Feasibility of reversing benzodiazepine tolerance with flumazenil

@article{Savic1991FeasibilityOR,
  title={Feasibility of reversing benzodiazepine tolerance with flumazenil},
  author={Ivanka Savic and Lennart Wid{\'e}n and Sharon Stone-Elander},
  journal={The Lancet},
  year={1991},
  volume={337},
  pages={133-137}
}
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86 Citations
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86 Citations

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No adequately designed long-term trials have been conducted on treatment of epilepsy using flumazenil, rendering evaluation of its use as a single-agent antiepileptic difficult.
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A pilot study of the effects of flumazenil on symptoms persisting after benzodiazepine withdrawal
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The benefits last between a few hours and several days despite flumazenil's otherwise short duration of action, however, symptoms did return to varying degrees in most cases, suggesting the need for repeated doses.
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These findings support previous human research studies indicating that flumazenil precipitates withdrawal after short chronic exposure to benzodiazepines and suggests that duration of exposure does not influence the intensity of withdrawal beyond the first week of exposure.
Benzodiazepine Receptor Antagonists
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Flumazenil represents a promising tool for pharmacological investigations of the GABAergic system and for imaging of the benzodiazepine receptor, and as a neuronal marker in epilepsy and cerebral ischaemia.
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In vivo studies on the mechanism of action of the broad spectrum anticonvulsant loreclezole
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TLDR
Concepts are presented here that could explain the modulatory function of the BZR, and a number of factors are proposed to determine the pharmacological and therapeutic profile of B zR ligands: intrinsic efficacy at the BzR, density of GABAA-BZR on neurons, functional reserve in GAB AA-BzRs, the intensity of the GABAergic input to a neuron, and the excitatory neuronal state.
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