Flumazenil

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[edit] BRAND NAMES

[edit] STRUCTURE

Flumazenil.jpg

[edit] MECHANISM OF ACTION

Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system.

[edit] INDICATIONS

  • In anesthesia: termination of general anesthesia induced and maintained with benzodiazepines.
  • To diagnose and treat benzodiazepines overdosage

[edit] DOSAGE

Flumazenil is for slow intravenous injection or infusion. It should only be administered under the supervision of an experienced physician.

Flumazenil may be used concurrently with other resuscitative procedures.

Adults: The recommended initial dose is 200 micrograms administered intravenously over 15 seconds. If the desired level of consciousness is not obtained within 60 seconds a further dose of 100 micrograms can be injected and repeated at 60-second intervals where necessary, up to a maximum total dose of 1mg or in intensive care situations, 2mg. The usual dose required is 300 - 600 micrograms.

If drowsiness recurs, an intravenous infusion of 100 - 400 micrograms per hour may be employed. The rate of infusion should be individually adjusted to achieve the desired level of arousal.

The individually titrated, slow injections or infusions of Flumazenil should not produce withdrawal symptoms, even in patients exposed to high doses of benzodiazepines and/or for long periods of time. If, however, unexpected signs of overstimulation occur, an individually titrated dose of diazepam (Valium) or midazolam (Hypnovel) should be given by slow intravenous injection.

If a significant improvement in consciousness or respiratory function is not obtained after repeated doses of Flumazenil, a non-benzodiazepine aetiology must be assumed.

[edit] CONTRAINDICATIONS

  • Hypersensitivity to flumazenil, benzodiazepines or any of the excipients.
  • Flumazenil is contraindicated in patients who have been given a benzodiazepine for control of a potentially life-threatening condition (e.g. control of intracranial pressure or status epilepticus).
  • In mixed intoxications with benzodiazepines and tricyclic and/or tetracyclic antidepressants, the toxicity of the antidepressants can be masked by protective benzodiazepine effects. In the presence of autonomic (anticholinergic), neurological (motor abnormalities) or cardiovascular symptoms of severe intoxication with tricyclics/tetracyclics, Flumazenil should not be used to reverse benzodiazepine effects.

[edit] PRECAUTIONS

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

[edit] SIDE EFFECTS

Nausea, vomiting and flushing may occur, rare reports of convulsions, especially in epileptics.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES