Flumazenil

Generic Details

Generic Name

Flumazenil

Other Names

  • Anexate

Drug Class

  • Benzodiazepine Antagonist

Chemical Formula

C15H14FN3O3

Molecular Weight

303.29 g/mol

Mechanism of Action

  • Competitive antagonist at the benzodiazepine binding site on the GABA-A receptor

Indications

  • Reversal of benzodiazepine-induced sedation
  • Benzodiazepine overdose
  • Diagnostic tool in coma of unknown etiology

Common Dosage Forms

  • Injection
  • Oral tablet

Typical Dosage

  • 0.2 mg to 1 mg IV/IM
  • 0.2 mg to 1 mg orally

Pediatric Dosage

  • Safety and efficacy not established

Geriatric Dosage

  • Dose reduction may be required due to potential age-related decrease in hepatic function

Side Effects

  • Flushing
  • Nausea
  • Dizziness
  • Headache
  • Injection site reactions

Contraindications

  • Hypersensitivity to flumazenil or benzodiazepines
  • Patients with a history of seizures

Pregnancy Category

  • C - Use with caution if benefits outweigh risks

Lactation Safety

  • Limited data available, use with caution

Drug Interactions

  • May decrease the efficacy of long-acting benzodiazepines if given for dependence

Overdose Symptoms

  • Seizures
  • Hypotension
  • Cardiorespiratory depression

Antidote for Overdose

  • Supportive care and monitoring

Storage Conditions

  • Store at room temperature away from light and moisture

Pharmacokinetics

  • Absorption: Well-absorbed after oral administration
  • Distribution: Distributed widely throughout the body and crosses the blood-brain barrier
  • Metabolism: Hepatic metabolism mainly via glucuronidation
  • Excretion: Excreted primarily in the urine as metabolites

Precautions

  • Use with caution in patients with a history of seizures or benzodiazepine dependence

Warnings

  • Risk of precipitating benzodiazepine withdrawal in patients with physical dependence on benzodiazepines

Others

  • Flumazenil has a short half-life and may need repeat dosing in cases of severe overdose