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A study in mice of bromo and chloro acylurea analogues of the sedative-hypnotic bromureides.

1. A series of 1-(2-chloroacyl)ureas, related to the sedative-hypnotic drugs bromvaletone and carbromal, was synthesized and tested in mice to determine central depressant and acute toxic effects. Four 1-(2-bromoacyl)ureas and two 3-halo compounds were included for comparison. 2. Large variations in potency were seen between the compounds. Much of this can be ascribed to differences in lipophilicity. Among homologous 1-(2-chloroacyl)ureas, those with 6 acyl carbons had maximal potency. Among groups of structural isomers, the most potent were 2-halo, 3-alkyl substituted compounds. 3. The most potent compounds were also those with the largest ratios of hypnotic to lethal activity. 4. The variation in the onset and duration of action of these compounds enables a choice to be made for a compound with a particular set of characteristics.

Animals↗

PubMed1998

Decreased sensitivity to the hypnotic effects of ethanol early in ontogeny.

Sensitivity to the hypnotic effects of ethanol was examined in Sprague-Dawley male and female rats at 16, 26, 36, 46, 56, or 96 days postnatally. Following administration of 3.5, 4.0, 4.5, or 5.0 g/kg of a 17% v/v ethanol solution, sleep times were recorded and blood alcohol levels (BALs) and brain alcohol levels (BrALs) were measured upon awakening. In addition to examining ethanol sleep time during ontogeny, data were used to estimate acute tolerance (indexed by the slope of the linear regressions of waking BALs and BrALs as a function of dose) and initial brain sensitivity to ethanol (indexed by calculating the y-intercept from the linear regression of BrALs as a function of sleep time). The results showed a marked increase in sensitivity to ethanol hypnosis during ontogeny, with young animals exhibiting shorter ethanol-induced sleep times and high waking BALs and BrALs. This ontogenetic increase in ethanol sensitivity was associated with a developmental decline in acute tolerance, with acute tolerance being most pronounced at postnatal day (P) 16 and evident only up to P36. Initial sensitivity conversely increased with age, with P16 pups showing lower initial brain sensitivity to ethanol than at all other ages. Gender differences emerged in adulthood, with males sleeping significantly longer than females at P56 and P96. These findings suggest that the marked insensitivity of young animals to the hypnotic effects of ethanol is related to both pronounced acute tolerance, as well as reduced initial brain sensitivity to ethanol early in life.

Age Factors↗

PubMed1981

The interaction of age, performance and hypnotics in the sleep of insomniacs.

Scant attention has been paid to the objective evaluation of insomnia as a function of age, particularly with reference to increased drug sensitivity and resulting loss in balance performance. Therefore, the electroencephalographic sleep and the balance-board performance of 10 young and 12 geriatric insomniacs were studied under baseline and hypnotic drug (ketazolam) conditions. In terms of objectively measured sleep, the geriatric insomniacs had worse sleep on every dimension except sleep latency and percentage of stage-2 sleep. These differences between aged and young insomniacs, however, were no greater than might be expected as a function of normal aging. Drug-age interactions indicated that ketazolam differentially increased sleep efficiency, decreased the percentage of REM sleep, and eliminated any learning improvement on the balance board in geriatric versus young insomniacs. The findings indicate that the geriatric subjects were more sensitive to the hypnotic drug, in that their sleep improved to a greater extent. However, an important loss in balance performance was also observed.

Adult↗

PubMed2005

Claims data studies of sedative-hypnotics and hip fractures in older people: exploring residual confounding using survey information.

OBJECTIVES: To identify the magnitude of confounding bias caused by factors not measured in claims data studies of sedative-hypnotic use and fractures. DESIGN: Cross-sectional survey data. SETTING: Medicare Current Beneficiary Survey (MCBS). PARTICIPANTS: Eight thousand seven hundred eighty-five survey participants aged 65 and older. MEASUREMENTS: To determine the association between sedative-hypnotic use and potential confounding factors, five factors not measured in Medicare claims data but measured in the MCBS were assessed: body-mass index, smoking, activity of daily living (ADL) score, cognitive impairment, and Rosow-Breslau physical impairment scale. The association between benzodiazepine or zolpidem use and these five factors was estimated. Combined with literature estimates of the associations between confounders and fractures, it was possible to compute the extent of residual confounding bias caused by a failure to adjust for them. RESULTS: Comparing zolpidem users with nonusers, there was considerable overestimation of an association with hip fractures if ADL scores (21.5% bias) or Rosow-Breslau impairment scales (10.6%) were unobserved in claims data. All five unmeasured confounders together resulted in net confounding of 9.8% (range 0-39%). Comparing benzodiazepine users with nonusers, effect estimates were moderately biased (6.1%). After correction for this bias, the association observed in claims data (relative risk (RR)=1.38; 95% confidence interval (CI)=1.14-1.66) was comparable with that found in a recent study using clinical data (RR=1.20, 95% CI=0.72-2.00). In contrast to the clinical study, the claims data study achieved formal statistical significance because of its much larger size (288 vs 1,222 hip fractures). CONCLUSION: Claims data studies tend to overestimate the relationship between benzodiazepine use and hip fractures. After correcting for such bias, a statistically significant association persists. Concluding that there is no relationship at all based on small clinical studies that did not reach statistical significance may be misleading.

Activities of Daily Living↗

PubMed1986

Special problems relating to the use of hypnotics in the elderly.

The problems experienced by elderly patients taking hypnotic drugs are reviewed. They include those associated with accumulation, tolerance, drug dependence and the intensity and duration of response. Biological mechanisms associated with ageing enhance some of these effects in the elderly. Care should be taken to define the precise indications for hypnotic use and to choose the correct drug and dose for the patient's condition and age.

Aged↗

PubMed1987

Long-term prognosis in addiction on sedative and hypnotic drugs analyzed with the Cox regression model.

The prognosis of 221 patients first admitted in 1941-1954 for dependence on sedative-hypnotic drugs was determined in a record-linkage and interview study concluded in 1984. Different outcomes were related to admission characteristics by means of the Cox proportional hazards regression model. An excess of unnatural deaths was noted; suicides in 11% of the men and 23% of the women. Of those with primary sedative-hypnotic dependence, 46% continued to abuse drugs till death or follow-up, and of those with a primary or concomitant alcohol abuse 72%. An unfavorable outcome was significantly related to primary psychiatric symptoms before the first admission, concomitant alcohol abuse, familial drug and alcohol abuse and health care occupation.

Adult↗

PubMed1989

Explorative single-blind study on the sedative and hypnotic effects of buspirone in anxiety patients.

In this single-blind study the sedative and hypnotic properties of buspirone, a nonbenzodiazepine anxiolytic, were investigated in 8 anxious outpatients. Polysomnographic recordings were gathered during baseline, at the start of active medication, after 3 weeks of treatment and one night after discontinuing treatment. Daytime alertness was measured using the Multiple Sleep Latency Test and performance tests. The effects of buspirone on sleep structure were minimal and of no clinical consequence. Subjectively, the patients reported improved sleep quality. There were no effects on daytime alertness at the beginning, after 3 weeks or at sudden discontinuation of the medication. It is concluded that buspirone does not have a sedative or hypnotic effect in anxiety patients.

Adult↗

PubMed2002

A novel method to assess initial sensitivity and acute functional tolerance to hypnotic effects of ethanol.

Loss of righting reflex (LRR) has traditionally been used to estimate hypnotic sensitivity to ethanol in rodents. Traditional methods of monitoring ethanol-induced sedation seems to lack accuracy in estimating blood ethanol concentration (BEC) at initial LRR, a measure of initial sensitivity. Herein, we present a novel method that improves detection of the onset of LRR by using a new apparatus and a loss-of-function criterion of 5 s. DBA/2J and C57BL/6J mice were placed in cylindrical restrainers after injection of 3 g/kg (20% v/v) ethanol. Restrainers were then turned until mice were no longer able to right themselves within 5 s from a position on their back, which represented the endpoint of the initial loss of righting reflex. Initial sensitivity and acute functional tolerance (AFT) to ethanol were assessed in the same group of mice by quantifying BEC at the initial loss and subsequent recoveries of righting reflex over four sequential injections [3 g/kg + (3 x 0.5 g/kg)]. Initial brain sensitivity was calculated from BEC at the first LRR, using the parameters of ethanol uptake kinetics. These values of initial sensitivity were similar for the two strains. On the other hand, DBA/2J mice recovered at higher BEC than C57BL/6J animals. AFT calculated as a difference between the maximum BEC at any recovery and the value of initial sensitivity was greater in DBA/2J mice. These results show that the novel method is a sensitive tool for the measurement of initial sensitivity and detection of AFT to the hypnotic effects of ethanol.

Algorithms↗

PubMed1969

Nitrazepam--a safe hypnotic.

In 27 patients nitrazepam (Mogadon) taken in acute overdosage produced no untoward effects except drowsiness, even when 80 tablets were consumed. A double-blind trial in patients in general medical wards established that nitrazepam was as effective as butobarbitone as a hypnotic. It is concluded that nitrazepam is a safe and effective hypnotic.

Adult↗

PubMed2005

Sedative hypnotics in older people with insomnia: meta-analysis of risks and benefits.

OBJECTIVES: To quantify and compare potential benefits (subjective reports of sleep variables) and risks (adverse events and morning-after psychomotor impairment) of short term treatment with sedative hypnotics in older people with insomnia. DATA SOURCES: Medline, Embase, the Cochrane clinical trials database, PubMed, and PsychLit, 1966 to 2003; bibliographies of published reviews and meta-analyses; manufacturers of newer sedative hypnotics (zaleplon, zolpidem, zopiclone) regarding unpublished studies. SELECTION CRITERIA: Randomised controlled trials of any pharmacological treatment for insomnia for at least five consecutive nights in people aged 60 or over with insomnia and otherwise free of psychiatric or psychological disorders. RESULTS: 24 studies (involving 2417 participants) with extractable data met inclusion and exclusion criteria. Sleep quality improved (effect size 0.14, P < 0.05), total sleep time increased (mean 25.2 minutes, P < 0.001), and the number of night time awakenings decreased (0.63, P < 0.001) with sedative use compared with placebo. Adverse events were more common with sedatives than with placebo: adverse cognitive events were 4.78 times more common (95% confidence interval 1.47 to 15.47, P < 0.01); adverse psychomotor events were 2.61 times more common (1.12 to 6.09, P > 0.05), and reports of daytime fatigue were 3.82 times more common (1.88 to 7.80, P < 0.001) in people using any sedative compared with placebo. CONCLUSIONS: Improvements in sleep with sedative use are statistically significant, but the magnitude of effect is small. The increased risk of adverse events is statistically significant and potentially clinically relevant in older people at risk of falls and cognitive impairment. In people over 60, the benefits of these drugs may not justify the increased risk, particularly if the patient has additional risk factors for cognitive or psychomotor adverse events.

Cognition Disorders↗

PubMed1972

Changes in human drug metabolism after long-term exposure to hypnotics.

The influence of the newer, non-barbiturate hypnotics Mandrax (diphenhydramine-methaqualone) and nitrazepam on drug-metabolizing capacity was assessed and compared with the effect of amylobarbitone, a known inducer of drug-metabolizing enzymes. Plasma antipyrine and phenylbutazone half-lives and urinary output of 6beta-hydroxycortisol were used as indices. Volunteer subjects were exposed to therapeutic amounts of these agents and, in the case of Mandrax and barbiturates, further studies were carried out in dependent patients.Mandrax but not nitrazepam increased the rate of drug metabolism, presumably by enzyme induction. The degree of induction was comparable with that produced by hypnotic doses of amylobarbitone. The Mandrax-dependent and barbiturate-dependent patients were the fastest metabolizers studied. It is concluded that drug interactions resulting from interference with drug metabolism are as likely to occur with Mandrax as with barbiturates. On the other hand, it is unlikely that such drug interactions would occur with nitrazepam.

Adolescent↗

PubMed1983

Pharmacology of hypnotics.

Sedative hypnotics belong to several chemical classes and thus have heterogeneous pharmacodynamic properties. Among various ways of approaches, conventional pharmacology using animal models allows one to define a common pharmacological profile. It still remains the best predictive tool of hypnotic efficacy in man. The study of discriminative properties is a useful extension of these conventional models. Electrophysiological and biochemical studies allow primarily to approach the problems of the sites and mechanisms of action, but only begin at the moment to lead to practical applications.

Aggression↗

PubMed1987

Adverse reactions to benzodiazepine hypnotics: spontaneous reporting system.

The rates of reported adverse drug reactions involving the central nervous system were compared among patients taking any of three benzodiazepine hypnotics: flurazepam, temazepam, and triazolam. These rates, based upon data collected through the spontaneous reporting system of the Food and Drug Administration, were controlled for the number and size of new prescriptions for each drug. In general, triazolam had much higher overall rates than did the other two drugs. Hyperexcitability and withdrawal effects were greatest for triazolam and least for flurazepam. Amnesia was reported almost exclusively with triazolam. Rates for other cognitive as well as affective and other behavioral effects were also much greater for triazolam and about equal for the other two drugs. Finally, daytime sedation was reported slightly more for flurazepam than triazolam and least for temazepam which was also reported most frequently as lacking hypnotic effect.

Adult↗

PubMed1977

L-tryptophan: a rational hypnotic with clinical potential.

The author states that the use of the amino acid L-tryptophan as a hypnotic might avoid the problems of nonspecificity in the currently used CNS depressants because L-tryptophan is chosen on the basis of the chemistry of normal sleep rather than on a purely empirical basis. He reviews nine studies from his laboratory dealing with the effects of L-tryptophan on sleep. Studies in rats, normal human subjects, and subjects with mild insomnia all demonstrate that L-tryptophan reduces sleep latency. Polygraphic studies demonstrate that L-tryptophan, unlike hypnotics, does not produce distortions of sleep physiology when first administered, on long-term administration, or after withdrawal.

Animals↗

PubMed1980

Neuropsychological impairment and exclusive abuse of sedatives or hypnotics.

In a group of 55 consecutively admitted patients who exclusively abused sedatives or hypnotics, neuropsychological performance was significantly lower and signs of intellectual impairment significantly more often diagnosed than in a matched control group taken from the general population. These results suggest a relationship between abuse of sedatives or hypnotics and cerebral disorder.

Adult↗

PubMed1984

A 4-6-year follow-up of 50 patients with primary dependence on sedative and hypnotic drugs.

The authors studied 50 of 55 patients originally hospitalized for primary sedative-hypnotic dependence 4-6 years after hospital discharge. Forty-two (84%) of the patients had resumed using sedative-hypnotics, 26 (52%) were abusing drugs at follow-up, and 21 (42%) had been readmitted for drug abuse. Three patients experienced delirious states and six experienced epileptic seizures associated with withdrawal. Physical signs of alcoholism had developed in 11 (22%); four (8%) had committed suicide. Social deterioration was noted in 24 patients. CAT scan results did not deviate from those found in a matched control sample.

Alcoholism↗

PubMed1977

Comparative effectiveness of nine hypnotic drugs: sleep laboratory studies.

The effectiveness of nine hypnotic drugs was compared using a standard protocol in separate sleep laboratory drug evaluation studies. All of these drugs were relatively effective in improving sleep with initial and short-term use. However, with intermediate-term use (two weeks), most of the drugs showed a marked decrease in their effectiveness. Following withdrawal, sleep was similar to baseline with most of the drugs, continued to be improved with flurazepam (Dalmane), 30 mg, and worsened beyond baseline levels with triazolam (U33030), 0.5 mg. The determination of a drug's effectiveness with continued use is most important clinically in enabling the physician to rationally and effectively use hypnotic drugs in the adjunctive treatment of insomnia.

Adult↗

PubMed1977

Temazepam (Euhypnos) as a hypnotic: a multicentre trial in general practice.

In a one week study of 236 patients, soft gelatine capsules containing 10 mg temazepam (Euhypnos) were evaluated as a hypnotic in general practice. Doses of 10-30 mg were generally well tolerated and performed satisfactorily in 76% of the patients. Seventy-two per cent experienced no hangover effect and 72% rated Euhypnos as good as or better than their previous hypnotic drugs.

Adolescent↗