Pharm 101: Flumazenil

Class

Benzodiazepine antagonist


Pharmacodynamics
  • Competitive antagonist for benzodiazepine binding site on GABA-A receptor
  • Reverses sedative effects of benzodiazepines
  • Unpredictable reversal of respiratory depression

Pharmacokinetics
  • IV administration
  • Rapid onset
  • Rapid hepatic clearance
    • Short half-life 1 hour

Clinical uses
  • Reversing CNS depressant effects of benzodiazepine overdose
  • Hasten recovering following use of drugs in anaesthetic and diagnostic procedures

Adverse effects
  • Agitation, confusion, dizziness, nausea
  • Severe precipitated abstinence syndrome in those with benzodiazepine dependence
  • Recurrence of sedation due to short half-life
    • Half-life of benzodiazepines if significantly greater
    • Repeated administration often necessary
  • Seizures and cardiac arrhythmias may occur if patient has co-ingested TCAs with benzodiazpines

Further reading

References

Pharm 101 700

Pharmacology 101

Top 200 drugs

MBBS (UWA) CCPU (RCE, Biliary, DVT, E-FAST, AAA) Emergency Medicine Advanced Trainee in Melbourne, Australia. Special interests in diagnostic and procedural ultrasound, medical education, and ECG interpretation. Editor-in-chief of the LITFL ECG Library. Twitter: @rob_buttner

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