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PubMed1987

A comparison of the antifibrillatory effect of midazolam and flunitrazepam in acute myocardial ischaemia in the dog.

A study was carried out using a model of myocardial ischaemia in the dog after ligation of the left coronary artery to determine the effects of the benzodiazepines, flunitrazepam and midazolam, on the ventricular fibrillation threshold. The fibrillation threshold was measured twice within 15 min and 8 min after ligation. Fifteen minutes after the onset of ischaemic heart attack, 1.2 mg midazolam/kg or 0.25 mg of ischaemia. Their effects on haemodynamics were negligible. It is suggested that both benzodiazepines can be used for increasing electrical stability of the heart in patients with acute myocardial infarction and to inhibit the psychic stress response. Because of its short biological half-life and water solubility, allowing painless intravenous administration, midazolam offers a more flexible approach to pharmacotherapy immediately after acute heart attack according to the patient's current clinical status.

Animals↗
PubMed1993

Therapeutic effects of flunitrazepam in dystonias and torticollis. Preliminary communication.

A new form of clinical treatment is proposed for dystonias and torticollis using flunitrazepam (FN), a powerful agonist of all benzodiazepine receptors of GABA neurons. FN has a specific effect in dystonic patients, specially those in which the hypnotic effect of this drug is absent or diminished, thus suggesting the existence of two different neurochemical categories of dystonias.

Dystonia↗
PubMed1999

Flunitrazepam (Rohypnol) abuse in combination with alcohol causes premeditated, grievous violence in male juvenile offenders.

This study focuses on 19 juvenile offenders who were frequently intoxicated by flunitrazepam (FZ), almost exclusively under the brand name Rohypnol. Street names for Rohypnol tablets are Rophies, Ropies, Roofies, Ropes, Roches, Rochas, Rochas Dos, Rophs, Ropers, Ribs, R-25, Roach-2s, Trip and Fall, Remember All, Mind Erasers, Forget Pills, and the Date Rape Drug. An overdose of FZ gives an increased feeling of power and self-esteem, reduces fear and insecurity, and provides the belief that everything is possible. FZ is also associated with loss of episodic memory and with impulsive violence, particularly when combined with alcohol. The subjects were taken from a subpopulation of 47 male juvenile offenders from Swedish national correctional institutions. Background information for subjects was obtained by in-depth interviewing and personality inventories including the Zuckerman Sensation-Seeking Scales, the Eysenck Personality Questionnaire, and the Karolinska Scales of Personality. Data concerning previous criminal offenses was obtained from the Swedish National Police Board. Almost all of the FZ abusers had been previously sentenced for serious violent offenses. Our data suggest that FZ abused by psychiatrically vulnerable subjects (i.e., with high scores on boredom susceptibility and verbal aggression) poses a serious hazard both to the abusers as well as the community. Our results support the finding that FZ should be classified as a Schedule I drug (i.e., a drug similar to heavy narcotics).

Adolescent↗
PubMed1999

Deposition of [3H]cocaine, [3H]nicotine, and [3H]flunitrazepam in mouse hair melanosomes after systemic administration.

Microautoradiography was employed to show that association of drugs from the serum directly with forming hair pigment is a primary pathway of deposition into the hair. After systemic administration of [3H]flunitrazepam, [3H]nicotine, and [3H]cocaine, association of all three drugs with melanin in the forming hair was observed within minutes of dosage. Sebum was determined to be an insignificant deposition route for all three drugs. Pigmented mice had significantly higher concentrations of all three drugs than did nonpigmented mice. The results provide a better basis for ultimately using hair for reliable analysis of drug and environmental toxin exposure.

Animals↗
PubMed1999

[Control of medical practitioners' prescription of flunitrazepam preparations in the County of Copenhagen and municipality of Frederiksberg].

Aiming to limit the misuse of Flunitrazepam medicaments, these were made subject to registered prescription from 11.3.1996. At the same time, The National Board of Health informed every medical practitioner of the recommended daily dose and duration of treatment. A systematic superintendence was established in the region. Medical practitioners prescribing more than four times the recommended dose were identified and applied to one respectively two years after implementation of the prescription registration. In most regions of Denmark the superintendence of the Medical Officers has been occasional. Consumption development was surveyed in the period of 1.1.1996-30.6.1998. At the end of the period the consumption was reduced with 90% in the region and with 85% in the rest of Denmark. The consumption level was at the end of the period significantly lower in this region compared to the rest of Denmark.

Anti-Anxiety Agents↗
PubMed2000

Cytotoxic and immunomodulative effects of flunitrazepam, zipeprol and trihexyphenidyl on human peripheral blood lymphocytes.

The cytotoxic effects of flunitrazepam, zipeprol and trihexyphenidyl on cell viability of peripheral blood mononuclear cells from healthy volunteers were studied at concentrations from 10(-2) to 10(-8) M by 2 colorimetric in vitro assays: the neutral red uptake assay and thiazolyl blue tetrazolium bromide assay. All tested drugs of abuse were non-cytotoxic at concentrations lower than 10(-5) M. Possible immunomodulative effects of these substances were evaluated through phytohemagglutinin induced lymphocyte proliferation ([3H]-thymidine DNA incorporation assay) and by a 51Cr release natural killer assay. The 3 drugs studied produced statistically significant immunomodulative alterations on both immunological parameters.

Adjuvants, Immunologic↗
PubMed2001

CYP3A4 is the major CYP isoform mediating the in vitro hydroxylation and demethylation of flunitrazepam.

The kinetics of flunitrazepam (FNTZ) N-demethylation to desmethylflunitrazepam (DM FNTZ), and 3-hydroxylation to 3-hydroxyflunitrazepam (3-OH FNTZ), were studied in human liver microsomes and in microsomes containing heterologously expressed individual human CYPs. FNTZ was N-demethylated by cDNA-expressed CYP2A6 (K(m) = 1921 microM), CYP2B6 (K(m) = 101 microM), CYP2C9 (K(m) = 50 microM), CYP2C19 (K(m) = 60 microM), and CYP3A4 (K(m) = 155 microM), and 3-hydroxylated by cDNA-expressed CYP2A6 (K(m) = 298 microM) and CYP3A4 (K(m) = 286 microM). The 3-hydroxylation pathway was predominant in liver microsomes, accounting for more than 80% of intrinsic clearance compared with the N-demethylation pathway. After adjusting for estimated relative abundance, CYP3A accounted for the majority of intrinsic clearance via both pathways. This finding was supported by chemical inhibition studies in human liver microsomes. Formation of 3-OH FNTZ was reduced to 10% or less of control values by ketoconazole (IC(50) = 0.11 microM) and ritonavir (IC(50) = 0.041 microM). Formation of DM FNTZ was inhibited to 40% of control velocity by 2.5 microM ketoconazole and to 30% of control by 2.5 microM ritonavir. Neither 3-OH FNTZ nor DM FNTZ formation was inhibited to less than 85% of control activity by alpha-naphthoflavone (CYP1A2), sulfaphenazole (CYP2C9), omeprazole (CYP2C19), or quinidine (CYP2D6). Thus, CYP-dependent FNTZ biotransformation, like that of many benzodiazepine derivatives, is mediated mainly by CYP3A. Clinical interactions of FNTZ with CYP3A inhibitors can be anticipated.

Anti-Anxiety Agents↗
PubMed2002

Violent behavior, impulsive decision-making, and anterograde amnesia while intoxicated with flunitrazepam and alcohol or other drugs: a case study in forensic psychiatric patients.

It is known that many male juvenile delinquents commit violent crimes while intoxicated with flunitrazepam (FZ), often in combination with alcohol or other drugs. We have also noted the combined abuse of FZ with, for example, alcohol in male forensic psychiatric patients. Our objective was to study violent behavior, impulsive decision-making, and amnesia in male forensic psychiatric patients who were intoxicated predominantly with FZ, to increase knowledge of the abuse of FZ in vulnerable subjects. We studied five forensic psychiatric patients, all of whom were assessed in 1998. All of the subjects reported earlier reactions to FZ, including hostility and anterograde amnesia. At the time of their crimes they were all intoxicated with FZ, often in combination with alcohol or other drugs, such as amphetamine or cannabis. In contrast to their behavior based on their ordinary psychological characteristics, their crimes were extremely violent, and the subjects lacked both the ability to think clearly and to have empathy with their victims. Our observations support the view that FZ abuse can lead to serious violent behavior in subjects characterized by vulnerable personality traits, and that this effect is confounded by the concurrent use of alcohol or other drugs. It is evident that FZ causes anterograde amnesia. Previous research and the results presented herein allow us to draw the following conclusion: on the basis of the neuropsychopharmacologic properties of FZ, legal decisions, such as declaring FZ an illegal drug, are needed in countries where it is now legal.

Adolescent↗
PubMed2002

[Combined use of melatonin and low-dose flunitrazepam for treatment of sleep disturbance in a child with spastic quadriplegia: evaluation using polysomnography].

A 14-year-old boy born at 39 gestational weeks with the birth weight of 3,250 g, had severe mental retardation and spastic quadriplegia of unknown etiology from early childhood. At 7 years of age, disturbance of night sleep appeared with several awakenings. Combined treatment with melatonin (MLT; 0.04 mg/kg) and flunitrazepam (FNZ; 0.025 mg/kg) was more effective than monotherapy with FNZ for the sleep disturbance. Difference of the effects of the combined therapy and the monotherapy for the sleep disturbance were assessed by polysomnographies (PSGs), consisted of EEG (C3, C4), bipolar EOG and surface EMG on the mentalis muscle. The PSGs were performed twice at 13 years 6 months old, and at 14 years 1 month old. In both trials, the number of awakening was fewer, total sleep time was longer, percent (%) stage I and II were lower and %REM sleep was larger in combined MLT and FNZ therapy than in FNZ monotherapy. The present study suggests that the combined MLT and FNZ therapy not only reduces awakening during sleep but also normalizes sleep architecture. This therapy is valuable because normalization of sleep is important for the developing brain as it reflects the normal functioning of the aminergic neurons of the midbrain and the brainstem which have important roles for morphological and functional development of the brain in immature brain.

Adolescent↗
PubMed1992

Pentobarbital-enhanced [3H]flunitrazepam binding throughout the rat brain: an autoradiographic study.

The gamma-aminobutyric acidA/benzodiazepine receptor contains distinct ligand binding sites for hypnotic barbiturates and benzodiazepines. It is thought that barbiturate-induced sedation is produced, in part, by enhancing agonist binding to this receptor. The present study tested the hypothesis that pentobarbital would enhance benzodiazepine binding in a site-specific manner across the rat brain. In vitro receptor autoradiography was used to localize and quantitatively map [3H]flunitrazepam ([3H]FLU) binding in the absence and presence of pentobarbital in 133 brain areas. Each area demonstrated a statistically significant increase in [3H]FLU binding in the presence of in vitro pentobarbital (P < or = 0.05). Hindbrain nuclei dominated the top 20% of brain areas demonstrating the greatest pentobarbital-induced increases in [3H]FLU binding. The greatest mean percent increase in [3H]FLU binding occurred in the medulla, including areas known to be important for cardiovascular control, breathing, motor tone and regulating levels of arousal. These findings show that differential enhancement of benzodiazepine binding in the presence of pentobarbital occurred in brain areas controlling physiological functions known to be impaired by systemically administered pentobarbital.

Animals↗
PubMed1992

Acute poisonings with ethyle loflazepate, flunitrazepam, prazepam and triazolam in children.

Even though acute poisonings with benzodiazepines are extremely common, less is known of the clinical toxicity of recent derivatives, particularly in children. 1,989 cases involving ethyle loflazepate, flunitrazepam, prazepam or triazolam recorded at the Lyons Poison Center and due to 1 compound and associated with clinical symptoms were selected for study. Children less than 16-y of age accounted for 482 cases. Sleepiness, agitation and ataxia were significantly more frequent in the children. Hypotonia was seldom observed but was indicative of severe poisoning. The dangerous toxic dose of these compounds in children is suggested to be 0.78-0.90 mg ethyle loflazepate/kg, 0.26-0.29 mg flunitrazepam/kg, 7.80-9.00 mg prazepam/kg and 0.06-0.07 mg triazolam/kg. These results are in keeping with the relatively low acute toxicity of the older benzodiazepines.

Adolescent↗
PubMed1976

The amnesic action of diazepam, flunitrazepam and lorazepam in man.

Studies in man show that it is possible to reliably study the incidence, degree and duration of amnesia produced by drugs by showing patients 10 postcards and testing their ability to recall or recognise them six hours later. Using this method of study it was found that 1 mg flunitrazepam produced a comparable degree of amnesia to 10 mg diazepam, although its action was slightly longer. This difference was more marked when double doses were studied. The onset of the amnesic action of both drugs occurred within 2 minutes of their intravenous injection and rarely persisted for more than 10-15 minutes. In contrast, with 4 mg lorazepam the onset of amnesia was slower and persisted for up to 270 minutes. This was accompanied by a moderate but not excessive amount of drowsiness. Possible clinical uses for such a drug deserve serious consideration.

Amnesia↗
PubMed1977

[Anaesthesia with flunitrazepam (rohypnol) and fentanyl for geriatric patients (author's transl)].

Favorable clinic experiences with an anaesthetic involving rohypnol (flunitrazepam) and fentanyl led to an investigation of the haemodynamic effect of this procedure in a group of 9 geriatric patients, aged from 86 to 95 years. Anaesthesia was induced with 0.5 mg rohypnol and 0.1 to 0.2 mg fentanyl depending on the narcotic effect of rohypnol, intubation was performed under relaxation with suxamethonium and long term relaxation was achieved with pancuronium. The patients were normoventilated with nitrous oxide/oxygen. The individual values of the changes in cardiac output and total peripheral resistance showed a great variation. There was a significant correlation between the relative changes in mean arterial pressure and total peripheral resistance (r = 0.69, p less than 0.05) but no correlation between mean arterial pressure and cardiac output (r = 0.09). This indicates that the pronounced drop in arterial pressure which occurred in 4 patients can be explained by a decrease in total peripheral resistance. Careful dosage of the drugs, in particular of fentanyl, and knowledge of adequate measures to treat a decrease in blood pressure if it occurs, appears to be a prerequisite for the use of this type of anaesthesia in poor risk patients.

Age Factors↗
PubMed1977

Determination of flunitrazepam, desmethylflunitrazepam and clonazepam in plasma by gas liquid chromatography with an internal standard.

A method is developed for gas-chromatographic determination of flunitrazepam, desmethylflunitrazepam and clonazepam in plasma, using methylclonazepam as internal standard. Following extraction of the benzodiazepines and their hydrolysis, the benzophenones are analyzed by gas-chromatography, with a glass column filled with 3% OV-225 on Gas Chrom Q and a 63Ni electron capture detector. The technique has a good selectivity. Its limit of sensitivity is about 0.5 ng/ml of plasma. It is suitable for investigations on pharmacokinetics and bioavailability as well as for monitoring the correlation between plasma level and therapeutic efficacy and toxicology.

Administration, Oral↗
PubMed1991

[A comparative study of the efficacy and tolerance of dipotassium clorazepate and flunitrazepam for oral premedication].

The literature shows that benzodiazepines, in view of their anxiolytic, sedative, amnesic, muscle relaxant and anticonvulsive action, are the most important substances for premedication. Eminent workers regard anxiolysis as the most important aim of premedication. In the present clinical study, oral administration of the two different benzodiazepine derivatives, flunitrazepam (F) and chlorazepate dipotassium (CD) have been explored with a view to side effects, tolerance, quality of sleep during the night, anxiolytic effect and sedation. The study involved 108 women patients aged from 20 to 60 years (ASA class I or II), all scheduled to undergo gynecological surgery in general anesthesia. There were also 20 women who received no premedication. The three groups of patients were further divided into early (operation started before 10:30 a.m.) and late-operation (operation started after 10:30 a.m.) groups. The test drugs were administered as follows: 43 women received 50 mg CD p.o. on the evening before the operation, followed by 25 mg p.o. in the morning; 45 women received 2 mg F p.o. on the evening before the operation, followed by 1 mg p.o. in the morning. All patients took the preoperative premedication at 7 o'clock in the morning. Following this medication, the anxiolytic, sedative, and amnesic effects, side effects, vigilance and O2 saturation (SaO2) were determined at defined points during the day of the operation and the 1st postoperative day. Blood pressure and heart rate were recorded and interpreted as physiological stress parameters. Anxiolysis was determined using the Erlangen Anxiety Scale (EAS) of Galster and Spörl; the degree of sedation was assessed by the anesthesiologist; amnesia was determined by the patients' recognition of picture cards; vigilance and side-effects were assessed by standardized questionnaires. Both active drugs clearly improved the quality of sleep in the night before the operation over that experienced with no premedication. There were no significant differences among the three groups in the physiological stress parameters. The preoperative SaO2 saturation was decreased significantly by oral F, but it was always more than 95%. CD had little influence on the SaO2. Unwanted somatic symptoms were found a little more frequently in the group without any premedication. There were no signs of restricted tolerance for either of the test drugs. In the premedicated groups, pre- and postoperative anxiety decreased significantly.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗
PubMed1977

[Change in the mental contents in the paradoxical stage and in stage 2 under the effects of a benzodiazepine, flunitrazepam].

In some insomniacs under flunitrazepam treatment is noted on one hand a global increase of dream memories, and on the other hand an increase of dreams with unpleasant or anxious contents. The present investigation is intended first to test the hypothesis of a possible increase of mental contents in sleep outside the paradoxical phases, to account for the increase of dream memories without concomitant increase of paradoxical stage. Second it intends to investigate if the increase of unpleasant dreams may be found in the normal subject in laboratory.

Adult↗
PubMed1991

[Sedation with flunitrazepam and its antagonism with flumazenil in endoscopic urological procedures: our clinical experience].

Patients, especially males, do not easily stand endoscopic urological diagnostic examinations. So flunitrazepam (0.01 mg/kg IV) has been used to insure a suitable sedation. At the end of such examination flumazenil, a selective benzodiazepine antagonist has been injected. The levels of sedation and orientation so obtained and the cardiorespiratory parameters have been collected during a one hour follow-up from the intravenous injection of the antagonist. This method presents minimal side effects (a marginal, but statistically significative, systolic arterial pressure reduction), a completely normal coordination of movements and awareness of space and time relationship at the end of the observation period. Therefore it is a very good solution for short time examinations giving the chance to safely and shortly dismiss the patient.

Adult↗
PubMed1989

The use of flunitrazepam (Rohypnol) in paediatric plastic surgery.

The efficacy of flunitrazepam, a sedative and hypnotic agent, in facilitating minor procedures in plastic surgery was assessed in 25 children. The drug was administered in a dose of 0.030 mg/kg body weight. Adequate sedation was achieved with minimal side effects. The respiratory rate and the blood pressure showed minimal change whereas the pulse rate was unaltered.

Child↗