Diazepam

Overdose accidental or otherwise. ABCs, monitor O2 sats and give oxygen. Respiratory and airway support. Flumazenil may be given with caution.

About:

•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 were 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 - clonazepam can act as an anticonvulsants with minimal sedation.

•Anxiolytic, Muscle relaxant, Hypnotic for insomnia, Premedication.

•Movement disorders, Myoclonus.

•Amnesia - useful for unpleasant procedures.

•Alcohol withdrawal.

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.

▪p450 enzyme inhibitors can increase diazepam levels - See BNF/Datasheet.

▪Caution with IM olanzapine.

Dose:

》Anxiety/Sedation : Diazepam 2 mg tds up to 30 mg per day in divided doses.

》Seizures: Diazepam 5-10 mg slow iv (Diazemuls is less irritating). Up to 20 mg may be used with skill and facilities for managing of any respiratory depression.

》Seizures : A PR Diazepam formulation can be used with doses of 2.5 mg/5 mg/10 mg/20 mg as required. Useful when IV access not available or in children.

Reference:Tara V Shanbhag

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