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flumazenil (Romazicon, Mazicon)

Tradenames: Mazicon, Romazicon. Indications: 1) benzodiazepine sedation reversal: a) 0.2 mg IV over 15 sec, then 0.2 mg every 1 min PRN b) up to 1 mg. 2) benzodiazepine overdose reversal: a) 0.2 mg IV over 30 sec, then 0.3-0.5 mg every 30 sec PRN b) up to 3 mg. * Note: 1/2 life 40-80 minutes is considerably less than that of most benzodiazepines Contraindications: 1) patients with serious signs of tricyclic antidepressant overdose 2) patients given benzodiazepines for control of potentially life-threatening conditions a) status epilepticus b) control of intracranial pressure Pharmacokinetics: 1) rapidly inactivated by the liver by hydroxylation 2) 1/2life is 1 hour 3) reversal of benzodiazepine may take effect in 1-3 minutes & last 1-5 hours Adverse effects: 1) common (> 10%) - nausea/vomiting - dizziness 2) less common (1-10%) - headache, pain at injection site, increased sweating, asthenia, malaise, hot flashes, anxiety, nervousness, dry mouth, tremor, insomnia, dyspnea, hyperventilation, abnormal crying, euphoria, depression, vision disorders 3) uncommon (< 1%) - shivering, hearing disorder, bradycardia, tachycardia, chest pain, hypertension, variations in blood pressure, hiccups, somnolence, thick tongue, ventricular asystoles, anxiety, sensation of coldness, generalized convulsions*, withdrawal syndrome 4) other [4] - may precipitate seizures* - resedation may occur * Be prepared to manage seizures prior to administration. Drug interactions: - toxic effects of tricyclic antidepressant overdose may emerge with reversal of benzodiazepine effect Mechanism of action: - competitively antagonizes the effects of benzodiazepines on GABA-mediated inhibitory pathways in the CNS

Related

benzodiazepine tricyclic antidepressant (TCA)

General

antidote

Properties

INHIBITS: benzodiazepine MISC-INFO: elimination route LIVER KIDNEY 1/2life 40-80 MINUTES pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM cid=3373

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Seger DL. Flumazenil--treatment or toxin. J Toxicol Clin Toxicol 2004; 42:209 PMID: 15214628
  5. An H, Godwin J. Flumazenil in benzodiazepine overdose. CMAJ. 2016 Dec 6;188(17-18):E537. PMID: 27920113 Free PMC Article
  6. Department of Veterans Affairs, VA National Formulary