introduction: in this study the effect of matricaria recutita extract on acute pain in the presence and absence of flumazenil (antagonist of benzodiazepine) and lesioned paragigantocellularis (pgi) nucleus was investigated. method: wistar male rats (250±20 g) were used. animals were grouped randomly into intact, sham and bilateral lesion of pgi nucleus. intact and lesioned animals, each divided...

We assessed the efficacy of subcutaneous administration of flumazenil (Anexate, Roche), a specific benzodiazepine antagonist, in preventing resedation after initial reversal of midazolam sedation in 30 patients (ASA I-II) undergoing gynaecological surgery. In the post-operative period, the patients received flumazenil i.v. and placebo s.c. (group A), flumazenil i.v. and flumazenil s.c. (group B...

BACKGROUND Portal systemic encephalopathy (PSE) is a complex neuropsychiatric syndrome associated with hepatic failure. Small scale studies have shown the benzodiazepine receptor antagonist flumazenil to be effective in ameliorating PSE. AIMS To determine the efficacy of flumazenil in patients with non-comatous mild to moderate PSE (stages I to III) due to severe chronic liver disease. PATI...

BACKGROUND Flumazenil is an imidazobenzodiazepine that promptly reverses via competitive inhibition the hypnotic/sedative effects of benzodiazepines on gamma-aminobutyric acid receptors. Endogenous benzodiazepine ligands (endozepines) were isolated in urine, cerebrospinal fluid, and breast milk of women who had not received benzodiazepines. The bispectral index (BIS), an electroencephalographic...

Forty adult patients undergoing elective surgery, anaesthetized with diazepam, alfentanil and nitrous oxide in oxygen, and paralysed with atracurium were given flumazenil or placebo i.v. in a double-blind randomized study to assess the efficacy of flumazenil. Awake state, heart rate, arterial pressure, rate of ventilation and arterial blood-gas values were measured at 0, 5, 30, 120 and 240 min ...

We have studied the effect of i.v. flumazenil 0.01 mg kg-1 on the amnesia and sedation caused by midazolam 2 mg and 5 mg i.v. in volunteers in order to determine the relationship between the actions of the antagonist on these two effects. Midazolam caused dose-dependent central neural depression as assessed by critical flicker fusion frequency, and dose-dependent amnesia for word cards. In subj...

The objective of this study was to examine the role of oxygen radicals, protein kinase C (PKC), and ATP-sensitive K(+) (K(ATP)) channels in mediating flumazenil-produced preconditioning. Chick cardiomyocyte death was quantified using propidium iodide, and oxygen radical generation was assessed using 2',7'-dichlorofluorescin oxidation. Preconditioning was initiated with 10 min of ischemia follow...

Adverse effects of benzodiazepines limit their clinical use; these effects might be reduced without altering therapeutic effects by administering other positive GABA(A) modulators (i.e., neuroactive steroids) with benzodiazepines. One concern with this strategy involves reversing these combined effects in case of overdose. The current study examined whether flumazenil can attenuate the combined...

Neuronal loss in Alzheimer's disease, a better correlate of cognitive impairment than amyloid deposition, is currently gauged by the degree of regional atrophy. However, functional markers, such as GABA(A) receptor density, a marker of neuronal integrity, could be more sensitive. In post-mortem hippocampus, GABA(A) messenger RNA expression is reduced even in mild cognitive impairment. We measur...

[(11)C]Flumazenil, a highly selective benzodiazepine antagonist is the most extensively used GABA(A) ligand for PET so far. To overcome half life disadvantages of (11)C a [(18)F]-labeled flumazenil derivative, 2'-[(18)F]fluoroflumazenil (FFMZ) was developed and biologically evaluated with respect to the GABA(A) receptor. Organ with the highest uptake was the pituitary gland. Brain uptake was hi...