CAS 78755-81-4 Pharmaceutical Raw Materials Flumazenil For Nootropic Supplement

Supériorité

Zhongshan Latterson Biotechnology Co., Ltd., est une entreprise pharmaceutique complète, qui s'est spécialisé dans la technologie biopharmaceutique 7 années. L'entreprise est située dans la ville de Zhongshan, Province de Guangdong , Chine.
Notre usine couvre une superficie de 33500 mètres carrés, avec un environnement propre et une belle mise en page. Il existe plusieurs ateliers de grande ou moyenne taille et un centre d'assurance qualité et de recherche avec un équipement de pointe. Maintenant, nos principaux produits sont des séries de stéroïdes anabolisants, Série peptidique, Série d'anesthésie locale. Nos produits atteignent le niveau avancé du marché intérieur, dont beaucoup atteignent la norme internationale, les certificats contiennent: KASCHER , ISO 9001:2008 , BPF , SGS.

La 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, contenant 500 μg in 5 mL.

Half life:

Initial distribution half-life is 4 à 11 minutes and the terminal half-life is 40 à 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 à 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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