Pharmacology of flumazenil
@article{Whitwam1995PharmacologyOF, title={Pharmacology of flumazenil}, author={James G. Whitwam and Roman Amrein}, journal={Acta Anaesthesiologica Scandinavica}, year={1995}, volume={39} }
Flumazenil, an imidazobenzodiazpine, is the first benzodiazepine antagonist available for clinical use. It is a specific competitive antagonist at benzodiazepine receptors, which are associated with receptors for gammaaminobutyric acid, the most important inhibitory neurotransmitter in the central nervous system. Administered orally, it has a low bioavailability and the preferred route is intravenous. Its usual clinical role is to reverse the effects of benzodiazepine sedation; however…
86 Citations
A Risk-Benefit Assessment of Flumazenil in the Management of Benzodiazepine Overdose
- MedicineDrug safety
- 1997
Caution should be exercised when using this agent in patients who have co-ingested chloral hydrate or carbamazepine or whose ECG shows abnormalities typical of those seen after overdose with tricyclic antidepressants (TCAs); the use of flumazenil in the presence of these drugs can sometimes induce treatable cardiac dysrrhythmia.
Intravenous flumazenil versus oxazepam tapering in the treatment of benzodiazepine withdrawal: a randomized, placebo‐controlled study
- Medicine, PsychologyAddiction biology
- 2002
The effectiveness of FLU may reflect its capacity to upregulate BZD receptors and to reverse the uncoupling between the recognition sites of BzD and GABA, on the GABA A macromolecular complex, that has been reported in tolerant subjects.
Continuous Infusion of Flumazenil in the Management of Benzodiazepines Detoxification
- MedicineFrontiers in Psychiatry
- 2021
Elastomeric FLU infusion for BzD detoxification is a feasible administration device to maintain adequate, constant, and tolerated FLU concentrations for reducing BZD withdrawal symptoms.
Flumazenil-induced ballism.
- Psychology, BiologyJournal of Korean medical science
- 2003
It is conceivable that flumazenil may antagonize the GABA-benzodiazepine receptor complex and induce dopamine hypersensitivity, thus induce dyskinesic symptoms, and be used to reverse the adverse pharmacological effects of benzodiazepines.
A comparison of chlordiazepoxide, bretazenil, L838,417 and zolpidem in a validated mouse Vogel conflict test
- Biology, PsychologyPsychopharmacology
- 2005
The novel GABAA receptor ligand L838,417 was anxiolytic in this mouse model, and unlike the non-selective compounds, had no effect on unpunished drinking.
Pharmacoeconomic evaluation of flumazenil for routine outpatient EGD.
- MedicineGastrointestinal endoscopy
- 2000
Ascorbic acid antagonizes the sedative effect of diazepam possibly through inhibition of GABA(Aρ₁) and GABA(B1) receptors.
- BiologyCellular and molecular biology
- 2020
DZP is a GABA receptor agonist and AA may reverse DZP-mediated sedative effects in a non-competitive binding fashion in mice through inhibition of GABA(Aρ₁) and GABA(B1) receptors.
Stressful reactions and panic attacks induced by flumazenil in chronic benzodiazepine users
- Psychology, MedicineJournal of psychopharmacology
- 1998
Caution should be exercised when giving flumazenil to panic patients who are taking BZDs as maintenance treatment, as it triggered a qualitatively different reaction amounting to a panic attack during infusion in nine out of 15 patients.
Restoration Of GABAA Receptor Function After Benzodiazepine Use: A Meta-Analysis
- Psychology
- 2020
A meta-analysis compiles multiple literature sources to determine novel ways to restore GABAA receptor function so that recovering patients can maintain long-term abstinence from BZDs.
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