A.J. Clatworthy, L. V. Jones, Martin J. Whitehouse,
... chromatography mass spectrometry of the major metabolites of flurazepam A. J. Clatworthy, A. J. Clatworthy The Metropolitan ... spectra and gas chromatographic data are presented for flurazepam and its metabolites; monodesethyl flurazepam, didesethylflurazepam, hydroxyethylflurazepam, N1-desalkylflurazepam, N1-desalkyl-3-hydroxy flurazepam, and flurazepam-N1-acetic acid. The on-column thermal degradation of didesethylflurazepam, N1-desalkyl-3-hydroxyflurazepam and flurazepam-N1-acetic acid is reported and discussed. Mass ...
Tópico(s): Neuroscience and Neuropharmacology Research
1977 - Wiley | Biological Mass Spectrometry
L. C. Johnson, David M Seales, Paul Naitoh, Michael W. Church, M. Sinclair,
To further evaluate the effects of flurazepam on EEG during sleep, following 7 nights of placebo baseline, flurazepam (30 mg) was administered to 6 young adult poor sleepers for ... sleepers and 11 poor sleepers. Repeated use of flurazepam caused a gradual decrease in delta amplitude and ... nights than the rate of decrease in amplitude. Flurazepam also significantly reduced evoked K-complex amplitude but ... study indicate that the reduction of SWS with flurazepam during the initial drug nights is due primarily ...
Tópico(s): EEG and Brain-Computer Interfaces
1979 - Elsevier BV | Electroencephalography and Clinical Neurophysiology
Clarence E. Elallenger, Don W. King, Brian B. Gallagher,
... The present experiment investigated the effects of chronic flurazepam treatment on the mRNA levels for alpha 1, ... cortex, cerebellum, and hippocampus. Rats were treated with flurazepam for 2 or 4 weeks, and the mRNA ... receiving drug or 48 hr after 4-week flurazepam treatment had been stopped. The level of alpha ... rats 4 hr after a single injection of flurazepam or diazepam. The levels of mRNAs were analyzed ... in cortex and hippocampus were not changed after flurazepam treatment for 2 weeks. However, with rats treated ...
Tópico(s): Memory and Neural Mechanisms
1983 - Lippincott Williams & Wilkins | Neurology
Barry D. Waterhouse, Hylan C. Moises, Hermes H. Yeh, Herbert M. Geller, D.J. Woodward,
... present study was that the benzodiazepines (i.e., flurazepam) and norepinephrine (NE) share a common mechanism to ... following groups: 1) naive, 2) acute or chronic flurazepam treated, 3) chronic desmethylimipramine treated and 4) injected ... were examined before, during and after NE or flurazepam microiontophoresis in all treatment groups. Drug response histograms were generated and used to quantitate NE and flurazepam effects on spontaneous activity and GABA-induced inhibitory ... GABA facilitating action in naive controls, iontophoretically applied flurazepam was ineffective in augmenting GABA-induced suppression of ...
Tópico(s): Neuroscience and Neuropharmacology Research
1984 - American Society for Pharmacology and Experimental Therapeutics | Journal of Pharmacology and Experimental Therapeutics
... the effects and the mechanism of action of flurazepam and diazepam on human platelet activation. One minute preincubation with flurazepam (3-300 microM) or diazepam (3-300 microM) ... concentration of diazepam (265 microM) as compared to flurazepam (58 microM), was required to inhibit arachidonic acid ... production of malondialdehyde (MDA) by 50%. In addition, flurazepam and not diazepam inhibited the release of arachidonic ... in a concentration dependent manner. In other experiments flurazepam but not diazepam also blocked aggregation and secretion ...
Tópico(s): Receptor Mechanisms and Signaling
1985 - Elsevier BV | Thrombosis Research
Martin B. Scharf, Paul B Roth, Roberto A. Dominguez, J. Catesby Ware,
... the safety and efficacy of estazolam compared with flurazepam as hypnotics. Outpatients complaining of insomnia were randomized to receive either estazolam 2 mg, flurazepam 30 mg or placebo for 7 consecutive nights. ... The patient subjective questionnaire indicated that estazolam and flurazepam signiflcantly improved all parameters ( P < .05) as compared ... 63/81) and 36% (27/76) of estazolam, flurazepam, and placebo recipients, respectively. There were no significant differences in hypnotic effect between estazolam and flurazepam. All efficacy parameters of the investigators' global evaluation ...
Tópico(s): Memory and Neural Mechanisms
1990 - Wiley | The Journal of Clinical Pharmacology
Tai-Jun Zhao, Ted H. Chiu, Howard C. Rosenberg,
... The present experiment investigated the effects of chronic flurazepam treatment on the mRNA levels for alpha 1, ... cortex, cerebellum, and hippocampus. Rats were treated with flurazepam for 2 or 4 weeks, and the mRNA ... receiving drug or 48 hr after 4-week flurazepam treatment had been stopped. The level of alpha ... rats 4 hr after a single injection of flurazepam or diazepam. The levels of mRNAs were analyzed ... in cortex and hippocampus were not changed after flurazepam treatment for 2 weeks. However, with rats treated ...
Tópico(s): Amino Acid Enzymes and Metabolism
1994 - American Society for Pharmacology and Experimental Therapeutics | Molecular Pharmacology
Yunxing Wu, Howard C. Rosenberg, Ted H. Chiu,
... BZ) binding in rats treated 4 weeks with flurazepam was relatively greater and more widespread when measured ... zolpidem binding was studied in rats treated with flurazepam. [3H]Zolpidem binding was also studied in rats ... to cause tolerance. Rats were chronically treated with flurazepam for 1 or 2 weeks, or with midazolam ... group of rats was acutely treated with desalkyl-flurazepam and killed 30 min later. After 2 weeks of flurazepam treatment, the Bmax of [3H]zolpidem binding was ... Kd in any region. After 1 week of flurazepam treatment, the Bmax was decreased by 23% in ...
Tópico(s): Memory and Neural Mechanisms
1995 - Elsevier BV | European Journal of Pharmacology
... efficacy of triazolam was compared to that of flurazepam and placebo in 120 out-patient insomniacs. Each ... 0.5 mg) was compared to placebo and flurazepam (30 mg). Triazolam (0.25 mg) was compared to flurazepam (15 mg and 30 mg). Triazolam (0.5 mg) was preferred to both placebo and flurazepam (30 mg). Triazolam (0.5 mg) was superior ... awakenings. Triazolam (0.5 mg) was superior to flurazepam (30 mg) in speeding sleep onset and increasing ... sleep. Triazolam (0.25 mg) was preferred to flurazepam (15 mg) and was significantly better than flurazepam ...
Tópico(s): Homelessness and Social Issues
1978 - SAGE Publishing | Journal of International Medical Research
The effects of flurazepam hydrochloride on GABA- or glutamate-evoked responses recorded from the lobster muscle fibre and the frog isolated spinal cord were studied using electrophysiological techniques. On lobster muscle flurazepam (up to 100 μM) reversibly antagonized responses to ... any effect on GABA responses. Higher concentrations of flurazepam (>200 μM) sometimes increased the resting membrane conductance, ... In the tetrodotoxin (TTX)-treated frog spinal cord flurazepam (5 μM) reversibly antagonized both glutamate- and GABA- ...
Tópico(s): Neuroscience and Neural Engineering
1978 - Elsevier BV | Neuropharmacology
W. A. Mahon, T. Inaba, R.M. Stone,
The metabolism of flurazepam-5-14C has been studied in man following catheterization of the portal and hepatic veins. Flurazepam was administered through a tube into the stomach ... a rapid and early appearance of metabolites of flurazepam consistent with the metabolism of the flurazepam by the intestinal mucosa and at times when ... blood were the mono- and didesetyl metabolies of flurazepam. Considerable hepatic uptake of flurazepam and its metabolites occurred, as evidenced by the ... the hepatic vein. Thus, "first-pass" metabolism of flurazepam following oral administration occurs in the small bowel ...
Tópico(s): Drug Transport and Resistance Mechanisms
1977 - Wiley | Clinical Pharmacology & Therapeutics
Robert J. Marley, Ronald K. Freund, Jeanne M. Wehner,
... the anesthetic, hypothermic and anticonvulsant effects of benzodiazepine, flurazepam, was determined. Flurazepam (75–300 mg/kg) induced a dose-dependent ... fold greater sensitivity to the anesthetic effects of flurazepam. A dose-dependent decrease in body temperature was also observed following administration of flurazepam (25–150 mg/kg), but the two lines ... this measure. Determination of the anticonvulsant effects of flurazepam (1–6 mg/kg) against seizures induced by ... LS and SS mice differ in response to flurazepam, but the nature of the difference depends on ...
Tópico(s): Memory and Neural Mechanisms
1988 - Elsevier BV | Pharmacology Biochemistry and Behavior
Xiaojing Hu, Maharaj K. Ticku,
We have investigated the effect of chronic flurazepam HCl treatment on the gamma-aminobutyric acid (GABA)A receptor complex in cultured mammalian cortical neurons. Chronic flurazepam (1-5 microM, for 1-10 days) treatment ... not altered after the chronic treatment. However, chronic flurazepam treatment produced uncoupling between GABA and pentobarbital sites ... and pentobarbital were not significantly altered after chronic flurazepam treatment; however, their Emax values were decreased by approximately 50%. The effect of chronic flurazepam treatment on the observed uncoupling was both time ...
Tópico(s): Analytical Chemistry and Chromatography
1994 - American Society for Pharmacology and Experimental Therapeutics | Molecular Pharmacology
... in vitro have been investigated. The benzodiazepine agonist, flurazepam, at high concentrations, blocked pentagastrin‐induced excitations in ... of CCK A receptors leads to neuronal depolarization, flurazepam also produced a weak block of the CCK response. Flurazepam blocked CCK responses but not carbachol‐induced excitations ... VMH neurones. The inhibition of CCK responses by flurazepam was not blocked by the benzodiazepine antagonist, flumazenil. These data suggest that flurazepam is a weak antagonist at central CCK B ...
Tópico(s): Hypothalamic control of reproductive hormones
1994 - Wiley | British Journal of Pharmacology
James N. Reynolds, Rajatavo Maitra,
... propofol and benzodiazepines, the effect of propofol and flurazepam on GABAA receptor function was examined in Xenopus ... 1-10 microM) concentrations of propofol together with flurazepam (0.25-0.5 microM) was significantly greater ... indicated a strong synergistic interaction between propofol and flurazepam at either of the receptor constructs examined. In ... facilitation of GABA receptor-activated current compared to flurazepam, produced a less than additive potentiation when combined with propofol. Flurazepam significantly decreased the EC50 concentration of propofol for ...
Tópico(s): Memory and Neural Mechanisms
1996 - Elsevier BV | European Journal of Pharmacology
John T. G. Hamilton, Peggy A. Stone,
... of the peripheral neuromuscular activity of the benzodiazepine, flurazepam. In previous reports we have documented peripheral neuromuscular ... phrenic nerve diaphragm preparation. The water soluble benzodiazepine, flurazepam, has been studied on the rat phrenic nerve ... rectus abdominis in vitro. On the former preparation flurazepam enhanced and then blocked the response to indirect ... tetanic contracture (30 Hz). On the later preparation, flurazepam blocked in a noncompetitive manner the response of ... blockade in preparations pretreated with low concentrations of flurazepam. This was not observed when flurazepam was given ...
Tópico(s): Anesthesia and Neurotoxicity Research
1982 - NRC Research Press | Canadian Journal of Physiology and Pharmacology
DeMing Song, Shide Zhang, K. Kohlhof,
... NCI) mass spectrometric method for the determination of flurazepam and its metabolites N-1-hydroxyethyl-flurazepam and N-1-desalkyl-flurazepam in mouse and rat plasma was described. Derivatization of the metabolites of flurazepam with BSTFA allowed a highly stable, accurate, and ... were 0.1 ng/ml for N-hydroxyethyl-flurazepam-TMS (Mr = 404), 0.5 ng/ml for desalkyl-flurazepam-TMS (Mr = 360), and 0.5 ng/ml for flurazepam (Mr = 387) with an injection volume of 1 ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
1994 - Elsevier BV | Journal of Chromatography B Biomedical Sciences and Applications
Kosho AKUTAGAWA, Minoru Makino, Kenji Ishii,
Effects of flurazepam, a benzodiazepine derivative, on Ca2+-induced cardio-stimulant contractile activity in normal Tyrode's solution and Ca2+-mediated ... from guinea-pigs. In normal Tyrode's solution, flurazepam (1 X 10(-6), 1 X 10(-5) ... In K+ (19 mM)-rich Tyrode's solution, flurazepam (3 X 10(-5) M) decreased contractile amplitude ... time-dependently. In K+ (19 mM)-depolarized preparations, flurazepam (3 X 10(-5) M) competitively shifted the ... 8 X 10(-6) M)-treated atrial preparation, flurazepam (3 X 10(-5) M) consistently suppressed contraction. ...
Tópico(s): Neuroscience and Neuropharmacology Research
1983 - Japanese Pharmacological Society | The Japanese Journal of Pharmacology
Thomas Röth, P Piccione, Patricia J. Salis, M Krámer, M Kaffeman,
The effect of temazepam 15 and 30 mg, flurazepam 15 and 30 mg, quinalbarbitone 100 and 200 ... maintenance were observed with temazepam 30 mg and flurazepam 30 mg. REM sleep was suppressed by quinalbarbitone, and by flurazepam 30 mg. Flurazepam 30 mg had the greater effect on cognitive ... Subjective assessments of alertness were most affected by flurazepam, and by quinalbarbitone 200 mg. The results suggest ... effects and is shorter acting than quinalbarbitone and flurazepam.
Tópico(s): Sleep and Wakefulness Research
1979 - Wiley | British Journal of Clinical Pharmacology
Mary A. Carskadon, Wesley F. Seidel, David J. Greenblatt, William C. Dement,
The effects of triazolam (0.25 mg) or flurazepam (15 mg) were evaluated in 13 elderly (ages ... in both groups. MSLT showed increased sleepiness with flurazepam and decreased sleepiness with triazolam. MSLT scores were unrelated to nocturnal sleep parameters in the flurazepam group and showed a pattern of correlation, though ... in the triazolam group. Vigilance was impaired with flurazepam and unchanged with triazolam. Other performance tests showed ... with drugs. Mood tended to be improved after flurazepam ingestion and unchanged after triazolam. These findings suggest ...
Tópico(s): Sleep and Wakefulness Research
1982 - Oxford University Press | SLEEP
J.C. Blanchard, Jean‐Luc Zundel, L Julou,
... propofol and benzodiazepines, the effect of propofol and flurazepam on GABAA receptor function was examined in Xenopus ... 1–10 μM) concentrations of propofol together with flurazepam (0.25–0.5 μM) was significantly greater ... indicated a strong synergistic interaction between propofol and flurazepam at either of the receptor constructs examined. In ... facilitation of GABA receptor-activated current compared to flurazepam, produced a less than additive potentiation when combined with propofol. Flurazepam significantly decreased the EC50 concentration of propofol for ...
Tópico(s): Memory and Neural Mechanisms
1983 - Elsevier BV | Biochemical Pharmacology
Merrill M. Mitler, Wesley F. Seidel, Johanna Van den Hoed, David J. Greenblatt, William C. Dement,
... daytime function in insomniac patients who took either flurazepam, 30 mg, triazolam, 0.5 mg, or placebo ... 2, subjects took placebo; weeks 3 to 7, flurazepam, triazolam, or placebo; weeks 8 and 9, placebo. ... during weeks 1, 3, 5, 7, and 8. Flurazepam showed hypnotic efficacy for weeks 3 to 5. ... to 7. Although not significant overall, discontinuation of flurazepam produced rebound insomnia in six of seven subjects ... concentration of desalkylflurazepam, the principal active metabolite of flurazepam, and sleep disturbance suggested that the onset of ...
Tópico(s): Schizophrenia research and treatment
1984 - Lippincott Williams & Wilkins | Journal of Clinical Psychopharmacology
Mortimer Mamelak, Leslie T. Buck, A Csima, Victoria Price, Alison Smiley,
... middle-aged insomniac patients were treated with placebo, flurazepam, or zopiclone for 12 consecutive days in a ... compare the residual daytime effects of long-acting flurazepam and short-acting zopiclone on a variety of ... withdrawal. The study demonstrated persistent performance effects with flurazepam. Testing at the end of the treatment period showed that movement time was impaired in the flurazepam treated group. Flurazepam also enhanced the increment of movement time produced ... became severely confused when given ethanol after using flurazepam for 12 days. None of these effects were ...
Tópico(s): Memory and Neural Mechanisms
1987 - Oxford University Press | SLEEP
Barbara Gothe, Neil S. Cherniack, Lin Williams,
... ingestion of a single dose of 30 mg flurazepam. Progressive hypercapnia was produced at two levels of ... hyperoxic CO2 response curve was not affected by flurazepam during wakefulness or sleep. After administration of flurazepam to the subjects, the shift of the CO2 ... was similar in the control condition and after flurazepam. We conclude that (a) both natural and flurazepam-induced sleep depress ventilatory responses to hyperoxic and ... interact as arousal stimuli in both natural and flurazepam-induced sleep.
Tópico(s): Sleep and Wakefulness Research
1986 - Oxford University Press | SLEEP
A schedule of treatment with the benzodiazepine, flurazepam, in mice for 7 days caused a significant enhancement of the convulsive effects of the partial inverse agonist FG7142. Full convulsions were seen with FG7142 after the chronic administration of flurazepam, although this compound does not cause convulsions in ... at 24 hr after the last dose of flurazepam and lasted for up to a week. The chronic treatment with flurazepam caused tolerance to the effects of flurazepam, but the tolerance was of shorter duration than ...
Tópico(s): Pain Mechanisms and Treatments
1988 - Elsevier BV | Neuropharmacology
Jay B. Cohn, Charles S. Wilcox, J. Douglas Bremner, Milton G. Ettinger,
... to compare its hypnotic efficacy to that of flurazepam, generally considered the reference standard. The hypnotic efficacy ... and 2 mg) was compared with that of flurazepam (30 mg) in a double‐blind, placebo‐controlled, ... differences were noted between estazolam 2 mg and flurazepam 30 mg on any of six sleep parameters. ... three active treatment groups; estazolam 2 mg and flurazepam also decreased sleep latency significantly. The percentage of ... who reported any adverse experience was 68% for flurazepam, 58% for estazolam 2 mg, and 54% for ...
Tópico(s): Epilepsy research and treatment
1991 - Wiley | The Journal of Clinical Pharmacology
Yuming Wu, Howard C. Rosenberg, Ted H. Chiu, Vicki Ramsey-Williams,
... BZ) receptors was studied in rats treated with flurazepam or diazepam protocols known to produce anticonvulsant tolerance. ... receptor population. Rats were treated 4 weeks with flurazepam, then sacrificed immediately or 48 hr later. After flurazepam treatment, the maximal binding capacity of [3H]zolpidem ... increased in the hippocampus. At 48 hr after flurazepam treatment, there was no significant difference in [3H] ... 3H]zolpidem binding. The data suggest that chronic flurazepam treatment causes downregulation primarily involving BZ1 receptors. The ...
Tópico(s): Memory and Neural Mechanisms
1994 - American Society for Pharmacology and Experimental Therapeutics | Journal of Pharmacology and Experimental Therapeutics
Tija C. Jacob, Guido Michels, Liliya Silayeva, Julia Haydon, Francesca Succol, Stephen J. Moss,
... approaches, we show that treatment with the BZ flurazepam decreases GABA A R surface levels and the ... GABA A Rs occurred within 24 h of flurazepam treatment, whereas GABA A Rs incorporating α1 subunits ... Coincident with decreased GABA A R surface levels, flurazepam treatment reduced miniature inhibitory postsynaptic current amplitude, which ... R endocytosis and insertion rates were unchanged by flurazepam treatment. Treatment with leupeptin restored flurazepam lowered receptor surface levels, strongly suggesting that flurazepam ...
Tópico(s): Photoreceptor and optogenetics research
2012 - National Academy of Sciences | Proceedings of the National Academy of Sciences
Elaine Woo, Susan M. Proulx, David J. Greenblatt,
... to receive either triazolam (0.125 mg) or flurazepam hydrochloride (15 mg) nightly under double‐blind conditions. ... on the tests, consistent with practice effects, whereas flurazepam recipients showed performance impairment during treatment. Triazolam—flurazepam differences were significant in the cardsorting and arithmetic ... ratings by physical therapists indicated significant impairment among flurazepam recipients in their capacity to cooperate with and ... persisted into the post‐treatment placebo period. Similar flurazepam—triazolam differences, although not significant, were reported by ...
Tópico(s): Sleep and Work-Related Fatigue
1991 - Wiley | The Journal of Clinical Pharmacology
D. J. McClure, Jared P. Walsh, Hye-Sook Chang, A. Oláh, R. J. Wilson, John C. Pecknold,
... doses of 2 mg lorazepam or 30 mg flurazepam were compared in a double‐blind cross‐over ... the study. Findings indicated lorazepam performed better than flurazepam in most sleep parameters. With lorazepam there was ... wake time from baseline improved (P < .05) with flurazepam (week 2). Objective and subjective sleep parameters did ... or vigilance test performance. Side effects (grogginess, lethargy; flurazepam only) were few and none was unexpected; neither ... summary, both lorazepam 2 mg at bedtime and flurazepam 30 mg at bedtime were found to be ...
Tópico(s): Sleep and Work-Related Fatigue
1988 - Wiley | The Journal of Clinical Pharmacology