Flumazenil

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Anexate, Flumazenil; Belgium: Anexate; Bulgaria: Anexate; Cyprus: Anexate, Flumazenil; Czech Republic: Anexate; Denmark: Flumazenil; Estonia: Flumazenil; Finland: Flumazenil, Lanexat; France: Anexate, Flumazenil; Germany: Anexate, Flumazenil; Greece: Anexate, Demoxate, Flumazenil; Hungary: Anexate, Flumazenil; Ireland: Anexate, Flumazenil; Italy: Anexate, Flumazenil; Latvia: Flumazenil; Lithuania: Flumazenil; Luxembourg: Anexate; Malta: Anexate; Netherlands: Anexate, Flumazenil; Poland: Anexate, Flumazenil; Portugal: Anexate, Flumazenilo; Romania: Anexate, Flumazenil; Slovakia: Anexate; Slovenia: Anexate; Spain: Anexate, Flumazenil, Flumazenilo; Sweden: Flumazenil, Lanexat; UK: Anexate, Flumazenil.

North America

Canada: Anexate, Flumazenil; USA: Flumazenil, Romazicon.

Latin America

Argentina: Fadaflumaz, Flumage, Flumanovag, Flumazen, Flumazenil; Brazil: Flumazen, Flumazenil, Flumazil, Lanexat; Mexico: Lanexat.

Asia

Japan: Anexate, Flumazenil.

Drug combinations

Chemistry

Flumazenil: C~15~H~14~FN~3~O~3~. Mw: 303.29. (1) 4H-Imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, ethyl ester; (2) Ethyl 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate. CAS-78755-81-4 (1987).

Pharmacologic Category

Central Nervous System Agents, Miscellaneous. Antidotes. (ATC-Code: V03AB25).

Mechanism of action

Flumazenil, a 1,4-imidazobenzodiazepine derivative, is a benzodiazepine antagonist. Competitively inhibits activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex.

Therapeutic use

Used in adults for 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 management of benzodiazepine intoxication.

Pregnancy and lactiation implications

Use during labor and delivery not recommended since effects of flumazenil on neonate are not known. Unknown whether flumazenil is distributed in milk. Caution advised if drug is administered in nursing women.

Unlabeled use

Contraindications

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. Also contraindicated in known hypersensitivity to the drug or benzodiazepines.

Warnings and precautions

Does not consistently reverse amnesia (patient may not recall verbal instructions after procedure). Resedation: Occurs more frequently where a large single dose or cumulative dose of a benzodiazepine has been administered along with a neuromuscular-blocking agent and multiple anesthetic agents. Benzodiazepine reversal may result in seizures in some patients (use with caution in patients relying on a benzodiazepine for seizure control). Use with caution in head injury, hepatic dysfunction, or panic disorder. Use caution in drug and ethanol-dependent patients. Not recommended for treatment of benzodiazepine dependence. Use with caution in mixed drug overdoses. Use not recommended in manifestations of serious cyclic antidepressant poisoning (e.g. twitching, rigidity, focal seizure, wide QRS, ventricular dysrhythmia, heart block, mydriasis, dry mucosa, hypoperistalsis, cardiovascular collapse). Possible local pain or inflammation at injection site following extravasation. Not recommended as primary treatment of patients with serious lung disease who experience serious respiratory depression secondary to benzodiazepines.

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