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PubMed1983

Flunitrazepam and nitrazepam as hypnotics in psychogeriatric inpatients.

The efficacy and clinical effects of flunitrazepam (1 mg) and nitrazepam (5 mg) as somnifacients were studied in 37 psychogeriatric inpatients. Each drug was administered in a double-blind manner to randomized groups of patients for 14 nights. Compared with placebo, both benzodiazepines proved to be effective in inducing and maintaining sleep. Although both drugs were well tolerated, insomnia resulted when each was withdrawn.

Aged↗
PubMed1981

Anesthesia with flunitrazepam and fentanyl supplemented with droperidol or chlorpromazine (Largactil) in coronary surgery.

Sixty coronary patients undergoing aortocoronary bypassgrafts, some with left ventricular resection and some with associated valvular surgery were anesthetised with flunitrazepam, pancuronium and fentanyl according to systolic blood pressure (SBP) and heart rate (HR). When 40 micrograms kg-1 fentanyl was amounted, a neuroleptic was added to the protocol either droperidol (D series, 30 cases), or chlorpromazine (L series, 30 cases), 0.005 mg kg-1 at random, if the SBP remained above 100 mm Hg or when the mean BP rose during the ECC at constant flow. Analgesia was maintained adding 0.05 mg fentanyl to each 2.5 mg neuroleptic dose. A stable cardiovascular state was achieved during the entire procedure in both series. Total doses were 53.25 +/- 10 mukg-1 (D) and 49.45 +/- 6.46 micrograms kg-1 (L) fentanyl, 0.5 +/- 0.25 microgram kg-1 droperidol and 0.38 +/0 0.032 mg kg-1 chlorpromazine. The large dispersion in the doses of neuroleptics was due to a few cases of resistance to their action during ECC. A low dose of neuroleptic (less than 0.4 mg kg-1) was sufficient in a statistically different number of patients in each series, 23 patients were given 0.25 +/- 0.1 mg kg-1 chlorpromazine and only 9 patients were given 0.23 +/- 0.11 mg kg-1 droperidol. This is thought to be due to the longer duration of action of chlorpromazine. All patients came off bypass easily. No low output state developed. During the postoperative period hypertension was not a problem when taking into account that hypertensive patients were not excluded. Thirteen patients in each series had a HR greater than or equal to 100 b.p. m. during more than 1 h, but longer after chlorpromazine (n.s.). There was no other difference in the course of the 2 series until discharge. These results prompt us to continue using droperidol because of its more satisfactory pharmacokinetic characteristics.

Anesthesia↗
PubMed1994

Modified screening procedure with fluorescence detection for flunitrazepam and its metabolites via acridine derivatives.

A modified thin-layer chromatographic method with fluorescence detection is described for the screening of flunitrazepam and its major metabolites in urine. The method is based on the hydrolysis and subsequent formation of acridine derivatives by cyclization in dimethyl-formamide. This reliable screening procedure, which has proven its usefulness in many laboratories, provides valid results in the absence of diclofenac, carbamazepine, and tricyclic antidepressants. On the other hand these latter substances are frequently detectable in urine samples taken from addicts especially during therapy. So it was necessary to modify the procedure.

Acridines↗
PubMed1993

Comparison of interactions of [3H]muscimol, t-butylbicyclophosphoro[35S]thionate, and [3H]flunitrazepam with cloned gamma-aminobutyric acidA receptors of the alpha 1 beta 2 and alpha 1 beta 2 gamma 2 subtypes.

The alpha 1 beta 2 and alpha 1 beta 2 gamma 2 subtypes, common subtypes of gamma-aminobutyric acid (GABA)A receptors in the brain, are known to share many ligands, but only the latter interacts with benzodiazepines. In this study, we attempted to examine whether the presence of the gamma 2 subunit in the cloned receptors alters the binding properties of GABA and t-butylbicyclophosphorothionate (TBPS) (a highly sensitive probe for conformational changes in the chloride ionophore of GABAA receptors) and their interactions. Using a high-level expression system of SF-9 cells infected with baculovirus, we produced a group of cloned GABAA receptors with variations in the ratio (0 to 3) of the virion carrying the cDNA for the gamma 2 subunit to those carrying the cDNAs for the alpha 1 and beta 2 subunits. The number of benzodiazepine binding sites increased as the level of the gamma 2 virion was raised and reached that of GABA high affinity sites at a gamma 2 to alpha 1 beta 2 ratio of 0.5 or more. It appears that the conversion of the alpha 1 beta 2 to the alpha 1 beta 2 gamma 2 subtype is favorable and complete in the presence of a sufficient level of the gamma 2 subunit, assuming the number of the GABA sites to be equal to the total number of the cloned GABAA receptors. In all preparations, the dissociation constants for flunitrazepam, muscimol, and TBPS were fairly constant, and the maximal number of binding sites for TBPS appeared to be equal to that for muscimol, with no dependence on the gamma 2 virion levels. The effect of GABA on TBPS binding, however, were markedly altered by the gamma 2 subunit. With the alpha 1 beta 2 subtype GABA at concentrations occupying its high affinity sites markedly stimulated but at higher concentrations (micromolar ranges) inhibited TBPS binding, whereas with the alpha 1 beta 2 gamma 2 subtype GABA inhibited TBPS binding without the early stimulatory phase. We also confirmed the selective interaction of Zn2+ (50 microM) with the alpha 1 beta 2 subtype, as probed with TBPS binding, and observed a progressive disappearance of Zn2+ sensitivity as the gamma 2 virion level increased.(ABSTRACT TRUNCATED AT 400 WORDS)

Animals↗
PubMedDate not supplied

Age-dependent modification of aspecific cellular effects of the benzodiazepine flunitrazepam.

The experiments presented here demonstrate an aspecific effect of the benzodiazepine derivative flunitrazepam (FNZ). It differs in sites and mechanisms of action, both from benzodiazepine (BZ) specific effects on gamma-aminobutyric acid (GABA) blocking transmission via central BZ receptors and from BZ effects mediated by peripheral BZ receptors. The aspecific effect of FNZ can suitably be examined on isolated and identified neurons of the mollusc Lymnaea stagnalis (pond snail). The physiological sites of action are outside the synaptic zone, on the neuron somatic membrane and affect 'intrinsic' properties of membrane, including calcium, calcium-activated potassium and chloride channels. The aspecific FNZ effect exerts an influence on the metabolism of the cell by decreasing the permeability of the calcium channel, diminishing the excitability of the neuron membrane, and hyperpolarizing the cell, thus potentiating the specific effect of FNZ. The senile alterations of the neuron function intensify the aspecific effects of FNZ to such a degree that it must be taken seriously in consideration in anesthesia of elderly patients.

Journal Article↗
PubMed1988

Synthesis and biodistribution of an 123I labelled flunitrazepam derivative: a potential in vivo tracer for benzodiazepine receptors.

A method for the synthesis of no-carrier-added of 7-[123I]iodo-1,3-dihydro-5-(2-fluorophenyl)-1-methyl-2H-1,4- benzodiazepine-2-one with a radiochemical yield of 25-30% has been developed. This benzodiazepine was prepared by reaction of [123I]iodide with the corresponding piperidyltriazene in acid medium and the reaction has been optimized for solvent, time and temperature. The triazene was synthesized by reduction of flunitrazepam to the amine, diazotisation and coupling with piperidine. Biodistribution studies of this radioligand in rats showed a maximum brain uptake of 0.35% of the injected dose at 15 min, which decline to 0.02% at 120 min.

Animals↗
PubMed2001

Flunitrazepam induces geometrical changes at the lipid-water interface.

Flunitrazepam (FNTZ) effects on molecular packing and surface curvature in artificial model membranes were investigated. FNTZ, from the subphase under dipalmitoylphosphatidylcholine (dpPC) monolayers at the air-water interface, expanded the surface pressure-area isotherm and induced an increment in the limiting area; in this conditions, the collapse pressure of dpPC decreased, indicating a lowering in the stability of the monolayer. Thermodynamic-geometric correlations based on molecular parameters predicted a decrement in the aggregation number and stability, and an increase in the curvature of the self-aggregated structure of dpPC in aqueous medium in the presence of FNTZ. Accordingly, negative-staining electron microscopy of dpPC aqueous dispersions showed that the mean diameter of dpPC vesicles decreased 2 and 2.87 times in the presence of 10 nM and 50 µM FNTZ, respectively, compared with control samples. The release of a soluble marker entrapped in dpPC liposomes increased slightly respect to the control in the presence of FNTZ. In dpPC-dpPE mixed liposomes 50 µM FNTZ induced a decrement in the amount of the aminophospholipid exposed to the outer monolayer. Concluding, an FNTZ-induced expansion of dpPC-water interface region affected the constraints imposed on the lipid-water system by the molecular geometry, interacting free energies and entropy that determine the shape of a multimolecular structure. In liposomes composed of a pure phospholipid, the bilayer expansion leaded, through a structure instability, to reduce the liposome size; in mixed liposomes, phospholipid molecules translocation could be observed as another compensating mechanism of the initial perturbation. These results may be relevant for understanding benzodiazepines' effects non-mediated by membrane receptors.

Journal Article↗
PubMed2003

Flunitrazepam used in a case of poisoning.

A male was found in a drowsy condition after being given a cup of tea and a tablet by a neighbour. An ambulance was called, he was taken to hospital and attended the police station on release. A blood sample taken 9h after the incident contained eight times the normal therapeutic level for Flunitrazepam. No motive could be proved and the neighbour was charged with Administering Poison under the Offences against the Person Act of 1861.

Journal Article↗
PubMed1989

Tricyclic heteroaromatic systems: synthesis, [3H]flunitrazepam brain membrane binding inhibition, and structure-activity relationships of 2,3-dihydro-2-aryl-4-R-[1]benzopyrano[4,3-c]pyrazole-3-ones.

We report the synthesis and binding activity to the central benzodiazepine receptors of some 2,3-dihydro-2-aryl-4-R-[1]benzopyrano[4,3-c]pyrazole-3-ones, which are isosteres of the CGS series. Although the compounds of the CGS series are potent ligands of the benzodiazepine receptors, none of the isosteres tested showed any significant inhibiting potency. This may be due to the change in electronic properties brought about by the replacement of the NH of the CGS series with an oxygen atom.

Animals↗