What is the mechanism of action of flumazenil?
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What is the mechanism of action of flumazenil?
Mechanism of Action Flumazenil is a benzodiazepine antagonist. It competitively inhibits the activity of benzodiazepine and non-benzodiazepine substances that interact with benzodiazepine receptors site on the GABA/benzodiazepine receptor complex.
Is flumazenil an inverse agonist?
Competitive antagonist and inverse agonist of the benzodiazepine receptor. Moderate lipid solubility, 50% protein bound. t1/2β < 1 hour – may require infusion.
Does flumazenil reverse propofol?
Conclusion: The effects of a multi-drug protocol consisting of midazolam, meperidine, and propofol can be significantly reversed by the administration flumazenil & naloxone.
What is the half life of flumazenil?
Flumazenil is extensively distributed in the extravascular space with an initial distribution half-life of 4 to 11 minutes and a terminal half-life of 40 to 80 minutes. Peak concentrations of flumazenil are proportional to dose, with an apparent initial volume of distribution of 0.5 L/kg.
When should you not take flumazenil?
Flumazenil should not be used routinely Flumazenil is contraindicated in patients with unknown or mixed overdose, benzodiazepine tolerance, seizure disorders or a prolonged QRS interval.
What drugs can be reversed by flumazenil?
Romazicon (Flumazenil) is a benzodiazepine antogonist used to reverse Versed (Midazolam) and Valium (Diazepam). It also has a rapid onset of action, producing a reversal in less than one minute. A dose of 0.2 – 1 mg is given slowly intravenously with a dose not exceeding 0.2 mg/min.
How is flumazenil metabolized?
Flumazenil is completely (99%) metabolized. Elimination of radiolabeled drug is essentially complete within 72 hours, with 90% to 95% of the radioactivity appearing in urine and 5% to 10% in the feces. Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes.
What is the half-life of flumazenil?
Does flumazenil need to be diluted?
When flumazenil is to be used in infusion, it must be diluted prior to infusion.
What are the risks for using flumazenil?
Adverse Events In Clinical Studies Adverse events most frequently associated with flumazenil alone were limited to dizziness, injection site pain, increased sweating, headache, and abnormal or blurred vision (3% to 9%).
Is flumazenil the same as naloxone?
Naloxone rapidly reverses sedation and respiratory depression due to previously administered narcotics, whereas flumazenil overturns the effects of mid- azolam on the central nervous system. Both agents are ad- ministered intravenously in repeated doses according to the patient’s response.
Why Propofol is white in Colour?
Newer generic formulations contain sodium metabisulfite or benzyl alcohol as antimicrobial agents. Propofol emulsion is a highly opaque white fluid due to the scattering of light from the tiny (about 150-nm) oil droplets it contains: Tyndall Effect.
How do you give flumazenil IV push?
The recommended starting dose is 200 micrograms administered intravenously over 15 seconds. If the required level of consciousness is not obtained within 60 seconds, a further dose of 100 micrograms can be injected and repeated at 60-second intervals, up to a maximum dose of 1000 micrograms.
