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PubMed1984

Stimulant and depressant properties of sedative-hypnotics in mice selectively bred for differential sensitivity to ethanol.

A genetic analysis of sedative-hypnotic response in selectively bred Long-Sleep (LS) and Short-Sleep (SS) mice showed LS mice to be more depressed by acetaldehyde, ethanol (ETOH), and t-butanol, but less sensitive to pentobarbital. Intermediate inheritance was shown by the two reciprocal F1 hybrids for the alcohols, but dominance to the LS genotype occurred for the aldehyde and the barbiturate. At several subhypnotic doses of ETOH in two experiments, LS mice showed less locomotor stimulation and greater disruption of coordination than the SS mice. The two reciprocal F1 hybrids did not differ from one another and had dose-response curves intermediate to the two parental lines. Study of the effects of t-butanol on locomotor activity revealed a pattern of line differences similar to that for ETOH. The genetic selection for LS and SS mice appears to have differentiated loci that pleiotropically influence a variety of behavioral responses to alcohols.

Analysis of Variance↗
PubMed1978

Model insomnia, noise, and methylphenidate, used for the evaluation of hypnotic drugs.

Experimental sleep disturbance (model insomnia) was produced by intermittent white noise and the administration of 10 mg of methylphenidate (MPD). The effects of flurazepam (FZP) 15 mg and triazolam (TZM) 0.25 mg on these models was investigated. All night sleep polygraphy was performed on 8 normal male subjects under each of the following 9 conditions: baseline, TZM 0.25 mg, FZP 15 mg, white noise alone, noise and TZM, noise and FZP, MPD alone, MPD and TZM, and MPD and FZP. A reduction in total sleep time and stage were (S-REM) and an increase in the wakening stage were observed with both noise and MPD. Stage 4 sleep was reduced only by MPD. Administration of TZM or EZP did not cause any significant change in sleep parameters. These drugs in combination with noise or MPD resulted in almost complete recovery of the sleep disturbance induced by noise or MPD, except for a reduction in S-REM. These results indicate that model insomnia, particularly MPD insomnia, will assist in the evaluation of hypnotic drugs.

Adult↗
PubMed1984

Effects of some volatile sedative-hypnotics on punished behavior.

Lever-press responses of rats were established under a schedule in which punished and unpunished responding alternated. Every 30th response produced food (unpunished responding) during an alternate schedule component, while every tenth response produced both food and shock (punished responding) during an alternate schedule component. Each schedule component was correlated with a different visual stimulus. Unpunished behavior was characterized by high sustained rates which followed brief pauses after food delivery. Punished behavior occurred at less than 10% the rate of unpunished behavior. Oral administration of diazepam, ethchlorvynol, chloral hydrate, tertiary-butanol, and ethanol all produced marked dose-related increases in punished behavior at doses that decreased or had little effect on unpunished responding. Potency estimates for increasing punished responding varied over a 400-fold range. The potency ranking was diazepam greater than ethchlorvynol greater than chloral hydrate greater than tertiary-butanol greater than ethanol. Higher doses of all drugs decreased unpunished responding with relative potencies comparable to those found for doses producing maximal increases in punished responding. Increases in punished behavior appear to be a characteristic feature of drugs with sedative-hypnotic properties.

Animals↗
PubMedDate not supplied

Effect of hypnotic and anxiolytic agents on regional concentration of acetylcholine in rat brain.

Pentobarbital (30 and 60 mg/kg) and chloral hydrate (300 and 600 mg/kg) administered in anesthetic/hypnotic doses produced significant increases in acetylcholine concentration in the cerebral cortex, striatum, hippocampus and brainstem. Hypnotic/anxiolytic agents like diazepam, flurazepam (100 mg/kg each) and triazolam (30 mg/kg) significantly increased the acetylcholine concentration only in the cerebral cortex and striatum. Alprazolam and ketazolam had no significant effect on regional distribution of acetylcholine in the brain. The results have been discussed with respect to the role of central cholinergic system in anesthetic and hypnotic actions of these drugs.

Acetylcholine↗
PubMed1980

Comparative study of zopiclone, a novel hypnotic, and three benzodiazepines.

The hypnotic effect and tolerance of zopiclone 7.5 mg, nitrazepam 5 mg, flurazepam 30 mg, flunitrazepam 2 mg and placebo were compared in a one-night double blind study in 414 hospitalised patients who were to undergo an operation on the following day. Zopiclone was slightly superior to nitrazepam but was inferior both to flurazepam and flunitrazepam. All the active drugs differed clearly from placebo. The results from a subset of patients, excluding those who felt anxious either before treatment on the evening prior to the operation or on the following morning, were analysed separately. All the active products differed significantly from placebo; zopiclone was slightly less effective than the three benzodiazepines. All the benzodiazepines decreased the percentage of patients feeling anxious about the operation by about 25%, zopiclone by about 10% and placebo did not change it at all.

Adult↗
PubMed1989

Involvement of noradrenergic system in a remarkably rapid tongue clonus produced by acute hypnotic doses of ethanol in Fischer F344 rats.

Ethanol (2.95 g/kg, IP) eliminated the righting reflex and induced vigorous tongue clonus spontaneously or following tactile tongue stimulation in Fischer F344 rats. Responses normally lasted 30-60 min, and was reinstated by tactile stimulation in those cases where it subsided quickly. Sub-hypnotic (1.95 g/kg) or high (3.95 g/kg) doses failed to elicit clonus, even after tactile stimulation. A lipophilic alpha 1-adrenergic agonist (St 587) promptly initiated tongue clonus in rats treated with a 3.95 g/kg dose of ethanol. Prazosin, a selective alpha 1-adrenergic antagonist, blocked clonus, while the dopamine selective antagonist pimozide failed to modify this response. We infer an alpha 1-adrenergic effect in which norepinephrine is released by ethanol.

Animals↗
PubMed1987

Comparison of the clinical hypnotic effects of zopiclone and triazolam.

In a double blind crossover therapeutic trial the hypnotic effect of Zopiclone 7.5 mg and Triazolam 0.5 mg given orally at bedtime for 7 consecutive days have been compared. 5 of the items in Spiegel's questionnaire and 12 of the 18 items in Norris' visual analogue scale were significantly more improved by Zopiclone than by Triazolam. Both drugs caused few side-effects.

Adult↗
PubMed1983

Comparison of quazepam, flunitrazepam and placebo as single-dose hypnotics before surgery.

The hypnotic effect and tolerance of quazepam (Sch 16134) 15 and 30 mg, flunitrazepam 1 and 2 mg and placebo were evaluated in a one-night, randomized, double-blind, parallel group study of 100 hospitalized patients, who were to undergo a planned operation on the following day. All active drugs were rated as superior to placebo by the physician. Subjectively, quazepam 30 mg and flunitrazepam 1 and 2 mg were superior to placebo. Hangover effects were not distinguishable from placebo. Vigilance and ataxia tests were not altered by any of the drugs.

Adolescent↗
PubMed1990

Sleep laboratory investigations on hypnotic properties of melatonin.

Melatonin (MLT), a pineal hormone, has some sedative and hypnotic properties. To explore this effect further 20 young, healthy volunteers exposed to artificial insomnia participated in a double-blind, placebo controlled, parallel group design study. They slept in a sleep laboratory for several consecutive nights and were polygraphically monitored and subjected to a battery of psychometric tests and standardized self-report questionnaires each morning. One night all subjects received only placebo (21:00 hours) and on a second night half of them were subjected to placebo and half to MLT. On the later night blood MLT levels were measured. Polygraphic recordings revealed that MLT at bedtime decreased the time the subjects were awake before sleep onset (P less than 0.025), sleep latency (P less than 0.05), and the number of awakenings during the total sleep period (P less than 0.025), and increased sleep efficiency (P less than 0.05). In addition, it decreased sleep stage 1 (P less than 0.05) and increased sleep stage 2 (P less than 0.025). On the morning following the treatment most objective and subjective measures for awakening quality showed a trend towards improvement after MLT. One hour after its oral administration, serum MLT rose to a high pharmacological level (25817 pg/ml; median), but individual peak serum MLT levels varied by a factor of 300.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1993

Testing the effects of hypnotics on memory via the telephone: fact or fiction?

The two benzodiazapines used in this experiment, namely midazolam and flunitrazepam, have both been shown to have effects on memory processing in laboratory studies. In spite of the potential hazards involved in real life testing, it should be possible to replicate such findings in everyday environments and it is argued that a successful replication would be a very meaningful extension to the existing laboratory data. The present study was successful in producing significant "hangover" effects in healthy volunteers using a novel "user-friendly" telephone testing technique. Compared to placebo, the two hypnotics reduced speed of processing in tasks which required retrieval from long-term semantic memory (semantic verification) and the manipulation of material in working memory (syntactic reasoning). We suggest that this new method offers the potential for carrying out large-scale psychopharmacological studies with real patients and achieves a meaningful step forward in the search for ecological validity.

Adult↗
PubMed1996

Hypnotic self administration and dose escalation.

The dependence liability of benzodiazepines in the context of their use as hypnotics (i.e. by insomnia patients as pre-sleep medications) is unresolved. A recent study found that insomniacs self administer capsules at bedtime at a high rate, with triazolam (0.25 mg) taken as often as placebo. This study sought to determine if differential self administration would develop when multiple capsules are available nightly. Eighteen men and women, age 21-45 years, with insomnia complaints (nine with objective sleep disturbance and nine without) were studied, 1 week with placebo and 1 week with triazolam (0.25 mg). The two conditions were administered double-blind and presented in a counter-balanced order with a week between conditions. In each condition, after 3 consecutive sampling nights of the available single capsule for that condition, subjects could self administer 0-3 capsules before bed on the 4 subsequent nights. Triazolam was self administered as many nights as placebo, but the number of placebo capsules self administered was twice that of triazolam capsules. The objective insomniacs self administered more capsules than the subjective insomniacs and neither group differentially choose triazolam over placebo. The number of triazolam capsules taken nightly was stable and the number of placebo capsules variable. It is concluded that insomniacs show no short-term escalation of triazolam dose, but do choose an increased and variable number of placebos, a pattern which is interpreted as being insomnia relief-seeking behavior.

Adult↗
PubMed2001

Hypnotic and cardiovascular effects of proprietary and generic propofol formulations do not differ.

PURPOSE: The aim of the study was to compare the potency of two different propofol formulations: proprietary and generic propofol using the bispectral index (BIS) monitoring. METHODS: Forty female patients undergoing breast surgery received propofol 3 mg x kg(-1) followed by propofol infusion adjusted to maintain a 40% BIS value, supplemented by 50% nitrous oxide. Proprietary or generic propofol was administered in a randomized double-blind manner. RESULTS: The propofol mg/BIS% ratio obtained after the bolus dose, the cumulative infused propofol mg/BIS% ratio at the end of each five-minute interval and the total dose of propofol administered as bolus + infusion were similar between the two groups. The two groups did not differ with regard to systolic and diastolic blood pressure, heart rate, end-tidal carbon dioxide and arterial oxygen saturation. CONCLUSION: The two propofol formulations are equipotent when hypnotic effect is assessed by BIS monitoring.

Adult↗
PubMed1997

Influence of zopiclone, a new generation hypnotic, on the intermediate stage and paradoxical sleep in the rat.

This study examined the influence of zopiclone, a third generation hypnotic, on the transition from slow wave sleep to paradoxical sleep (PS) which is increased at the expense of PS by barbiturates and benzodiazepines. The compound decreased sleep latency and increased the latency of the intermediate stage (IS) and PS at 2.5, 5 and 7.5 mg/kg IP. The amount of the IS was decreased because of the decrease in phase number up to 6 h at all doses. PS amount was decreased during 2 h at 2.5 mg/kg and during 4 h at 5 and 7.5 mg/kg also because of the decrease in phase number. The IS never substituted for PS. The IS spindle characteristics were not modified and the theta rhythm frequency slightly decreased at 5 mg/kg (IS) and 7.5 mg/kg (PS).

Animals↗
PubMed1997

Hypnotic self administration: forced-choice versus single-choice.

Twenty-four men and women with insomnia, age 21-50 years, self administered hypnotics under a single-choice with placebo, single-choice with triazolam (0.25 mg), or forced-choice of placebo versus triazolam (0.25 mg) paradigm. Subjects received 4- sampling nights of placebo or triazolam in the single-choice conditions or 2 nights of each in the forced-choice condition. Then on 7 choice nights they could self administer a capsule, or not, in the single-choice conditions, or were required to choose one of two color-coded capsules in the forced-choice condition. In the single-choice conditions, subjects chose placebo 80% of nights and triazolam 77% of nights, while in the forced-choice condition triazolam was chosen on 86% of nights. Thus, the self administration of triazolam did not vary significantly between single or forced choice conditions, but that of placebo did. Placebo rate was high when it was the only alternative, but low when competing with triazolam. On sampling nights, compared to placebo, triazolam produced a significant increase in total sleep time, a reduction in latency to sleep, wake after sleep onset, and percentage stage 1 sleep. Triazolam, relative to placebo, also improved mood in the morning on some sampling nights. For subjects choosing capsules < 100% of opportunities (n = 14), on nights a capsule was chosen versus nights none was chosen (regardless of whether placebo or triazolam was the choice), self-ratings 30 min before bedtime on the Profile of Mood States vigor scale were significantly higher.

Adult↗
PubMed2006

Interaction between grapefruit juice and hypnotic drugs: comparison of triazolam and quazepam.

OBJECTIVE: Grapefruit juice (GFJ) inhibits cytochrome P450 (CYP) 3A4 in the gut wall and increases blood concentrations of CYP3A4 substrates by the enhancement of oral bioavailability. The effects of GFJ on two benzodiazepine hypnotics, triazolam (metabolized by CYP3A4) and quazepam (metabolized by CYP3A4 and CYP2C9), were determined in this study. METHODS: The study consisted of four separate trials in which nine healthy subjects were administered 0.25 mg triazolam or 15 mg quazepam, with or without GFJ. Each trial was performed using an open, randomized, cross-over design with an interval of more than 2 weeks between trials. Blood samples were obtained during the 24-h period immediately following the administration of each dose. Pharmacodynamic effects were determined by the digit symbol substitution test (DSST) and utilizing a visual analog scale. RESULTS: GFJ increased the plasma concentrations of both triazolam and quazepam and of the active metabolite of quazepam, 2-oxoquazepam. The area under the curve (AUC)(0-24) of triazolam significantly increased by 96% (p<0.05). The AUC(0-24) of quazepam (+38%) and 2-oxoquazepam (+28%) also increased; however, these increases were not significantly different from those of triazolam. GFJ deteriorated the performance of the subjects in the DSST after the triazolam dose (-11 digits at 2 h after the dose, p<0.05), but not after the quazepam dose. Triazolam and quazepam produced similar sedative-like effects, none of which were enhanced by GFJ. CONCLUSION: These results suggest that the effects of GFJ on the pharmacodynamics of triazolam are greater than those on quazepam. These GFJ-related different effects are partly explained by the fact that triazolam is presystemically metabolized by CYP3A4, while quazepam is presystemically metabolized by CYP3A4 and CYP2C9.

Adult↗
PubMed1998

Development of congenics for hypnotic sensitivity to ethanol by QTL-marker-assisted counter selection.

Mouse strains congenic for individual quantitative trait loci (QTLs) conferring hypnotic sensitivity to ethanol were constructed by backcrossing genotypically selected ILS x ISS N2 individuals to either inbred Long Sleep (ILS) or inbred Short Sleep (ISS) mice. We used a novel "speed congenic" approach in which N2 mice were genotyped for markers flanking each of the five originally identified QTLs. Genotypic selection for ISS regions at four of the five QTLs, and for ILS/ISS at the fifth QTL, allowed rapid fixation of the genetic background. We call this strategy "QTL-Marker-Assisted Counter Selection" or QMACS. By the N4 generation, phenotypic assessments showed that in some sublines the QTL had not been captured; these sublines were discarded and positive lines split to create new replicate sublines. One QTL, on Chromosome (Chr) 8, was not confirmed. At the N8, virtually all sublines on the remaining QTLs retained the phenotypic difference between heterozygotes and ISS homozygotes. Small numbers of interim congenics were produced at the N6 and later generations in which the ILS QTL was made homozygous on the ISS background; as expected, these congenic mice showed an increased sleep time. For later backcrosses (after the N4), the parents were selected on the basis of phenotype as well as genotype. The parent-offspring correlation over all QTLs was significant, supporting the use of phenotypic selection in congenic construction.

Animals↗
PubMed2002

[Benzodiazepines and benzodiazepine-like anxiolytics and hypnotics. The implausible contraindication of closed angle glaucoma].

Official drug information materials mention angle-closure glaucoma as an absolute or relative contraindication for benzodiazepines, albeit with some unexplained variability. A systematic review of the literature reveals that this contraindication seems to be based on only one published case while 22 other investigations, some of them controlled, tend to favor that benzodiazepines reduce intraocular pressure. The common 1990-2001 database of the Drug Commission of the German Medical Profession and the Federal Institute for Drugs and Medical Devices contained one spontaneous report of glaucoma related to a benzodiazepine-like hypnotic.

Anti-Anxiety Agents↗
PubMed1991

The hypnotics triazolam and zolpidem have identical metabolic effects throughout the brain: implications for benzodiazepine receptor subtypes.

Using Sokoloff's 2-deoxyglucose autoradiography procedure, the effects of trizolam, a classical benzodiazepine (BZ) hypnotic, were compared to those of zolpidem, which preferentially binds to BZ1 receptor subtypes. Triazolam depressed metabolism in 40 of the more than 60 brain regions evaluated. Zolpidem depressed metabolism in all of these areas, including the spinal cord, an area where the BZ1 receptor subtype is not supposed to exist. Zolpidem and triazolam also depressed metabolism in the molecular layer of the dentate gyrus, an area low in BZ1 receptors. Neither drug affected metabolism in 21 areas, including the regions most specific for the BZ1 subtype (cerebellum, inferior colliculus, globus pallidus, and substantia nigra pars reticularis). It is concluded that: (i) zolpidem and triazolam depress energy metabolism of the same areas of the brain, (ii) zolpidem's effects may not be mediated solely through the BZ1 receptor subtype, and (iii) the BZ2 receptor may be functionally more significant than the BZ1 receptor.

Animals↗