flumazenil: clinical use

Prescribing considerations

• Confirm that benzodiazepine effects are the likely cause; lack of improvement should prompt consideration of another cause.
• Assess long-term or high-intensity benzodiazepine exposure, epilepsy, panic disorder, substance dependence, hepatic impairment, head injury and possible mixed ingestion.
• Avoid rapid reversal where abrupt awakening, withdrawal or loss of anticonvulsant protection may be hazardous.
• Ensure peripheral neuromuscular blockade has been fully reversed before use at the end of anaesthesia.
• Paediatric licensing is limited to reversal of conscious benzodiazepine sedation in children older than one year.

Contraindications and cautions

• Hypersensitivity to flumazenil or any excipient.
• Benzodiazepine treatment used to control a potentially life-threatening condition, such as status epilepticus or raised intracranial pressure.

Monitoring

• Monitor alertness, respiratory status, oxygen saturation, pulse, blood pressure and ECG as clinically appropriate.
• Observe for recurrent sedation, respiratory depression and residual benzodiazepine effects.
• Consider longer observation in hepatic impairment because elimination may be delayed.
• Be prepared to manage seizures, withdrawal, dysrhythmia and serious hypersensitivity.

Clinical pharmacology

Flumazenil is an imidazobenzodiazepine that competitively antagonises the benzodiazepine receptor. It acts rapidly after intravenous administration, is mainly metabolised in the liver to an inactive metabolite and has a shorter elimination half-life than many benzodiazepines.

Formulation and product differences

• The selected product is a clear, colourless solution for intravenous injection or infusion in single-use glass ampoules.
• For infusion, use only compatible solutions specified in the product information; compatibility with other injection solutions is not established.
• Use opened ampoules immediately and discard unused solution.

Injection

Route: Parenteral

Strengths: 100 micrograms/mL