving/operating machinery due to sedation
- Reduce dose in elderly, renal or liver failure
Side effects
- Respiratory depression, sedation, drowsiness, amnesia
- Rebound insomnia on stopping, Amnesia, Tolerance, Withdrawal
- Drowsiness, Ataxia, reduced psychomotor performance
- Dependence after 4-6 weeks with a withdrawal syndrome
- Long-acting metabolites e.g. with Diazepam can give hangover effects
Interactions
- Effects are reversed by Flumazenil but risk of rebound seizure
- Caution with other sedative medications and olanzapine
- p450 enzyme inhibitors can increase diazepam levels - See BNF/Datasheet
References