Benzodiazepine Toxicity Medication

Updated: Apr 28, 2022
  • Author: J Michael Kowalski, DO; Chief Editor: Gil Z Shlamovitz, MD, FACEP  more...
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Medication Summary

Flumazenil is a selective competitive antagonist of the gamma-aminobutyric acid (GABA) receptor and is the only available specific antidote for benzodiazepine (BZD) toxicity. It will reverse the effects of BZDs but must be used with caution.


Antidotes, Other


Flumazenil is a competitive BZD receptor antagonist and is the only available specific antidote for BZDs, although its use in acute BZD is controversial and its risks usually outweighs any benefit.

Flumazenil does not consistently reverse central respiratory depression due to BZDs, and over half the patients in a large multicenter study experienced re-sedation after use.

In benzodiazepine-dependent patients, flumazenil may precipitate life-threatening withdrawal. In patients taking BZDs for a medical condition, flumenazil may result in exacerbation of the condition. 

In addition to those patients on long-term BZD use, flumazenil should not be used in any patient at an increased risk of having a seizure, including those with a seizure history, head injury, coingestion of BZD and a tricyclic antidepressant or other proconvulsant, or even a possibly ingestion of a proconvulsant.

The ideal consideration for flumazenil use is isolated iatrogenic BZD overdose in BZD-naive patients (eg, during conscious sedation on BZD-naive patient).