II. Indication
- Benzodiazepine sedation reversal
III. Contraindications
- Mixed drug Overdose with compounds that may cause Seizure (e.g. Tricyclic Antidepressants, Cocaine)
- Chronic Benzodiazepine use (dependence)
- Seizure Disorder
IV. Dosing: Adults
-
Benzodiazepine Sedation Reversal
- Initial: 0.2 mg IV over 15 seconds
- Titrate: 0.2 mg each minute to 1 mg total
-
Overdose Reversal
- Initial: 0.2 mg IV over 30 seconds to 2 minutes
- Titrate: 0.3-0.5 mg every 1 to 2 minutes to 3 mg total
- Repeat dosing protocol
- Repeat Dose: 0.005 mg/kg q1-2 minutes
- Maximum cumulative dose: 1 mg
- May repeat regimen every 20 minutes
V. Dosing: Children
-
Overdose Reversal
- Start: 0.01 mg/kg slow IV push over 1 to 2 minutes (maximum 0.2 mg)
- May repeat at 1 minute intervals up to 4 doses at 0.0005 to 0.01 mg/kg
- Maximum total 0.05 mg/kg (or 1 mg)
- Ttrate to effect
VI. Precautions
- Avoid in patients with chronic use (risks of severe withdrawal including Seizures)
- Most toxicology guidelines do not recommend Flumazenil in Overdose
- Potential harms appear to outweigh benefits in most cases
- Penningo (2016) Basic Clin Pharmacol Toxicol 118(1): 37-44 +PMID:26096314 [PubMed]
- May cause acute withdrawal if physically dependent
- Do not give routinely to comatose patients
- Only use if identity of drug is known, and certain that the patient has not used chronically
- Reverses Seizure protection of Benzodiazepines
- Increases risk of drugs that lower Seizure threshold (Cocaine, Tricyclic Antidepressants)
VII. Pharmacokinetics
- Onset: 1 to 2 minutes
- Peak: 6 to 10 minutes
VIII. References
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Related Studies
Definition (NCI) | An imidazo-benzodiazepine derivative, effective in reversing benzodiazepine-induced activities. Flumazenil antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner. |
Definition (MSH) | A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses. |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | D005442 |
SnomedCT | 387575000, 96247007 |
English | Flumazenil, Flumazepil, 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, ethyl ester, 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic Acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, Ethyl Ester, flumazenil, flumazepil, flumazenil (medication), FLUMAZENIL, Flumazenil [Chemical/Ingredient], Flumazenil (product), Flumazenil (substance) |
Swedish | Flumazenil |
Czech | flumazenil |
Finnish | Flumatseniili |
Russian | FLUMAZEPIL, FLUMAZENIL, RO 15-1788, ФЛУМАЗЕНИЛ, ФЛУМАЗЕПИЛ |
Japanese | フルマゼピル, アネキセート, フルマゼニル |
Croatian | FLUMAZENIL |
Spanish | flumazenil (producto), flumacenil (producto), flumacenil, flumacenil (sustancia), flumazenil (sustancia), flumazenil, Flumazenil, Flumazepil |
Polish | Ro 15-1788, Flumazepil, Flumazenil |
French | Flumazénil |
German | Flumazenil, Flumazepil |
Italian | Flumazenile |
Portuguese | Flumazenil, Flumazepil |
Ontology: Romazicon (C0591091)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | D005442 |
English | Anexate, Romazicon, Hoffman La Roche Brand of Flumazenil, Hoffman-La Roche Brand of Flumazenil, Lanexat, Roche Brand of Flumazenil |