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[[File:Flumazenil.svg|350px|thumbnail|right|Flumazenil.]]
[[File:Flumazenil.svg|350px|thumbnail|right|Flumazenil.]]
'''Flumazenil''' (sold as '''Anexate''', '''Romazicon''', and known by its developmental code '''Ro 15-1788''') is a [[psychoactive class::antisedative]] substance of the [[chemical class::imidazobenzodiazepine]] chemical class that produces antisedative effects when [[administered]].
'''Flumazenil''' (sold as '''Anexate''', '''Romazicon''', and known by its developmental code '''Ro 15-1788''') is an [[psychoactive class::antisedative]] substance of the [[chemical class::imidazobenzodiazepine]] chemical class that produces antisedative effects when [[administered]], especially when reversing [[benzodiazepines]].


It is a highly selective benzodiazepine receptor antagonist<ref>Whitwam, J. G., & Amrein, R. (1995). Pharmacology of flumazenil. Acta Anaesthesiologica Scandinavica, 39(s108), 3-14.</ref> that is primarily used in the treatment of benzodiazepine overdoses via competitive inhibition at the benzodiazepine binding site on the GABA<sub>A</sub> receptor.{{citation needed}}<ref>Whyte, IM (2004). "Benzodiazepines". Medical toxicology. Philadelphia: Williams & Wilkins. pp. 811–22. ISBN 0-7817-2845-2.</ref> 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}}
It is a highly selective benzodiazepine receptor antagonist<ref>Whitwam, J. G., & Amrein, R. (1995). Pharmacology of flumazenil. Acta Anaesthesiologica Scandinavica, 39(s108), 3-14.</ref> that is primarily used in the treatment of benzodiazepine overdoses via competitive inhibition at the benzodiazepine binding site on the [[GABA|GABA<sub>A</sub>]] receptor,<ref>Whyte, IM (2004). "Benzodiazepines". Medical toxicology. Philadelphia: Williams & Wilkins. pp. 811–22. ISBN 0-7817-2845-2.</ref> 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 medically to reverse the effects of benzodiazepines following surgery, in a similar way naloxone is used for surgeries involving [[opioids]].{{citation needed}} 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}}
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}}
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 the body produces no known benzodiazepine receptor agonists, some studies suggest that flumazenil does produce effects.{{clarify}} <ref>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.</ref>
 
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.<ref>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.</ref>


==History and culture==
==History and culture==
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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.<ref>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.</ref> 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.
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.<ref>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.</ref> 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.





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Flumazenil.

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

This History and culture section is a stub.

As a result, it may contain incomplete or wrong information. You can help by expanding it.

Chemistry

This chemistry section is incomplete.

You can help by adding to it.

Flumazenil consists of a benzodiazepine core.

Pharmacology

This pharmacology section is incomplete.

You can help by adding to it.

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

This subjective effects section is a stub.

As such, it is still in progress and may contain incomplete or wrong information.

You can help by expanding or correcting it.

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

Toxicity and harm potential

This toxicity and harm potential section is a stub.

As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it.
Note: Always conduct independent research and use harm reduction practices if 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

This dangerous interactions section is a stub.

As such, it may contain incomplete or invalid information. You can help by expanding upon or correcting it.

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.

This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

See also

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.