Flumazenil (flumazenil)
Benzodiazepine Antagonists Intravenous Vial (ML)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Flumazenil, a 1,4-imidazobenzodiazepine derivative, is a benzodiazepine antagonist.
Flumazenil, a 1,4-imidazobenzodiazepine derivative, is a benzodiazepine antagonist. Flumazenil antagonizes the CNS effects (e.g., sedation, impaired recall, psychomotor impairment, respiratory depression) of benzodiazepines by competitively inhibiting the activity of the drugs at the benzodiazepine recognition site on the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex. Reversal of benzodiazepine-induced effects usually is evident within 1-2 minutes following completion of IV injection of flumazenil, with an 80% response occurring within 3 minutes, and the peak effect occurring at 6-10 minutes.
The duration and degree of reversal of benzodiazepine-induced effects appear to be related to the dose and plasma concentrations of flumazenil. However, because the elimination half-life of flumazenil (0.7-1.3 hours) is shorter than that of benzodiazepines, repeat doses of the drug may be needed to prevent resedation. The half-life of flumazenil appears to be shorter (averaging 40 minutes; range: 20-75 minutes) and more variable in children 1-17 years of age compared with that of adults.
Flumazenil is extensively metabolized in the liver with less than 1% of an administered dose excreted unchanged in urine. Ingestion of food during an IV infusion of the drug results in a 50% increase in clearance, most likely because of the increased hepatic blood flow that accompanies a meal.
Flumazenil is used in adults for the complete or partial reversal of benzodiazepine-induced sedation when benzodiazepines are used for induction or maintenance of general anesthesia or for diagnostic or therapeutic procedures (i.e., conscious sedation) and for the management of benzodiazepine intoxication. Flumazenil also is used in children 1-17 years of age for the reversal of benzodiazepine-induced sedation when benzodiazepines are used for diagnostic or therapeutic procedures. The manufacturer states that the safety and efficacy of flumazenil have not been established in pediatric patients for reversal of benzodiazepine-induced sedation when benzodiazepines are used for induction of general anesthesia, for the management of benzodiazepine intoxication, nor for the resuscitation of neonates. (See Special Populations: Pediatric Use.)
Generic name: flumazenil
Drug class: Benzodiazepine Antagonists
Therapeutic class: Antidotes and other Reversal Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Flumazenil
Indications
The following indications are listed for Flumazenil:
- Benzodiazepine Overdose
- Reversal Of Benzodiazepine-Induced Sedation
- Reversal Of Benzodiazepine-Maintained Anesthesia
Also known as: Benzodiazepine Poisoning, Benzodiazepine Toxicity.
Dosing
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Flumazenil is contraindicated in patients receiving a benzodiazepine for control of a potentially life-threatening condition (e.g., control of intracranial pressure or status epilepticus) and in those exhibiting manifestations of serious cyclic antidepressant overdosage. (See Warnings: Seizures.) Flumazenil also is contraindicated in patients with known hypersensitivity to the drug or benzodiazepines.
- Tricyclic antidepressant overdose
- Lower seizure threshold
- Seizure disorder
- Disease of liver
- Panic disorder
Adverse reactions
Adverse effects occurring in 3-9% of patients receiving flumazenil include dizziness, injection site pain, increased sweating, headache, and abnormal or blurred vision. In addition, serious adverse effects such as cardiac arrhythmias (e.g., junctional or ventricular tachycardias), seizures, and deaths have occurred. Most deaths occurred in patients with serious underlying disease or in patients who had ingested large amounts of non-benzodiazepine drugs (usually cyclic antidepressants) as part of an overdose. (See Warnings: Seizures in Cautions.)
More Frequent
- Agitation
- Headache disorder
- Tonic clonic seizure
Less Frequent
- Hypertension
- Mood changes
- Sedation
- Skin rash
Rare or Very Rare
- Cardiac arrhythmia
- Hallucinations
- Hearing loss
- Pruritus of skin
- Seizure disorder
- Urticaria
More Frequent
- Ataxia
- Blurred vision
- Dizziness
- Drowsy
- Hyperhidrosis
- Injection site sequelae
- Nausea
- Vertigo
- Visual changes
- Vomiting
Less Frequent
- Paresthesia
Rare or Very Rare
- Acute cognitive impairment
- Drug-induced hot flash
- Dysphasia
- Fatigue
- Flushing
- General weakness
- Hyperacusis
- Malaise
- Panic disorder
- Thrombophlebitis
Precautions
No enhanced messaging available.
Safety and efficacy of flumazenil in the reversal of conscious sedation in infants younger than 1 year of age have not been established. In addition, the manufacturer states that safety and efficacy of flumazenil, including the potential risks, benefits, and appropriate dosages, have not been established for the management of benzodiazepine overdosage, for neonatal resuscitation, nor for the reversal of sedation when benzodiazepines are used for induction of general anesthesia. However, published anecdotal reports discussing the use of flumazenil in pediatric patients for these indications have reported similar safety profiles and dosing guidelines to those described for the reversal of conscious sedation. The risks associated with flumazenil use in the adult population also apply to pediatric patients. (See Cautions: Warnings/Precautions.)
Category C. (See Users Guide.) Use during labor and delivery is not recommended since the effects of flumazenil on the neonate are not known.
It is not known whether flumazenil is distributed in milk. Caution is advised if the drug is administered in nursing women.
No substantial differences in safety or efficacy relative to younger adults, but increased sensitivity to flumazenil cannot be ruled out.
ICD codes
| Code | Type | Description |
|---|---|---|
| Benzodiazepine overdose | ||
| T42.4x1A | ICD10CM | Poisoning by benzodiazepines, accidental (unintentional), initial encounter |
| T42.4x2A | ICD10CM | Poisoning by benzodiazepines, intentional self-harm, initial encounter |
| T42.4x3A | ICD10CM | Poisoning by benzodiazepines, assault, initial encounter |
| T42.4x4A | ICD10CM | Poisoning by benzodiazepines, undetermined, initial encounter |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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