Flumazenil
Name: Flumazenil
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Adverse Effects
>10%
Nausea and vomiting (11%)
1-10%
Dizziness (10%)
Abnormal/blurred vision (3-9%)
Agitation (3-9%)
Dyspnea (3-9%)
Hyperventilation (3-9%)
Pain at injection site (3-9%)
Xerostomia (3-9%)
Diaphoresis (1-3%)
Emotional lability (1-3%)
Fatigue (1-3%)
Headache (1-3%)
Paresthesia (1-3%)
Tremor (1-3%)
Weakness (1-3%)
<1%
Delirium
Abnormal hearing
Junctional tachycardia
Thick tongue
Tinnitus
Coldness sensation
Generalized seizure
Flumazenil Dosage
Flumazenil is injected into a vein through an IV. A healthcare provider will give you this injection.
Tell your caregivers if you feel any burning, pain, or swelling around the IV needle when flumazenil is injected.
Your breathing, blood pressure, oxygen levels, and other vital signs will be watched closely after you receive flumazenil.
You may have temporary amnesia while you are waking up from sedation. You may not remember everything going on around you for up to 2 hours.
Since this medication is given by a healthcare professional in a medical setting, an overdose is unlikely to occur.
Because you will receive flumazenil in a clinical setting, you are not likely to miss a dose.
Inform MD
Before taking flumazenil, tell your doctor about all of your medical conditions. Especially tell your doctor if you:
- are allergic to flumazenil or any of its ingredients
- are allergic to benzodiazepines
- have liver problems
- have heart problems
- have lung problems
- are taking benzodiazepines
- are taking a class of medicines called tricyclic antidepressants
- are pregnant or breastfeeding
Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.
Flumazenil Overdose
If flumazenil is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.
How is flumazenil given?
Flumazenil is injected into a vein through an IV. A healthcare provider will give you this injection.
Tell your caregivers if you feel any burning, pain, or swelling around the IV needle when flumazenil is injected.
Your breathing, blood pressure, oxygen levels, and other vital signs will be watched closely after you receive flumazenil.
You may have temporary amnesia while you are waking up from sedation. You may not remember everything going on around you for up to 2 hours.
What happens if I miss a dose?
Because you will receive flumazenil in a clinical setting, you are not likely to miss a dose.
What happens if I overdose?
Since this medication is given by a healthcare professional in a medical setting, an overdose is unlikely to occur.
What other drugs will affect flumazenil?
Receiving flumazenil after taking large doses of certain antidepressants can cause dangerous or life-threatening side effects. Tell your doctor before you receive flumazenil if you have recently taken an antidepressant such as amitriptyline, doxepin, clomipramine, desipramine, imipramine, or nortriptyline.
Other drugs may interact with flumazenil, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.
Introduction
Benzodiazepine antagonist.1
Interactions for Flumazenil
Extensively metabolized in the liver, but the precise enzymes responsible are unknown.1
Specific Drugs
Drug | Interaction | Comment |
---|---|---|
Alcohol | Pharmacokinetic interaction not observedb | |
Anesthetics, inhalational | No deleterious interactions observed when flumazenil was administered after inhalation anesthetics1 | |
Benzodiazepines | Pharmacokinetic interaction unlikely1 May precipitate dose-dependent manifestations of withdrawal in patients with established physical dependence on benzodiazepines1 | Concomitant use contraindicated1 |
Cyclic antidepressants | Increased risk of seizures1 | Concomitant use contraindicated1 |
Neuromuscular blocking agents | Do not administer until the effects of neuromuscular blockade have been fully reversed1 | |
Nonbenzodiazepine hypnotics | Flumazenil blocks the effects of nonbenzodiazepine hypnoticsb | |
Opiate agonists | No deleterious interactions observed when flumazenil was administered after opiates1 | |
Skeletal muscle relaxants | No deleterious interactions observed when flumazenil was administered after skeletal muscle relaxants1 |
Actions
-
Antagonizes 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 GABA/benzodiazepine receptor complex.1
-
Does not antagonize the CNS effects of drugs affecting GABA-ergic neurons by means other than the benzodiazepine receptor (e.g., barbiturates, alcohol, general anesthetics) and does not reverse the effects of opioids.1
Advice to Patients
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Risk of impaired memory and judgment.1
-
Risk of increased adverse effects in regular users of benzodiazepines; importance of informing clinicians of history of benzodiazepine, alcohol, and/or sedative use prior to use of flumazenil.1
-
Importance of avoiding activities that require complete alertness, and not operating hazardous machinery or a motor vehicle until at least 18–24 hours after discharge and it is certain that no residual sedative effects of the benzodiazepine remain.1
-
Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1
-
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as concomitant illnesses.1
-
Importance of informing patients of other important precautionary information.1 (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
---|---|---|---|---|
Parenteral | Injection, for IV use | 0.1 mg/mL (0.5 and 1 mg)* | Flumazenil Injection (with parabens) | Abraxis, Apotex, Baxter, Bedford, Sabex, Sicor |
Romazicon (with parabens) | Roche |
Pronunciation
(FLOO may ze nil)
Onset of Action
1-2 minutes; 80% response within 3 minutes; Peak effect: 6-10 minutes
Special Populations Hepatic Function Impairment
Moderate: Mean total clearance decreased 40% to 60%. Severe: Mean total clearance decreased 75%.
Renal Dose Adjustments
No adjustments recommended