Flumazenil
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| Flumazenil
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| Systematic (IUPAC) name | |
| ethyl 8-fluoro-5,6-dihydro-5-methyl-6-oxo- 4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate | |
| Identifiers | |
| CAS number | |
| ATC code | V03 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C15H14FN3O3 |
| Mol. mass | 303.288 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | Hepatic |
| Half life | 7-15 min (initial) 20-30 min (brain) 40-80 min (terminal) |
| Excretion | Urine 90-95% Feces 5-10% |
| Therapeutic considerations | |
| Pregnancy cat. |
B3(AU) C |
| Legal status | |
| Routes | Intravenous |
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Flumazenil (also known as flumazepil, code name Ro 15-1788, trade names Anexate, Lanexat, Mazicon, Romazicon) is a benzodiazepine antagonist, used as an antidote in the treatment of benzodiazepine overdose. It reverses the effects of benzodiazepines by competitive inhibition at the benzodiazepine binding site on the GABAA receptor. It was introduced in 1987 by Hoffmann-La Roche under the trade name Anexate.
The onset of action is rapid and usually effects are seen within one to two minutes. The peak effect is seen at six to ten minutes. The recommended dose for adults is 200 μg every 1-2 minutes until the effect is seen, to a maximum of 3 mg per hour. It is available as a clear, colourless solution for intravenous injection, containing 500 μg in 5 mls.
All benzodiazepines (including midazolam) have longer half-lives than flumazenil. Therefore, repeat doses of flumazenil may be required to prevent recurrent symptoms of overdosage once the initial dose of flumazenil wears off. It is hepatically metabolised to inactive compounds which are excreted in the urine. Subjects who are physically dependent on benzodiazepines may suffer benzodiazepine withdrawal symptoms, including seizure, upon administration of flumazenil.
See also
References
- Romazicon product information, Roche USA
External links
- Flumazenil drug label/data at Daily Med from U.S. National Library of Medicine, National Institutes of Health.
Antidotes (V03AB) | |
|---|---|
| Methanol / Ethylene glycol | Ethanol - Fomepizole |
| Paracetamol (Acetaminophen) | Acetylcysteine - Glutathione - Methionine |
| Arsenic | Dimercaprol - Succimer |
| Cyanide | 4-Dimethylaminophenol - Amyl nitrite - Hydroxocobalamin - Sodium nitrite - Sodium thiosulfate |
| Heparin | Protamine |
| Nerve agent / Organophosphate pesticide | Atropine - Biperiden - Diazepam - Oximes (Pralidoxime, Obidoxime) - see also Cholinesterase |
| Opioid | Diprenorphine - Nalorphine - Naloxone - Naltrexone - Nalmefene |
| Benzodiazepine | Flumazenil |
| Toxic metals (Cadmium, Mercury, Lead etc) | Edetates - Dimercaprol |
| Other | Ipecacuanha - Prednisolone/promethazine - Methylthioninium chloride - Potassium permanganate - Physostigmine - Copper sulfate - Potassium iodide - Digoxin Immune Fab - Prussian blue |
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Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
