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PubMed1980

Total intravenous anaesthesia: a technique using flunitrazepam, ketamine, muscle relaxants and controlled ventilation of the lung.

A potentially acceptable and uncomplicated technique of total intravenous anaesthesia is described using flunitrazepam for induction, and maintenance by ketamine infusion with neuromuscular blockade and controlled ventilation using oxygen-enriched room air. A significant complication was the 23% incidence of nausea and/or vomiting encountered in the fifty-six patients studied. Definite factual recall of the surgical experience was reported by one patient. This was attributable to an accidental error in technique. Postoperative drowsiness was also a feature of the technique. The usual cardiovascular and psychomimetic effects associated with ketamine administration appeared markedly attenuated by flunitrazepam induction. Fifty-three (96.3%) patients expressed their willingness to receive the same anaesthetic again. Further experience of total intravenous anaesthesia with the introduction of cerebral function monitoring, allowing correlation of depth of anaesthesia with drug dosage, should allow further refinement of the technique to ensure successful and acceptable anaesthesia.

Adult↗
PubMed1975

Residual effects of flunitrazepam.

1 Twelve normal subjects were tested on a large battery of tests after a hypnotic dose of flunitrazepam(1 or 2 mg) and a placebo. Psychological tests were given 12 h after the drug and physiological tests 12, 15 and 18 h after the drug. 2 The tests included self-ratings of hypnotic effects and mood, the electroencephalogram, the auditory electroencephalographic evoked response, skin conductance, tapping, card-sorting and the symbol copying test. 3 Both doses of flunitrazepam were effective hypnotics according to the ratings, with an anxiolytic effect the following day. The EEG was significantly altered up to 18 h after the drug and the behavioural tests showed a motor impairment 12 h after drug administration. 4 Nearly all changes displayed linear dose-related trends.

Adult↗
PubMed1977

A repeated dose comparison of dichloralphenazone, flunitrazepam and amylobarbitone sodium on some aspects of sleep and early morning behaviour in normal subjects.

1 Seven normal subjects were given three different hypnotics (flunitrazepam 1 mg, amylobarbitone sodium 100 mg and dichloralphenazone 1300 mg) for four consecutive nights each. 2 All three substances improved subjective assessment of the ease of getting to sleep. Flunitrazepam was rated as better than eithr dichloralphenazone or amylobarbitone sodium in this respect. 3 The perceived quality of induced sleep was not altered by any of the preparations. 4 There was a disturbance of the subjective ratings of getting to sleep following cessation of treatment with dichloralphenazone, giving tentative support to the existence of a 'rebound' effect. 5 Dichloralphenazone produced an impairment in psychomotor performance as measured on a complex reaction time test following four nights medication with the drug.

Adolescent↗
PubMed1983

Effect of the benzodiazepine antagonist Ro 15-1788 on flunitrazepam-induced sleep changes.

1 The modifications of human sleep induced by benzodiazepines, and particularly by flunitrazepam, are complex. Stage 4 and paradoxical sleep are both decreased; however, these two effects have a different evolution during and after single or short-term drug administration. 2 The benzodiazepine antagonist Ro 15-1788 also tends to depress stage 4, but with immediate recovery in the post-drug night, and does not modify paradoxical sleep. 3 In combined administration, this drug totally reverses the hypnogenic effect of flunitrazepam, as well as its effect on paradoxical sleep but not the decrease of slow wave sleep. 4 Some of the benzodiazepine-induced alterations of sleep may be related to receptors different from central benzodiazepine receptors, or to mechanisms not directly connected to this type of receptors.

Adult↗
PubMed1987

Benzodiazepines as oral premedication. A comparison between oxazepam, flunitrazepam and placebo.

Oxazepam 25 mg, flunitrazepam 1 mg and placebo were compared as oral premedication in 602 gynecological patients in a double-blind randomised parallel study. In 251 patients undergoing major surgery the same drug was also given as a hypnotic the night before the operation. Both active drugs shortened the sleep-onset time, decreased the number of spontaneous awakenings at night and improved the quality of sleep when compared to placebo. The active drugs were significantly better than placebo as premedication when assessed by both the patients and the anesthesiologist. In 351 patients admitted for day-case minor surgery with no previous night medication, flunitrazepam was significantly better than placebo as premedication when assessed by both the patients and the anesthesiologist, while oxazepam was only better than placebo when judged by the anesthesiologist, not by the patients.

Administration, Oral↗
PubMed1983

Thyroid hormones and derivatives inhibit flunitrazepam binding.

Thyroid hormones and their derivatives were found to inhibit [3H]flunitrazepam binding stereospecifically and in a monophasic manner. Among the compounds tested, D-thyroxine was the most potent inhibitor (IC50 = 0.5 microM). The naturally occurring L-thyroxine was about 40-fold less potent (IC50 = 20 microM). The structure-activity relationships seem to imply that the thyronine base has the principal role in the inhibition of benzodiazepine receptor binding. The type of inhibition was examined with the most potent inhibitor, D-thyroxine, by Scatchard analysis. The apparent dissociation constant (KD) of the [3H]flunitrazepam binding increased and the receptor density (Bmax) decreased as a function of D-thyroxine concentration; this is characteristic of mixed-type inhibition.

Animals↗
PubMed1988

Increased binding of [3H]muscimol and [3H]flunitrazepam in the rat brain under hypoxia.

We examined the effects of in vivo hypoxia (10% O2/90% N2) on the gamma-aminobutyric acid (GABA)/benzodiazepine receptors and on glutamic acid decarboxylase (GAD) activity in the rat brain. Male Wistar rats were exposed to a mixture of 10% O2 and 90% N2 in a chamber for various periods (3, 6, 12, and 24 h). The control rats were exposed to room air. The brain regions examined were the cerebral cortex, striatum, hippocampus, and cerebellum. GABA and benzodiazepine receptors were assessed using [3H]muscimol and [3H]flunitrazepam, respectively. Compared with control values, GAD activity was decreased significantly following a 6-h exposure to hypoxia in all four regions studied. On the other hand, the numbers of both [3H]muscimol and [3H]flunitrazepam binding sites were increased significantly. The increase in receptor number tended to return to control values after 24 h. Treatment of the membrane preparations with 0.05% Triton X-100 eliminated the increase in the binding capacity. These results may represent an up-regulation of postsynaptically located GABA/benzodiazepine receptors corresponding to the impaired presynaptic activity under hypoxia.

Animals↗
PubMed1992

Effect of chronic ethanol treatment on the gamma-aminobutyric acid-mediated enhancement of [3H]flunitrazepam binding in rat cortex and hippocampus.

The mechanism by which ethanol affects the gamma-aminobutyric acid (GABA)/benzodiazepine complex is not clear. It is known that ethanol enhances the Cl- influx mediated by the GABAA receptor complex, and although chronic ethanol administration does not change the KD or Bmax for [3H]flunitrazepam binding, some reports have suggested that it could modify the modulation of benzodiazepine binding produced by GABA. In the present work, we studied the effect of chronic ethanol treatment on the modulation by GABA of [3H]flunitrazepam binding, using light microscopic autoradiography. This technique allows the measurement of densities of benzodiazepine receptors in different brain areas, the visual cortex and hippocampus, which appear to constitute the anatomical support for the behavioral and physiological responses affected by ethanol. We found enhancement of benzodiazepine binding by GABA at concentrations of greater than 10(-6) M for the various cortical and hippocampal areas studied from both control and ethanol-treated animals; this enhancement peaked at 10(-4) M GABA but decreased at 10(-3) M GABA. We found a clear effect of ethanol treatment on the modulatory properties of GABAA receptor, in both cortex and hippocampus, although only in cortex were the differences statistically significant between control and ethanol-treated animals.

Animals↗
PubMed1983

Correlations among minimal neurotoxicity, anticonvulsant activity, and displacing potencies in [3H]flunitrazepam binding of benzodiazepines.

Five clinically available 1,4-benzodiazepines (BDZs) (chlordiazepoxide, diazepam, oxazepam, nitrazepam, and clonazepam) and four investigational 1,4-BDZs (BDZ I, BDZ II, BDZ III, and BDZ IV) were tested in vivo for minimal neurotoxicity (TD50) and for ability to obtund seizures (ED50) induced by a battery of five well-standardized procedures (maximal electroshock, strychnine, pentylenetetrazol, bicuculline, and picrotoxin). In addition, these BDZs were also tested in vitro as inhibitors of [3H]flunitrazepam binding to BDZ receptors. The results with each of the six in vivo tests were compared with those with the in vitro receptor binding test, and the correlation coefficients (r) were calculated. There was a high correlation between the inhibitor constants (Ki) derived from BDZ binding studies and the TD50 values (r = 0.882) and the pentylenetetrazol ED50 values (r = 0.946). There was also good correlation between ED50 values of BDZs effective by the bicuculline and picrotoxin tests and their Ki values in the BDZ receptor binding studies (r = 0.868 and 0.892, respectively). However, BDZ I, BDZ II, and BDZ IV had Ki values of 1.830, 0.075, and 0.015 microM, respectively, but BDZ I was ineffective in nontoxic doses by the bicuculline and picrotoxin tests, BDZ II by the picrotoxin test, and BDZ IV by the bicuculline test. In contrast, there was no correlation between the BDZs' anticonvulsant potency, determined by either the maximal electroshock or strychnine test, and their inhibitory potency on [3H]flunitrazepam binding to receptor sites. The possible methodological and neurochemical bases for these differences are discussed. These studies indicate that BDZ binding studies can be used to screen BDZs for anticonvulsant activity (selectively for antipentylenetetrazol activity and less selectively for antibicuculline and antipicrotoxin activity). More importantly, they complement the conventional in vivo anticonvulsant threshold tests. Therefore, BDZ binding studies can be used in concert with conventional in vivo procedures for the pharmacological differentiation of candidate antiepileptic BDZs.

Animals↗
PubMed1997

Ethanol, flunitrazepam, and pentobarbital modulation of GABAA receptors expressed in mammalian cells and Xenopus oocytes.

GABAA receptors composed of human alpha 1 beta 2 gamma 2L, alpha 1 beta 2 gamma 2S, alpha 1 beta 3 gamma 2S, alpha 6 beta 3 gamma 2S, and alpha 5 beta 3 gamma 3 subunits as well as bovine alpha 1 beta 1 gamma 2L and alpha 1 beta 1 subunits were stably expressed in mammalian L(tk-) cells and transiently expressed in Xenopus oocytes. Effects of muscimol, ethanol, flunitrazepam, and pentobarbital on receptor function were compared for the two expression systems using a 36Cl- flux assay for cells and an electrophysiological assay for oocytes. Muscimol activated all receptors in both expression systems but was more potent for L(tk-) cells than oocytes; this difference ranged from 2.6-to 26-fold, depending upon subunit composition. The most pronounced differences between receptors and expression systems were found for ethanol. In L(tk-) cells, low (5-50 mM) concentrations of ethanol potentiated muscimol responses only with receptors containing the gamma 2L subunit. In oocytes, concentrations of 30-100 mM produced small enhancements for most subunit combinations. Flunitrazepam enhanced muscimol responses for all receptors except alpha 6 beta 3 gamma 2S and alpha 1 beta 1, and this enhancement was similar for both expression systems. Pentobarbital also enhanced muscimol responses for all receptors, and this enhancement was similar for L(tk-) cells and oocytes, except for alpha 6 beta 3 gamma 2S where the pentobarbital enhancement was much greater in oocytes than cells. The alpha 6 beta 3 gamma 2S receptors were also distinct in that pentobarbital produced direct activation of chloride channels in both expression systems. Thus, the type of expression/assay system markedly affects the actions of ethanol on GABAA receptors and also influences the actions of muscimol and pentobarbital on this receptor. Differences between these expression systems may reflect posttranslational modifications of receptor subunits.

Animals↗
PubMed1986

Saccadic eye movements in determination of the residual effects of flunitrazepam.

Saccadic eye movements and the subjective assessments of the volunteers were used in the determination of the residual effects of a single evening dose of flunitrazepam 0.5 mg, 1 mg and 2 mg or placebo. Sleep inducing and maintaining effects were subjectively assessed, too. Flunitrazepam at all three dose levels possessed sleep inducing and increasing effects (n = 9), but in the number of nocturnal awakenings and sedation in the morning (10 hrs after drug intake), no significant differences between placebo and the active medications were reported. However, saccadic eye movement recording could differentiate the residual effects produced by placebo or the active medication. No correlation was detected between the serum levels (radioreceptor assay) and saccadic eye movement recordings.

Adult↗
PubMed1977

Sequelae after the intravenous injection of three benzodiazepines--diazepam, lorazepam, and flunitrazepam.

The occurrence of thrombosis and phlebitis after intravenous injection of 10 mg diazepam, 4 mg lorazepam, or 1-2 mg flunitrazepam was studied on the second or third and the seventh to 10th days. A significantly higher incidence occurred with all drugs on days 7 to 10 than on days 2 and 3. Painless thrombosis occurred much more often with diazepam than with the other two benzodiazepines. Its incidence was greater in small hand or arm veins than in large antecubital vessels. Lorazepam and flunitrazepam therefore have clear advantages over diazepam.

Anti-Anxiety Agents↗
PubMed1976

Benzodiazepine-induced modifications of dream content: the effect of flunitrazepam.

The purpose of this study was to investigate the effect of flunitrazepam, a benzodiazepine with strong hypnotic properties, on dream content. Eight normal subjects were studied in laboratory by the awakening technique, and the dream contents were rated by two judges according to nine scaled dimensions: unreality, participation of the dreamer, pleasantness, unpleasantness, verbal aggresivity, physical aggressivity, sexuality, sensoriality and time of reference in the dreamer's life. By comparison with placebo condition, flunitrazepam induced more unpleasantness, more verbal aggressivity, more physical aggressivity, and more sexuality in dreams. This increase of emotionally loaded contents can be related to a disinhibitory effect of this drug, and the possible involvement of dopaminergic or serotoninergic systems is discussed.

Adult↗
PubMed2003

Do zopiclone, zolpidem and flunitrazepam have residual effects on simulated task of collision anticipation?

Few studies have addressed the modifications in visual information processing brought about by taking hypnotic substances. The present experiment with healthy subjects investigated the residual effects of taking a single night-time dose of hypnotics on collision anticipation capacities the next morning. Visual sequences simulated the movement of a driver approaching an intersection where another vehicle was arriving. Ten participants had to estimate, as quickly as possible, whether the other vehicle would arrive before or after them at the intersection. They were tested after having taken a capsule of zolpidem (10 mg), zopiclone (7.5 mg), flunitrazepam (1 mg) or a placebo. The results show no residual effects of the molecules. Only flunitrazepam, a benzodiazepine with a long half-life, appears to cause subjects to focus their attention on an element which, while relevant for the task (a road sign playing the role of a spatial reference), is not used correctly.

Accidents, Traffic↗
PubMed1977

Polygraphic sleep recordings before and after the administration of flunitrazepam.

By means of polygraphic sleep recordings (EEG, EOG, EMG, ECG, EDG, Respirogram, Positogram), neurologic-psychologic investigation and questionnaires on subjective feeling, ten patients aged from 22 to 40 years (mean: 29 years), who suffered from irregular disturbances in falling asleep and in sleeping continuously, were examined over a period of ten consecutives nights. The first investigation night was reserved for adaptation of the patients and could therefore not be evaluated. On the following three evenings placebo (Placebo I) was given, then 2 mg of flunitrazepam for the ensuing three nights and placebo again (Placebo II) for the last three nights. Thus, 90 investigation nights could be evaluated. 1. Latency times until the patients fell asleep and up to the first deep sleep were reduced significantly by the active preparation. Latency times up to the first REM-phase were prolonged. 2. The frequency of nocturnal awakenings was lessened significantly. Thus, disturbances in sleeping continuously disappeared for the duration of the treatment. Duration of wakefulness after having woken during the night decreased considerably. 3. Duration of wakefulness during the total night was reduced considerably, deeper sleep stages, such as D (stage III) and E(stage IV) were prolonged. 4. Duration of the REM-phases was reduced slightly. This reduction was not significant according to the t-test. 5. According to these results, the preparation showed a clear effect. A placebo-effect can be excluded, since the improvements mentioned were not found when placebo was given before administration of the medication and afterwards (Placebo I and II). 6. When comparing our results to those of other authors, who described the effects of various preparations, we found that the substance flunitrazepam showed different effects.

Adult↗
PubMed1983

Flunitrazepam: acute benefit-risk assessment in general practice.

A methodology is described which is practical in assessing the benefit-risk ratio of a single new drug prior to marketing. Flunitrazepam at doses of 0.5 mg, 1.0 mg (and 2 mg) nocte in 2,435 patients is shown to be effective in 78% of patients and the acute risk, predictable and low, irrespective of age or dose. One may conclude that the acute benefit-risk ratio is acceptable with respect to the class of drug and indication for which flunitrazepam is prescribed.

Adult↗
PubMed1985

Intravenous flunitrazepam (Rohypnol) in conservative and restorative dentistry.

The study was undertaken to assess the suitability of intravenous flunitrazepam (Rohypnol) in patients requiring sedative cover for prolonged dental surgery. Fifty patients received up to 2 mg flunitrazepam to induce a satisfactory level of sedation. Further maintenance doses and local anaesthesia were given if required. The results showed the level of sedation and working conditions, as assessed by anaesthetist and surgeon, to be satisfactory in all but one patient. The majority of patients remained slightly drowsy the following morning but all stated they would undergo a similar procedure again.

Adult↗
PubMed1983

A placebo-controlled, dose-ranging study comparing 0.5 mg, 1 mg and 2 mg flunitrazepam in out-patients.

A placebo-controlled, dose-ranging study was carried out in 18 patients, aged under 65 years, with sleep disturbance to compare the hypnotic effects of 0.5 mg, 1 mg and 2 mg flunitrazepam and placebo. Patients received each treatment in random order for 7 days. Assessments by both doctor and patients were made on entry and at the end of each treatment period. The results showed that the 1 mg flunitrazepam dose was optimal with respect to speed of action, duration of action, quality of sleep and lack of residual clinical sequelae.

Adult↗