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|Appearance:||White Powder||CAS Number:||78755-81-4|
|MOQ:||1g||Usage:||Pharmaceutical Raw Materials|
Local Anesthetic Agents,
Local Anesthetic Powder
Flumazenil CAS: 78755-81-4 White Raws for Treating Excessively Drowsy Patients
Flumazenil, an imidazobenzodiazepine, is a benzodiazepine antagonist which specifically blocks the
central effects of agents acting through the benzodiazepine receptor by competitive inhibition. In animal
experiments the effects of compounds showing no affinity for the benzodiazepine receptor, e.g.
barbiturates, ethanol, meprobamate, GABA mimetics, adenosine receptor agonists and other agents were
not affected by flumazenil, but those of nonbenzodiazepine agonists of benzodiazepine receptors, such
as cyclopyrrolones (e.g. zopiclone) and triazolopyridazines were blocked.
Chemical name: Flumazenil
Delivery time: 3~7 working days
|CAS No.||78755-81-4||Outer Packing||100G|
|Production date||02-07-2016||Shelf life||02-06-2018|
|Items of analysis||Specification||Results|
|Appearance||White crystalline powder||White crystalline powder|
|Identification||The sample'S IR spectrum is according with spectrum||Conforms|
|Melting point||198ºC to 202ºC||200.6ºC to 200.9ºC|
|Impurity C||NMT 0.2%||0.02%|
|Impurity A||NMT 0.10%||Not detected|
|Impurity B||NMT 0.2%||0.03%|
|Impurity D||NMT 0.10%||0.03%|
|Impurity E||NMT 0.10%||Not detected|
|Impurity F||NMT 0.10%||Not detected|
|Individual unknown impurituy||NMT 0.10%||0.02%|
|Total impurities||NMT 0.5%||0.1%|
|Loss on drying||NMT 0.5%||0.2%|
|Sulphated ash||NMT 0.1%||0.05%|
|Heavy metals||NMT 20ppm||5ppm|
|Microbial limits( for Injection)||Bacteria not more than 50CFU/g||<10 CFU/g|
|Microbial limits||Mildew and microzyme not more than 50CFU/g||<10 CFU/g|
|Microbial limits||Escherichia coli absence||Absence|
|Acetic acid||NMT4000ppm||Not detected|
|Assay (On dried substance)||98.0-102.0%|
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 opioids 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 zolpidem, zaleplon and zopiclone.
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.
Do NOT use flumazenil if:
you are allergic to any ingredient in flumazenil or to benzodiazepines (eg, alprazolam)
you have been given a benzodiazepine for control of a potentially life-threatening condition (eg, increased pressure in the head, seizures)
you are experiencing side effects due to an overdose of a medicine used to treat depression
Contact your doctor or health care provider right away if any of these apply to you.
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