FLUMAZENIL (Anexate)

 

Name: FLUMAZENIL (AnexateR)
Classification:

Benzodiazepine antagonist

  • Used in reversal of benzodiazepine induced CNS depression (will not necessarily reverse sedation or respiratory depression)
  • Used in diagnosis and/or management of benzodiazepine overdose
Dose:

Maximum cumulative dose is 3 mg. Patients with a partial response at 3 mg may require additional titration up to 5 mg. If no response 5 minutes after cumulative dose of 5 mg, the sedation is not likely due to benzodiazapines.

  • Benzodiazepine associated anaesthesia/sedation:
    • 0.2 mg IV direct over 15 seconds
    • further incremental doses of 0.1 mg IV direct every 60 seconds to a maximum total dose of 1 mg
  • Benzodiazepine overdose:
    • 0.3 mg IV direct over 30 seconds
    • further incremental doses of 0.3 mg IV direct over 30 seconds repeated every 60 seconds to a cumulative dose of 3 mg
  • IV Infusion
    • 0.2 - 0.4 mg/hr, titrate to individual response. Indicated for rebound drowsiness.
Administration: IV Infusion
1 mg/100 mL dextrose 5% or sodium chloride 0.9% (0.01 mg/mL)
Contraindications:
  • Contraindicated with raised ICP, seizures or tricyclic antidepression overdose
  • Should be used with caution in epileptic patients 
  • Should be used with caution in mixed overdoses where there has been co-ingestion of agents that decrease the seizure threshold (e.g. tricyclic antidepressants, phenothiazines) 
  • Should be used with caution with a history of cardiac arrhythmias
  • In liver failure, first dose is the same as non-liver failure but subsequent doses should be reduced
Adverse Effects: Due to abrupt benzodiazepine withdrawal:
  • Seizures 
  • Cardiac arrhythmias including bradycardia or ventricular asystole
  • Hypotension or hypertension
  • Nausea, vomiting
  • Agitation, discomfort, tearfulness, anxiety, emotional lability
  • Dry mouth
  • Blurred visions
  • Injection site pain
  • Hot flashes
  • Hiccoughs
  • Sensation of cold
Monitoring Therapy:
  • IV site
  • Neurological status
  • Signs of seizures
  • Heart rate
  • Blood pressure
  • Respiratory status
NOTE: duration of benzodiazepines will exceed that of flumazenil; observe closely for recurrence of sedation or respiratory depression
Adult Critical Care Protocol:
  • May be administered IV direct or by IV infusion by a nurse in Adult Critical Care.


Lynne Kelly, Pharmacist, CCTC
Brenda Morgan, Clinical Nurse Specialist, CCTC
Last Update: September 19, 2018; Reviewed: February 13, 2023