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Benzodiazepine antagonistAka: Flumazenil, Romazicon

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  1. Indication
    1. Benzodiazepine Sedation reversal
  2. Contraindications
    1. Mixed drug overdose
    2. Chronic Benzodiazepine use
  3. Dosing
    1. Benzodiazepine Sedation Reversal
      1. Initial: 0.2 mg IV over 15 seconds
      2. Titrate: 0.2 mg each minute to 1 mg total
    2. Overdose Reversal
      1. Initial: 0.2 mg IV over 30 seconds
      2. Titrate: 0.3-0.5 mg q30 seconds to 3 mg total
    3. Repeat dosing protocol
      1. Repeat Dose: 0.005 mg/kg q1-2 minutes
      2. Maximum cumulative dose: 1 mg
      3. May repeat regimen every 20 minutes
  4. Precautions
    1. May cause acute withdrawal if physically dependence
    2. Do not give routinely to comatose patients
      1. Only use if identity of drug is known
    3. Reverses Seizure protection of Benzodiazepines
      1. Increases risk of drugs that lower Seizure threshold
        1. Cocaine
        2. Tricyclic Antidepressants
  5. Pharmacokinetics
    1. Onset: 1 to 2 minutes
    2. Peak: 6 to 10 minutes

Flumazenil (C0016293)

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.
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.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD005442
EnglishFlumazenil, FLUMAZENIL PREPARATION, Flumazepil
Spanishflumacenil, flumazenil
Parent ConceptsBenzodiazepinones (C0005065), Neuroprotective Agents (C0242912), [AD900] ANTIDOTES/DETERRENTS, OTHER (C0973464), Benzodiazepine antagonist (C0360298)
SourcesAOD, CSP, MSH, MTHSPL, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Romazicon (C0591091)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD005442
EnglishAnexate, Hoffman La Roche Brand of Flumazenil, Hoffman-La Roche Brand of Flumazenil, Lanexat, Roche Brand of Flumazenil, Romazicon
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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