99% Purity Pharmaceutical Raw Material White Powder Antidote Flumazenil CAS 78755-81-4 For Nootropic Supplement

Product Name: Flumazenil

Product Details: 

Description:

Flumazenil (also known as flumazepil, code name Ro 15-1788) is a selective receptor antagonist primarily available by injection only, and the only GABAA negative allosteric modulator on the market today. It has antagonistic and antidote properties , through competitive inhibition. It 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. Intravenous flumazenil is primarily used to treat overdoses and to help reverse anesthesia. Administration of flumazenil by sublingual lozenge and topical cream has also been tested.

Fumazenil is an imidazobenzodiazepine derivative and a potent benzodiazepine receptor antagonist that competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benzodiazepine on the central nervous system. Reversing drowsiness, sedation, and other effects caused by benzodiazepine Flumazenil is a benzodiazepine antagonist. It works by blocking receptors in the brain and central nervous system that benzodiazepine need to reach to be active, which helps reduce drowsiness and sedation.

Applications:

Flumazenil is of benefit in patients who become excessively drowsy after benzodiazepines are used for either diagnostic or therapeutic procedures. It has been used as an antidote in the treatment of benzodiazepine overdoses.It reverses the effects of benzodiazepines by competitive inhibition at the benzodiazepine binding site on the GABAA receptor. There are many complications that must be taken into consideration when used in the acute care setting.These include lowered seizure threshold, agitation, and anxiousness. Flumazenil's short half-life requires multiple doses and careful patient monitoring to prevent recurrence of overdose symptoms.

It is also sometimes used to reverse the effects of benzodiazepines after surgery in a manner similar to naloxone's application to reverse the effect of opiates and opioid following surgery. This requires careful monitoring by an anesthesiologist due to potential side effects and serious risks associated with both over-administering flumazenil and the removal of patient life-support and monitoring equipment before the benzodiazepines have worn off (due to flumazenil masking their continued effect).

Flumazenil has been effectively used to treat overdoses of non-benzodiazepine hypnotics, such as zol-pidem,. It may also be effective in reducing excessive daytime sleepiness while improving vigilance in primary hypersomnias, such as idiopathic hypersomnia. It has also been used in hepatic encephalopathy, though results have been mixed. The onset of action is rapid and usually effects are seen within one to two minutes. The peak effect is seen at six to ten minutes. The recommended dose for adults is 200 μg every 1-2 minutes until the effect is seen, to a maximum of 3 mg per hour. It is available as a clear, colourless solution for intravenous injection, containing 500 μg in 5 mL.

Half life:

Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes. Prolongation of the half-life to 1.3 hours in patients with moderate hepatic impairment and 2.4 hours in severely impaired patients. Compared to adults, the elimination half-life in pediatric patients was more variable, averaging 40 minutes (range: 20 to 75 minutes).

Benefits and Effects:

Flumazenil is of benefit in patients who become excessively drowsy after benzodiazepine are used for either diagnostic or therapeutic procedures. It has been used as an antidote in the treatment of benzodiazepine overdoses. There are many complications that must be taken into consideration when used in the acute care setting.These include lowered seizure threshold, agitation, and anxiousness. Flumazenil's short half-life requires multiple doses and careful patient monitoring to prevent recurrence of overdose symptoms. Flumazenil has been effectively used to treat overdoses of non-benzodiazepine hypnotics, such as zolpidem, zaleplon and zopiclone.

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