Articles: flunitrazepam.
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1. Chronic benzodiazepine treatment of rat cerebellar granule cells induced a transient down-regulation of the gamma-aminobutyric acidA (GABAA) receptor alpha 1 subunit protein, that was dose-dependent (1 nM-1 microM) and prevented by the benzodiazepine antagonist flumazenil (1 microM). After 2 days of treatment with 1 microM flunitrazepam the alpha 1 subunit protein was reduced by 41% compared to untreated cells, which returned to, and remained at, control cell levels from 4-12 days of treatment. ⋯ This study has shown that both flunitrazepam and GABA treatment, via their respective binding sites, caused a reduction in the expression of the GABAA receptor alpha 1 subunit protein; an effect mediated through the same neurochemical mechanism. The results also imply that the benzodiazepine effect is independent of GABA, and that the benzodiazepine and GABA sites may not be equally coupled to the down-regulation process, with the benzodiazepine site being the more dominant. The biochemical mechanism underlying the benzodiazepine-mediated down-regulation of the alpha 1 subunit protein seems to involve the activity of staurosporine-sensitive protein kinases.
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Randomized Controlled Trial Clinical Trial
[Anesthesia with flunitrazepam/fentanyl and isoflurane/fentanyl. Unconscious perception and mid-latency auditory evoked potentials].
There is a high incidence of intraoperative awareness during cardiac surgery. Mid-latency auditory evoked potentials (MLAEP) reflect the primary cortical processing of auditory stimuli. In the present study, we investigated MLAEP and explicit and implicit memory for information presented during cardiac anaesthesia. ⋯ During general anaesthesia auditory information can be processed and remembered postoperatively by an implicit memory function, when the electrophysiological conditions of primary cortical stimuli processing is preserved. Implicit memory can be observed more often when high-dose opioid analgesia is combined with receptor-binding agents like the benzodiazepines than under non-specific anaesthetics like isoflurane. Non-specific anaesthetics seem to provide a more effective suppression of auditory stimuli processing than receptor-specific agents.
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The influence of several intravenous anaesthetics on the heart was assessed using the isolated rat heart-lung preparation. Each group received 10(-3)mol litre-1 and 10(-4)mol liter-1 of ketamine, 6 micrograms ml-1 and 60 micrograms ml-1 of midazolam, 6 micrograms ml-1 and 60 micrograms ml-1 of diazepam or 0.6 micrograms ml-1 and 6 micrograms ml-1 of flunitrazepam. Systolic blood pressure in rats receiving high doses of midazolam, diazepam and ketamine were higher than that in the control group. ⋯ None of the intravenous anaesthetics, even in doses which were 100 times greater than therapeutic doses, showed any depressant effects in this preparation. Moreover, it is surprising that midazolam and diazepam produced direct increases in myocardial contractility. These results suggest that the cardiodepressant effects of intravenous anaesthetics may be due to their effects on the central nervous system.
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Minerva anestesiologica · Mar 1994
Randomized Controlled Trial Comparative Study Clinical Trial[Trazodone versus flunitrazepam in premedication in day-care surgery].
A prospective single-blind study was conducted to compare flunitrazepam vs trazodone in the premedication of patients undergoing day-case surgery for termination of pregnancy, with particular regard to the degree of preoperative sedation, intraoperative analgesia and postoperative recovery. 86 patients were randomly allocated to receive orally 45 minutes before the surgical procedure either flunitrazepam 2 mg (group F) or trazodone 50 mg (group T). In both groups anaesthesia was achieved by i.v. fentanyl 2.5 micrograms/kg and ketamina 250 micrograms/kg. Patients in group F showed a deeper degree of preoperative sedation. ⋯ In the postoperative period, the incidences of emetic symptoms and dizziness were similar in both groups; the incidence of drowsiness was significantly higher in group F at 120 minutes but not at 180 minutes of observation. Psychomotor performance was assessed preoperatively two days before the surgical procedure and 60, 120 and 180 minutes after surgery, using the Toulouse-Pieron test and the reaction time to a luminous stimulus with the aid of a computerized analogic tachystoscope (Neurometer). Trazodone allowed a more rapid recovery of psychomotor performance and it can represent a valid alternative to the use of benzodiazepines in the premedication of day-case surgical patients.