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Biomedical subjects

B M Stone

Publications and source records attributed to B M Stone.

At least 55 records · Page 3Linked to original sources
PubMed1983

Imidazobenzodiazepines: sleep and performance studies in humans.

For hypnotics in which a fast elimination phase dominates the plasma decay, the initial fall in concentration from the peak value may nevertheless be slower than that of compounds with a sustained and rapid distribution. Drugs with fast elimination may therefore improve sleep throughout the rest period, even though residual sequelae, if any, around awakening will disappear rapidly. In the context of the balance between efficacy and residual effects, the activity of two imidazobenzodiazepines, loprazolam (0.5, 1.0, and 1.5 mg) and midazolam (10, 20, and 30 mg), each with fast elimination (about 6 and 2 hours, respectively) has been studied in healthy men with sleep electroencephalography, measures of performance, and assessments of mood. Loprazolam may be appropriate when a sustained hypnotic effect is required and when some residual activity is acceptable, while midazolam is likely to be suitable for those involved in skilled activity and may be useful in the management of sleep disturbance associated with shift work.

Adolescent↗
PubMed1982

6-(3-chloro)-phenoxy-2-methyl-1-oxa-4-azospiro-[4,5]decane-3-one (CERM 3726) and sleep of healthy men.

Immediate effects on sleep of 100, 200 and 300 mg 6-(3-chloro)-phenoxy-2-methyl-1-oxa-4-azospiro-[4,5]decane-3-one (CERM 3726) were studied in six healthy males. There was some sleep disturbance in two subjects with 100 and 200 mg, but only with 300 mg was there unequivocal evidence of reduced total sleep time and stage 2 sleep, together with a trend toward reduced rapid eye movement sleep. Arousal, at least as indicated by sleep studies, may be associated with the reported effect of the drug to oppose the deterioration in performance of tests of prolonged duration.

Adult↗
PubMed1982

Performance studies with the H1-histamine receptor antagonists, astemizole and terfenadine.

1 Effects of the antihistamines, terfenadine (60 mg) and astemizole (10 and 20 mg), on performance (visuo-motor coordination, arithmetical ability and digit symbol substitution) and on mood were studied in six healthy adult females. The study was double-blind, placebo controlled and included an antihistamine with known central effects (triprolidine 10 mg in sustained release form). 2 There were no changes in performance after terfenadine (60 mg) and astemizole (10 and 20 mg). Triprolidine (10 mg) caused a decrement in visuo-motor coordination (P less than 0.01) 0.5 h after ingestion which lasted until 3.5 h (P less than 0.001). The subject assessed their performance as impaired from 1.5-3.5 h (P less than 0.05) with triprolidine (10 mg), and their mood assessments were also altered. 3 Terfenadine (60 mg) and astemizole (10 and 20 mg) are likely to prove useful antihistamines for those involved in skilled activity.

Adult↗
PubMed1982

Hypnotic activity and effects on performance of lormetazepam and camazepam--analogues of temazepam.

1 The effects of lormetazepam and camazepam on sleep electroencephalography, visuo-motor coordination, digit symbol substitution and subjective assessments of mood and sleep quality were compared with placebo in six young adult males (18-27 years). The study was double blind. 2 Over the dose range 0.5, 1.0 and 2.0 mg, lormetazepam increased total sleep time (P less than 0.05), reduced wakefulness (P less than 0.05) and drowsy sleep (linear effect P less than 0.05). With 2.0 mg there were increases in stage 3 (P less than 0.05) and reduction in rapid eye movement sleep (P less than 0.01). Overnight ingestion of 2.0 mg, was followed by impaired visuo-motor coordination and fewer substitutions with the digit symbol test. 3 The hypnotic effect of 10-20 mg camazepam was limited to reduced awake activity (P less than 0.05), and with 20 mg there were increased substitutions on the digit symbol test. After 40 mg overnight stage 4 sleep was reduced (P less than 0.001) and performance at the digit symbol test was impaired (P less than 0.05 at 9.75 h). Morning ingestion of 20 mg camazepam did not alter performance, and the subjects assessed themselves to be more relaxed. 4 Lormetazepam is not specially indicated for those involved in skilled activity, but may prove useful for patients with insomnia resistant to other drugs. Camazepam would appear to be a promising anxiolytic with minimal effects on performance.

Adolescent↗
PubMed1982

Zopiclone: sleep and performance studies in healthy man.

Effects of 2.5, 5.0, 7.5, and 10.0 mg zopiclone on sleep and on performance the next day were studied in 6 healthy adult males aged between 21 and 33 years. The experiment was double-blind and placebo controlled. 5.0 and 10.0 mg zopiclone decreased the amount of awake activity and drowsy (stage 1) sleep over the first 6 h of sleep, but this effect was only present for the whole sleep period with the 10.0-mg dose. The duration and percentage of stage 3 sleep were increased with 7.5 mg. The 7.5- and 10.0-mg doses increased the combined duration of stages 2, 3, and 4 sleep over the first 6 h and over the whole night. The first period of rapid eye movement sleep was delayed with 7.5 mg, and with 10.0 mg the time spent in rapid eye movement sleep was reduced during the first 6 h of sleep, but not over the whole night. The number of substitutions in the digit symbol substitution test was decreased 9 h after ingestion of 7.5 and 10.0 mg, and the number of symbols copied reduced after 10.0 mg. The clinical dose range of zopiclone is likely to be up to 7.5 mg. The latter dose provides a useful hypnotic effect with minimal residual effects the next day, whilst 5.0 mg is appropriate for those involved in skilled tasks where even the most minor changes in performance during the early part of the next day must be avoided.

Adult↗
PubMed1980

Sleep and low doses of alcohol.

The effect of 3 doses of alcohol (0.16, 0.32 and 0.64 g/kg) on sleep was studied in 6 healthy young adults. Total sleep time was increased and awake activity was reduced by 0.16 g/kg. The sleep efficiency index was improved by 0.16 and 0.32 g/kg. All 3 doses reduced slow wave sleep, and this was related to the latter part of the night. There was some evidence that REM sleep was delayed, and the REM/NREM ratio reduced. Low doses of alcohol may partially improve sleep, but there are reductions in slow wave activity, and disturbances in REM sleep are likely above 0.32 g/kg.

Adult↗
PubMed1980

Studies on sleep and performance with a triazolo-1, 4-thienodiazepine (brotizolam).

1 Brotizolam, a triazolo-1,4-thienodiazepine, was studied in healthy young adults. Electroencephalographic sleep variables and subjective effects, and performance on a visuo-motor coordination task were measured. 2 In the sleep studies six males each ingested 0.2, 0.4 and 0.6 mg brotizolam overnight. All doses increased total sleep time, improved the sleep efficiency index, and reduced drowsy sleep and number of awakenings. Brotizolam 0.4 and 0.6 mg also reduced awake activity and increased stage 2 sleep. There was some evidence of a delay to the first REM period, but only 0.6 mg reduced the total duration of REM sleep. There were no changes in slow wave sleep. 3. In the performance studies six females each ingested 0.4 mg in the morning and 0.2, 0.4 and 0.6 mg brotizolam at night. After morning ingestion of 0.4 mg there was impaired performance from 0.5 to 5.5 h. There were no residual effects after 0.2 mg brotizolam, but with 0.4 mg there was a residual effect at 9.5 h, and 0.6 mg led to impairments up to 15.0 h after ingestion. 4 Brotizolam is a short-acting hypnotic. In doses around 0.2 mg it has useful hypnotic activity free of adverse effects on sleep and residual effects on performance. With 0.4 mg the hypnotic effect is enhanced with only minimal residual effects.

Adolescent↗
PubMed1980

Efficacy of some benzodiazepines for day-time sleep.

1 Effects of flunitrazepam (0.25-0.50 mg) and the 1,4-triazolodiazepines, triazolam (0.25-0.50 mg) and brotizolam (0.3-0.6 mg), on day time sleep were studied by electroencephalography. 2 Flunitrazepam (0.25-0.50 mg) and triazolam (0.25-0.50 mg) reduced awake activity (P < 0.05) and improved the sleep efficiency index (P < 0.05). The higher dose of each drug increased total sleep time (P < 0.05 and < 0.01 respectively) and duration of stage 2 sleep (P < 0.01), and also delayed the first REM period (P < 0.05 and < 0.01 respectively). 3 Brotizolam (0.6 mg) markedly increased total sleep time (P < 0.001) and the sleep efficiency index (P < 0.01), and prolonged stages 2 (P < 0.01 and slow wave (P < 0.01) sleep. Over the dose range 0.3-0.6 mg, the latency to stage 3 sleep was shortened (P < 0.05), and that to the first REM period lengthened (P < 0.05). 4 All three drugs improved day time sleep. However the present observations and data from previous studies suggest that flunitrazepam (0.25-0.50 mg) may be particularly appropriate for sleep at unusual times.

Adolescent↗
PubMed1980

Wakefullness and reduced rapid eye movement sleep: studies with prolintane and pemoline.

1 Effects of prolintane (15 and 30 mg) and pemoline (60 and 100 mg) on sleep were studied in six healthy adult males. Sleep was assessed by electroencephalography and by analogue scales. 2 Prolintane (15 and 30 mg) reduced rapid eye movement (REM) sleep both by delaying the first period (P < 0.05 and < 0.001 respectively) and by reducing total REM sleep (P < 0.05 and < 0.001 respectively). In some subjects there were increased awakenings during the early part of the night, and in two subjects long periods of wakefulness occurred. 3 With pemoline (60 and 100 mg) sleep duration was marked reduced (P < 0.001). There was evidence in some subjects of delay to the first REM period, and reduced percentage REM sleep (P < 0.01). Shortened and fragmented sleep with 60 and 100 mg were associated with reduced sleep efficiency indices (P < 0.001), and shorter sleep period times led to reduced REM/NREM ratios. Absence of an effect on REM latency for the subjects as a group may be related to relatively slow absorption. 4 The heterocyclic amphetamine derivatives have variable effects on sleep. The differences may be dose related, and wakefulness and reduced REM sleep may be seen together or separately. Alterations in sleep occur with doses of pemoline and prolintane which also modify performance.

Adult↗
PubMed1979

L-tryptophan and sleep in healthy man.

The effect of L-tryptophan on night-time and day-time sleep (from 14.00 h) sleep was studied in six healthy males aged between 20 and 30 years. The doses used in the night-time studies were 2, 4 and 6 g, and in the day-time studies 1, 2 and 4 g. It was not possible to establish an effect of L-tryptophan compared with placebo on night-time sleep, but analysis of the sleep measures with 4 g compared with placebo and the other doses of L-tryptophan considered together suggested reduced awakenings, increased stage 3 and an increased percentage of REM sleep. With 4 g L-tryptophan there was an increase in the duration of stage 3 of day-time sleep compared with placebo. The studies provide marginal evidence that REM sleep may be modified by L-tryptophan in man, though the evidence is somewhat stronger that SWS may be increased. The effect on REM sleep may involve circadian mechanisms. The hypnotic activity of L-tryptophan per se is limited and uncertain.

Adult↗