BACKGROUND [11C]Flumazenil and positron emission tomography (PET) are used clinically to assess gamma-aminobutyric acid (GABA)-ergic function and to localize epileptic foci prior to resective surgery. Enhanced P-glycoprotein (P-gp) activity has been reported in epilepsy and this may confound interpretation of clinical scans if [11C]flumazenil is a P-gp substrate. The purpose of this study was t...

PURPOSE In vivo the biotransformation of the imidazobenzodiazepine antagonist flumazenil leads to the formation of two metabolites, flumazenil acid and N-demethylated flumazenil. In the present study we investigated the role of carboxylesterases for the metabolism of flumazenil. METHODS We purified a non-specific carboxylesterase (EC 3.1.1.1) from human liver microsomes that catalyzes the hyd...

M a i n r e s u l t s 6 placebo-controlled studies involving 641 patients (326 assigned to flumazenil and 315 assigned to placebo) met the selection criteria. Treatment duration ranged from 5 minutes to 3 days. Combining data from 5 trials (317 patients assigned to flumazenil and 306 to placebo) showed that more patients who received flumazenil had clinical improvement than did those who receiv...

BACKGROUND Benzodiazepines have a hypnotic/sedative effect through the inhibitory action of γ-aminobutyric acid type A receptor. Flumazenil antagonizes these effects via competitive inhibition, so it has been used to reverse the effect of benzodiazepines. Recently, flumazenil has been reported to expedite recovery from propofol/remifentanil and sevoflurane/remifentanil anesthesia without benzod...

In this study we assessed the discriminative stimulus, self-reported, and performance effects of flumazenil in humans. The first group (n = 6) was trained to discriminate flumazenil (0.56 mg/70 kg i.v.) from saline and tested with flumazenil (0.10, 0.32, 0.56, and 1.0 mg/70 kg) under a two-response drug discrimination procedure. The second group (n = 8) was trained to discriminate flumazenil (0...

UNLABELLED In an effort to clarify the mechanism of action of isoflurane, we studied the effect of flumazenil on mice chronically treated with isoflurane or diazepam. Mice were pretreated with diazepam, isoflurane, or saline, with and without flumazenil. After 2 wk, responses to isoflurane and diazepam were assessed, and central benzodiazepine receptor (CBR) binding characteristics were assayed...

Flumazenil, an imidazobenzodiazepine, is the first benzodiazepine antagonist and is being used to reverse the adverse pharmacological effects of benzodiazepine. There have been a few reports on the central nevous system side effects with its use. We report a patient with generalized ballism following administration of flumazenil. The mechanism through which flumazenil induced this symptom is un...

We have compared the EEG and auditory evoked wave P300 with psychometric tests in assessing vigilance after flumazenil antagonism of midazolam sedation in 12 healthy volunteers. Measurements were made before and after midazolam 0.1 and 0.2 mg kg-1 i.v., and immediately and 30, 60, 120 and 240 min after administration of flumazenil 1 mg. The sedative effects of midazolam and antagonism by flumaz...

The purpose of the present study was to study gamma-aminobutyric acid (GABA)-A receptor function in alcohol-dependent subjects during withdrawal, using the benzodiazepine antagonist flumazenil. In particular, we wanted to examine the hypotheses that an endogenous inverse agonist ligand at the GABA-A benzodiazepine receptor (GBzR) is active during withdrawal (in which case flumazenil should be a...