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PubMed1978

[Effects of diazepam and flunitrazepam on the undesired postoperative side-effects of ketamine anaesthesia (author's transl)].

150 patients undergoing minor gynaecological procedures (curretages) were anesthetized with ketamine and either diazepam flunitrazepam or placebo in order to establish the best combination for the prevention of postoperative psychotomimetic effects. From observations, up to 24 h after operation, it was found and statistically proven that the combination of ketamine/flunitrazepam as compared to the combinations ketamine/diazepam and ketamine/placebo led to a remarkable reduction of psychotomimetic side reactions.

Adult↗
PubMed1985

Effects of pentobarbital on t-[35S]butylbicyclophosphorothionate and [3H]flunitrazepam binding to membrane-bound and solubilized preparations from rat forebrain.

The binding sites for t-[35S]butylbicyclophosphorothionate ([35S] TBPS) and [3H]flunitrazepam ([3H]Flu) were solubilized from freshly prepared and washed membranes from rat forebrain with 20 mM 3-[(cholamidopropyl)-dimethylamonio]-1-propanesulfonate in the presence of protease inhibitors. Approximately 64% of the protein, 56% of the [35S]TBPS sites and 45% of the [3H] Flu sites were solubilized. The soluble and membrane-bound binding sites for [3H]Flu were relatively stable on storage at 0 degree C or at -65 degrees C for 11 days. Binding of [35S]TBPS to membranes was increased after freezing the membranes at -65 degrees C for 1 to 11 days and was relatively unchanged if the membranes were stored at 0 degree C for 1 to 11 days. Solubilized [35S]TBPS binding sites were stable when stored at -65 degrees C but declined to 20% of control when stored at 0 degree C for 11 days. Tested shortly after preparation, [35S]TBPS binding to both soluble and membrane preparations demonstrated similar affinity, temperature dependence and noncompetitive inhibition by pentobarbital (pb). Stimulation by pb of [3H]Flu binding to the soluble fraction decayed on storage of the solubilized material at 0 degree C with a time course similar to the loss of [35S]TBPS binding. This finding might suggest that the stimulation of [3H]Flu binding by pb is mediated via its action on TBPS sites. However in membrane preparations stored at 0 degree C, [35S]TBPS binding was stable whereas the pb effects declined with time.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1987

GABA enhancement of flunitrazepam binding in mice selectively bred for differential sensitivity to ethanol.

The binding of the benzodiazepine [3H]flunitrazepam (FNZ) and the allosteric enhancement of FNZ binding by gamma-aminobutyric acid (GABA) were investigated in brain tissue from short-sleep (SS) and long-sleep (LS) mice, lines selectively bred for differential sensitivity to ethanol. GABA enhanced FNZ binding in a dose-dependent manner in both lines. This enhancement was greater in SS than in LS cortical and cerebellar regions, but did not differ between lines in midbrain or hindbrain regions. In whole brain, no difference was observed between the two lines in the number or affinity of benzodiazepine receptors, as determined by FNZ binding. These results suggest that the nature of allosteric interactions within the GABA-benzodiazepine receptor complex is different for LS and SS mice.

Animals↗
PubMed1988

Diazepam, flunitrazepam and midazolam for elective endoscopy--a comparative study.

One hundred twenty patients undergoing elective endoscopies were studied. They were allocated into three groups and accordingly they received Diazepam, Flunitrazepam and Midazolam. The effect of these drugs on the task performance of the patient's memory, anxiety and sedation level were assessed using objective tests. Cardiovascular and respiratory parameters were also assessed. All observations were subjected to student's t-test and chi squared assessment. We concluded that there are no major differences between the three drugs in the dosage used. However, the Midazolam group showed faster recovery, more sedation, less pain on injection than the Diazepam group. As for the cardiovascular system, there was a tendency for hypotension and tachycardia in all groups. Patients in the Midazolam group had more amnesia as compared to the other groups.

Adult↗
PubMedDate not supplied

[Sedation with flunitrazepam during spinal anesthesia].

The clinical effects of flunitrazepam (FNZ) as IV sedative agent for spinal anaesthesia was studied. Of 112 elderly patients undergoing hip surgery, 40.2% have required a total dose of 26.6 +/- 2.3 mcg X kg-1. The repeat doses were 9.3 to 13.3 mcg X kg-1. A good state of sedation was obtained in 81% of patients, with a linear relationship between narcosis states and FNZ's doses. In 93% of cases, FNZ was provided peroperative amnesia without post-operative somnolence. No clinically adverse cardiovascular effects were encountered. There was a small, but statistically significant increase in arterial carbon dioxide tension. In summary, FNZ provided useful sedation.

Aged↗
PubMed1986

Failure of thyrotropin releasing hormone to reverse fentanyl-flunitrazepam anesthesia in man.

The effect of thyrotropin releasing hormone (TRH) on modified neuroleptanesthesia with fentanyl-flunitrazepam was investigated in an open pilot study of 15 neurosurgical patients. Before and 15, 30, and 60 minutes after extubation and subsequent administration of 400 micrograms TRH, the following parameters were evaluated: PaO2, PaCO2, vigilance, and pain sensation. Although no TRH-related impairment of postoperative analgesia was observed, respiratory depression and impaired vigilance were not significantly reversed. These findings contradict a number of experimental studies using animal models which indicated that TRH, due to its centrally mediated ergotropic activity, antagonizes the narcotic effect of various CNS depressants and anesthetics.

Adult↗
PubMed1986

[Effectiveness of the benzodiazepine antagonist Ro 15-1788 following anesthesia induced by flunitrazepam].

The competitive benzodiazepine antagonist Ro 15-1788 proved efficacious after general anaesthesia induced by flunitrazepam. It showed a quick onset of action within 1-2 min. After antagonisation, the heart rate, blood pressure and respiratory rate remained stable. No increased demand for analgesics could be demonstrated postoperatively. A transient anxiety that could be observed in 7 of 38 patients after doses between 0.5 and 2.0 mg seemed of minor clinical importance but may indicate that Ro 15-1788 acted not only as a pure antagonist but as a partially inverse agonist as well. Recurrence of sedation could be observed in 6 out of 38 patients after 2 h of Ro 15-1788 dosage. Careful observation of the patients for at least 2 h is therefore recommended even if antagonisation seemed successful. It was possible to reverse the benzodiazepine action successfully with doses between 0.3 and 0.8 mg. After these doses the patients will awake gently and gradually and unwanted side effects will be avoided. In our experience, Ro 15-1788 is a useful improvement in benzodiazepine application after surgical anaesthesia.

Anesthesia, General↗
PubMed1988

[Risks of premedication with benzodiazepines exemplified by a case of asphyxia caused by flunitrazepam].

Oral premedication with benzodiazepines is well established in clinical anaesthesia. Appreciation of the specific pharmacodynamic profile of available drugs suggest individual prescription for certain groups of patients. We report a case of severe respiratory depression following oral premedication with flunitrazepam 1 mg in a patient with intracranial neoplasma. With respect to this complication and a review of the literature we suggest administration of short acting benzodiazepines with pronounced anxiolytic and moderate sedative properties (lormetazepam type) for neurosurgical patients.

Asphyxia↗
PubMed1979

[Flunitrazepam with anterograde amnesia and reduction of blood pressure before local anaesthesia without intubation in 3000 ENT operations (author's transl)].

After premedication with flunitrazepam=Rohypnol 2 mg orally (2--3 hours preop.) and morphine-atropine (30 min preop.) the patient receives slowly "Ro" i.v. until the phenomenon of volume reduction when speaking is observed. This allows for the smallest possible dosis to achieve sufficient amnesia. After about 20 min the patient becomes responsive again, while his amnesia lasts for about 3 hours more. The cardiovascular functions remain stable with a 25% decrease of systolic blood pressure. Vomiting is reduced. The dry operative field makes microsurgery much easier and improves the final result of the operation. After gaining sufficient experience of the staff, 100% amnesia was achieved in all operations during the last 3 months.

Administration, Oral↗
PubMed1979

Influence of flunitrazepam on body functions.

The effects of intravenous flunitrazepam (Rohypnol, Roche) on various body functions were studied and the following conclusions were reached: it is a very potent sedative/hypnotic even in small doses, it may cause depression of spontaneous breathing, it does not give rise to raised cerebrospinal fluid or intra-ocular pressure, it does not adversely affect renal function, and it can be used quite safely in combination with fentanyl or pentazocine in anaesthetic practice.

Adult↗
PubMed1979

Practical experiences with flunitrazepam in anesthesia.

Flunitrazepam was used in general and local anesthesia. Little effect was noted on the respiratory and cardiovascular systems. In our patients there was an impressive period of amnesia and often we observed a central anticholinergic syndrome, which could be reversed by the use of physostigmine salicylate (0.04/kg body weight).

Adolescent↗
PubMedDate not supplied

[Study of flunitrazepam in the insomnia of the aged (author's transl)].

The efficiency of flunitrazepam was evaluated on the three phases of sleep in 20 patients 65 years old and more hospitalized suffering from severe insomnia. The experiment lasted 6 days. The initial dosage of half a tablet was sufficient and was maintained in 13 patients. In 5 subjects, dosage had to be increased to one tablet. In one subject, it was reduced to a quarter of a tablet. In the three quarters of the patients, the onset of sleep was of better quality; their actual sleep was longer and also of higher quality. The waking up was much easier in 18 patients who felt relaxed and alert during the morning. The alertness tests confirmed the patients state. The efficiency was satisfactory and the tolerance was very good. Taking into account the individual sensitivity of the aged, initial dosages must be small and adjusted according to the therapeutic responses.

Aged↗
PubMed1980

[Comparison of the effectiveness of triazolam (Halcion) and flunitrazepam (Rohypnol) in the preoperative period. A double blind crossover study].

The hypnotic effects of triazolam (Halcion) 0.25 mg and flunitrazepam (Rohypnol) 2 mg were compared in a randomized double-blind crossover study of 55 surgical patients in the preoperative stage. At these doses there was no significant difference between the two benzodiazepines regarding duration of sleep, depth of sleep and interruption of sleep. Sleep induction time was significantly shorter with Rohypnol, whereas waking was far pleasanter for patients after Halcion. The absence of hangover after Halcion is significant.

Anti-Anxiety Agents↗
PubMedDate not supplied

Sleep laboratory and clinical studies of the effects of triazolam, flunitrazepam and flurazepam in insomniac patients.

Polysomnographic recordings allow the recognition of three normal sleep stages: wakefulness, NREM and REM sleep. There are quantitative changes in these stages from childhood to old age. Most characteristic are progressive decreases in total sleep time, stage 4 NREM sleep and REM sleep. Insomnia can be defined as an alteration of both the quantity and quality of sleep. It can be associated with psychophysiological factors, psychiatric disorders, use of drugs and alcohol, sleep apnea, sleep-related myoclonus and restless legs, medical, toxic and environmental conditions, or REM sleep interruptions. At present, the benzodiazepines are the most frequently prescribed hypnotics. Their efficacy has been evaluated in the sleep laboratory and by means of sleep questionnaires (clinical studies). Their derivatives are grouped according to their pharmacokinetic profiles as short acting (triazolam), intermediate acting (flunitrazepam) and long acting (flurazepam). At the EEG level these compounds induce an increase in fast frequencies and in the number of sleep spindles. Slow wave activity is markedly decreased. All of the derivatives effectively and significantly induce and maintain sleep. Total sleep time increase is related to an imcrement of stage 2 sleep while REM sleep and stages 3 + 4 sleep are consistently reduced. Triazolam withdrawal is followed by a rebound insomnia. In contrast, under the same circumstances, flurazepam has a carry-over effect.

Adolescent↗