Talk:Flumazenil

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Summary sheet: Flumazenil
Flumazenil
Flumazenil.svg
Chemical Nomenclature
Common names Anexate, Flumazepil, Romazicon, Ro 15-1788
Substitutive name Flumazenil
Systematic name ethyl 8-fluoro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
Class Membership
Chemical class Benzodiazepine
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.











Intravenous
Dosage
Common 0.2 - 1 mg
Duration

DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.


Flumazenil (sold as Anexate, Romazicon, and known by its developmental code Ro 15-1788) is an antisedative substance of the imidazobenzodiazepine chemical class that produces antisedative effects when administered, especially when reversing benzodiazepines.

It is a highly selective benzodiazepine receptor antagonist[1] that is primarily used in the treatment of benzodiazepine overdoses via competitive inhibition at the benzodiazepine binding site on the GABAA receptor,[2] although it has also been used to treat overdoses of non-benzodiazepine hypnotics such as zolpidem and zopiclone (see Z-drug). However, it is ineffective for reversing overdoses of barbiturates, opioids, or alcohol. Due to its short half-life, multiple doses and careful patient monitoring are required to prevent recurrence of overdose symptoms.(<-- is this sentence necessary here?) [citation needed] (1. I think it should be elsewhere? 2. The cite flag isn't really too needed. Although it's definitely preferred, it's obvious that if flumazenil lasts short, some benzodiazepines last longer.)

It is also used medically to reverse the effects of benzodiazepines following surgery, in a way similar to naloxone being used for surgeries involving opioids.[citation needed] <--(Is a cite flag needed much here? That's kind of a "common sense"/inferrable thing) Outside of an acute care setting, flumanezil may also be effective in reducing excessive daytime sleepiness while improving vigilance in primary hypersomnias, such as idiopathic hypersomnia.[citation needed] (this def needs a cite flag)

Flumazenil was first introduced in 1987 by Hoffmann-La Roche under the trade name"Anexate, but only approved by the FDA on December 20, 1991. Flumazenil went off patent in 2008, so, at present, generic formulations of this drug are available.[citation needed](this def needs a cite flag)


Whether flumazenil produces any psychoactive effects on its own is currently subject to debate. Although the body produces no known benzodiazepine receptor agonists, some studies suggest that flumazenil does produce effects on its own.[3]

History and culture

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Chemistry

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Flumazenil consists of a benzodiazepine core.

Pharmacology

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Flumazenil is a benzodiazepine receptor antagonist.[4] Barbiturates, opioids, and alcohol, as they all act in different ways, will not have their actions reversed by flumazenil. Although used in benzodiazepine overdose, multiple doses or an IV infusion is often needed due to flumazenil's short duration of action. Therefore, benzodiazepine overdose care is primarily supportive in nature.

Subjective effects

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Flumazenil producing any effects in the body on its own is questionable. A study has suggested that it produces performance-declining effects that appear to be dose-dependent.[5] Flumazenil often produces effects by means of immediate withdrawal, similar to naloxone. As such, a patient may wake up agitated, extremely wakeful, or could experience seizures.


Physical effects
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Toxicity and harm potential

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We also recommend that you conduct independent research and use harm reduction practices when using this substance.

It is strongly recommended that one use harm reduction practices when using this substance.

Lethal dosage

Tolerance and addiction potential

Dangerous interactions

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Although many psychoactive substances are reasonably safe to use on their own, they can quickly become dangerous or even life-threatening when taken with other substances. The following lists some known dangerous combinations, but cannot be guaranteed to include all of them. Independent research should always be conducted to ensure that a combination of two or more substances is safe to consume. Some interactions listed have been sourced from TripSit.

Legal status

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See also

External links

Literature

References

  1. Whitwam, J. G., & Amrein, R. (1995). Pharmacology of flumazenil. Acta Anaesthesiologica Scandinavica, 39(s108), 3-14.
  2. Whyte, IM (2004). "Benzodiazepines". Medical toxicology. Philadelphia: Williams & Wilkins. pp. 811–22. ISBN 0-7817-2845-2.
  3. Neave, N., Reid, C., Scholey, A., Thompson, J., Moss, M., Ayre, G., ... & Girdler, N. (2000). Dose-dependent effects of flumazenil on cognition, mood, and cardio-respiratory physiology in healthy volunteers. British dental journal, 189(12), 668.
  4. Whitwam, J. G., & Amrein, R. (1995). Pharmacology of flumazenil. Acta Anaesthesiologica Scandinavica, 39(s108), 3-14.
  5. Neave, N., Reid, C., Scholey, A., Thompson, J., Moss, M., Ayre, G., ... & Girdler, N. (2000). Dose-dependent effects of flumazenil on cognition, mood, and cardio-respiratory physiology in healthy volunteers. British dental journal, 189(12), 668.