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Flumazenil A Selective GABAA Receptor Antagonist and its Therapeutic Applications

Reference Price:USD 1-2/g

  • Product Name Flumazenil
  • CAS No. 78755-81-4
  • MF C15H14FN3O3
  • MW 303.288363
  • EINECS 616-650-9
  • Density 1.39
  • Melting point 201-203℃

Detailed Description

Flumazenil, also known as flumazepil or code name Ro 15-1788, is a selective GABAA receptor antagonist that can be administered via injection, otic insertion, or intranasally. It acts as both an antagonist and antidote to benzodiazepines, particularly in cases of overdose, through competitive inhibition. This article explores the therapeutic benefits, usage as an antidote, and potential applications of flumazenil in various medical settings.

I. Mechanism of Action:
A. Selective GABAA receptor antagonist
B. Competitive inhibition at the benzodiazepine recognition site
C. Reversal of benzodiazepine effects

II. Antidote for Benzodiazepine Overdose:
A. Importance of competitive inhibition in overdose cases
B. Benefits of flumazenil in reversing excessive sedation
C. Complications and risks associated with acute care use
D. Considerations for multiple dosing and careful monitoring

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III. Post-Surgical Application:

A. Reversal of sedative effects of benzodiazepines after surgery

B. Similarities to naloxone's use in opioid reversal

C. Anesthesiologist monitoring and post-surgical considerations


IV. Treatment of Non-Benzodiazepine Hypnotic Overdoses:

A. Effectiveness of flumazenil in treating zolpidem, zaleplon, and zopiclone overdoses


V. Potential Applications in Hypersomnia and Gastrointestinal Side Effects:

A. Reduction of excessive daytime sleepiness in primary hypersomnias

B. Alleviation of gastrointestinal side effects caused by cancer treatments

C. Protection of intestinal stem cells during chemotherapy and radiation therapy


VI. Importance of Balancing GABAA Receptor Inhibition:

A. Protecting intestinal stem cells from DNA damage during radiotherapy

B. Ensuring cancer cell killing is not compromised



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Flumazenil, a selective GABAA receptor antagonist, serves as a valuable antidote in benzodiazepine overdose cases, offering competitive inhibition and reversal of sedative effects. Its applications extend to post-surgical use, treatment of non-benzodiazepine hypnotic overdoses, and potential benefits in hypersomnia and gastrointestinal side effects. Careful monitoring and consideration of risks are essential when administering flumazenil, particularly in acute care and post-surgical settings. Further research is needed to explore its full potential in protecting intestinal stem cells during cancer treatments while maintaining cancer cell-killing efficacy.

Specification

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