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Drug overview for FLUMAZENIL (flumazenil):
Generic name: FLUMAZENIL
Drug class: Benzodiazepine Antagonists
Therapeutic class: Antidotes and other Reversal Agents
Flumazenil, a 1,4-imidazobenzodiazepine derivative, is a benzodiazepine antagonist.
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
Flumazenil, a 1,4-imidazobenzodiazepine derivative, is a benzodiazepine antagonist.
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.)
DRUG IMAGES
FLUMAZENIL 0.1 MG/ML VIAL
The following indications for FLUMAZENIL (flumazenil) have been approved by the FDA:
Indications:
Benzodiazepine overdose
Reversal of benzodiazepine-induced sedation
Reversal of benzodiazepine-maintained anesthesia
Professional Synonyms:
Benzodiazepine poisoning
Benzodiazepine toxicity
Indications:
Benzodiazepine overdose
Reversal of benzodiazepine-induced sedation
Reversal of benzodiazepine-maintained anesthesia
Professional Synonyms:
Benzodiazepine poisoning
Benzodiazepine toxicity
The following dosing information is available for FLUMAZENIL (flumazenil):
Flumazenil is used in adults for the management of benzodiazepine overdosage. The drug is an adjunct to, not a replacement for, appropriate supportive and symptomatic measures (e.g., ventilatory and circulatory support) in the management of benzodiazepine overdosage. Because patients admitted to hospitals for drug overdoses may have ingested multiple substances and/or are being treated for concomitant illnesses (e.g., depression, substance abuse), the presence of contraindications or precautions, which may limit the use of flumazenil therapy, should be considered.
(See Contraindications under Warnings/Precautions, in Cautions.) Flumazenil has no known benefit other than reversal of benzodiazepine-induced sedation in seriously ill patients with multiple-drug overdosage, and the drug should not be used in cases where seizures (from any cause) are likely. In addition, the manufacturer warns that flumazenil should not be used in patients with serious cyclic depressant overdosage. (See Drug Interactions: Cyclic Antidepressants.)For information on the pathogenesis, manifestations, and treatment of benzodiazepine overdosage, see Acute Toxicity in the Benzodiazepines General Statement 28:24.08.
Efficacy of flumazenil has been established in 2 studies in patients who were presumed to have taken an overdose of a benzodiazepine, either alone or in combination with a variety of other agents. In these studies, of patients who were proven to have taken a benzodiazepine, 80% of those who received flumazenil responded with an improvement in level of consciousness. Of those who responded to flumazenil, 75% responded to a total dose of 1-3 mg.
However, reversal of sedation was associated with an increased frequency of symptoms of CNS excitation, and 1-3% of patients who received flumazenil were treated for agitation or anxiety.
When flumazenil is used for known or suspected benzodiazepine overdosage in adults, the usual initial dose is 0.2 mg given IV over 30 seconds; if the desired consciousness level is not achieved after waiting 30 seconds, an additional 0.3-mg dose may be administered over 30 seconds.
If an adequate response still is not achieved, further additional 0.5-mg doses may be administered over 30 seconds at 1-minute intervals up to a cumulative dose of 3 mg. Most patients respond to cumulative flumazenil doses of 1-3 mg, and cumulative doses exceeding 3 mg have not been shown reproducibly to provide additional benefit.
However, some patients who exhibit a partial response after a 3-mg cumulative dose rarely may require additional doses up to a total of 5 mg. If no response is observed within 5 minutes after administration of an initial 5-mg cumulative dose of flumazenil, the major cause of sedation may not be a benzodiazepine and additional flumazenil doses likely will provide little if any beneficial effect. If resedation occurs, the initial dosing regimen (i.e., up to 1 mg given in divided 0.5-mg doses at 1-minute intervals) may be repeated no more frequently than every 20 minutes up to a maximum dose of 3 mg in any 1-hour period.
(See Contraindications under Warnings/Precautions, in Cautions.) Flumazenil has no known benefit other than reversal of benzodiazepine-induced sedation in seriously ill patients with multiple-drug overdosage, and the drug should not be used in cases where seizures (from any cause) are likely. In addition, the manufacturer warns that flumazenil should not be used in patients with serious cyclic depressant overdosage. (See Drug Interactions: Cyclic Antidepressants.)For information on the pathogenesis, manifestations, and treatment of benzodiazepine overdosage, see Acute Toxicity in the Benzodiazepines General Statement 28:24.08.
Efficacy of flumazenil has been established in 2 studies in patients who were presumed to have taken an overdose of a benzodiazepine, either alone or in combination with a variety of other agents. In these studies, of patients who were proven to have taken a benzodiazepine, 80% of those who received flumazenil responded with an improvement in level of consciousness. Of those who responded to flumazenil, 75% responded to a total dose of 1-3 mg.
However, reversal of sedation was associated with an increased frequency of symptoms of CNS excitation, and 1-3% of patients who received flumazenil were treated for agitation or anxiety.
When flumazenil is used for known or suspected benzodiazepine overdosage in adults, the usual initial dose is 0.2 mg given IV over 30 seconds; if the desired consciousness level is not achieved after waiting 30 seconds, an additional 0.3-mg dose may be administered over 30 seconds.
If an adequate response still is not achieved, further additional 0.5-mg doses may be administered over 30 seconds at 1-minute intervals up to a cumulative dose of 3 mg. Most patients respond to cumulative flumazenil doses of 1-3 mg, and cumulative doses exceeding 3 mg have not been shown reproducibly to provide additional benefit.
However, some patients who exhibit a partial response after a 3-mg cumulative dose rarely may require additional doses up to a total of 5 mg. If no response is observed within 5 minutes after administration of an initial 5-mg cumulative dose of flumazenil, the major cause of sedation may not be a benzodiazepine and additional flumazenil doses likely will provide little if any beneficial effect. If resedation occurs, the initial dosing regimen (i.e., up to 1 mg given in divided 0.5-mg doses at 1-minute intervals) may be repeated no more frequently than every 20 minutes up to a maximum dose of 3 mg in any 1-hour period.
No enhanced Administration information available for this drug.
No dosing information available.
No generic dosing information available.
The following drug interaction information is available for FLUMAZENIL (flumazenil):
There are 0 contraindications.
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for FLUMAZENIL (flumazenil):
Drug contraindication overview.
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.
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.
There are 1 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Tricyclic antidepressant overdose |
There are 2 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Lower seizure threshold |
| Seizure disorder |
There are 2 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Disease of liver |
| Panic disorder |
The following adverse reaction information is available for FLUMAZENIL (flumazenil):
Adverse reaction overview.
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.)
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.)
There are 13 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Agitation Headache disorder Tonic clonic seizure |
Hypertension Mood changes Sedation Skin rash |
| Rare/Very Rare |
|---|
|
Cardiac arrhythmia Hallucinations Hearing loss Pruritus of skin Seizure disorder Urticaria |
There are 21 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Ataxia Blurred vision Dizziness Drowsy Hyperhidrosis Injection site sequelae Nausea Vertigo Visual changes Vomiting |
Paresthesia |
| Rare/Very Rare |
|---|
|
Acute cognitive impairment Drug-induced hot flash Dysphasia Fatigue Flushing General weakness Hyperacusis Malaise Panic disorder Thrombophlebitis |
The following precautions are available for FLUMAZENIL (flumazenil):
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.)
Contraindicated
Severe Precaution
Management or Monitoring Precaution
The risks associated with flumazenil use in the adult population also apply to pediatric patients. (See Cautions: Warnings/Precautions.)
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
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.
The following prioritized warning is available for FLUMAZENIL (flumazenil):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for FLUMAZENIL (flumazenil)'s list of indications:
| Benzodiazepine overdose | |
| T42.4x1A | Poisoning by benzodiazepines, accidental (unintentional), initial encounter |
| T42.4x2A | Poisoning by benzodiazepines, intentional self-harm, initial encounter |
| T42.4x3A | Poisoning by benzodiazepines, assault, initial encounter |
| T42.4x4A | Poisoning by benzodiazepines, undetermined, initial encounter |
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