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PubMedDate not supplied

Conformational analysis and pharmacophore design for selected 1-(2-pyrimidinyl)piperazine derivatives with sedative-hypnotic activity.

The conformational of selected 1-(2-pyrimidinyl)piperazine derivatives with high sedative-hypnotic activity was analysed and the model bioactive conformations were suggested. Subsequently, the pharmacophores of analysed compounds were designed. It was suggested that the pharmacophore of bioactive derivatives should be composed of 11 features that characterise the binding model of pyrimidinylpiperazine ligands to the binding site at the hypothetic receptor. This 11 feature pharmacophore was compared to three other pharmacophores designed for the selected anxiolytics (benzodiazepines and buspirone analogues) and the sedative-hypnotic agents (benzodiazepines and barbiturates). Several substantial differences between the pharmacophores were found: the number of pharmacophoric features and their distribution in 3-D space were unique for selected groups of compounds that exhibit sedative-hypnotic or anxiolytic activity.

Hypnotics and Sedatives↗
PubMed2001

Choice of the hypnotic and the opioid for rapid-sequence induction.

The choice of hypnotics and opioids for rapid-sequence induction, and the use of premedication, is influenced by the choice of the muscle relaxant. Anaesthetic agents have a major influence on the quality of intubation when rapid-sequence induction is achieved without a muscle relaxant. Premedication is important, along with a high dose of propofol (2.5 mg kg-1 or more) and a short-acting opioid such as alfentanil (30-40 micrograms kg-1) or remifentanil (up to 4 micrograms kg-1). It has also been demonstrated that i.v. lidocaine can improve intubating conditions. When a muscle relaxant is used, the choice of the anaesthetic agents depends on the onset of action of the relaxant. With a rapid-acting compound such as rocuronium at a dose of 0.6 mg kg-1, the hypnotic agents need to be supplemented with only a small dose of opioids, e.g. alfentanil 10-20 micrograms kg-1. When succinylcholine, rocuronium 1.0 mg kg-1 or rapacuronium 1.5 mg kg-1 are used, excellent intubating conditions may be obtained by relatively smaller doses of hypnotic agents even without opioids; however, haemodynamic and intraocular pressure changes are better controlled when small doses of opioids are administered.

Analgesics, Opioid↗
PubMed2002

Actigraphic assessment of the preoperative hypnotic effects of brotizolam and zopiclone.

Brotizolam and zopiclone have a common ability to bind to the benzodiazepine recognition site and have been used as useful preoperative hypnotics. The aim of the present study was the quantitative evaluation of the preoperative hypnotic effects of brotizolam and zopiclone by actigraphy. Forty patients received brotizolam 0.25 mg (group B) or zopiclone 7.5 mg (group Z) in randomized manner at 21:30 on the night before surgery. Sleep and awake was identified by wrist activity measured with a motion-logger actigraph. Sleep time was assessed in total period from 22:00 to 6:00 and its 4 subdivided 2-hour periods (22:00-24:00, 24:00-2:00, 2:00-4:00, 4:00-6:00). The total sleep time in group B (448 +/- 23 min) was significantly longer than that in group Z (416 +/- 43 min). Group Z showed a significant reduction in sleep time in period 4 (4:00-6:00), compared with other periods, whereas group B did not show any difference among 4 periods. In comparison of each period between 2 groups, group B showed significant longer sleep time in period 4. An actigraphic assessment of sleep time has demonstrated the quantitative difference of the effects of brotizolam and zopiclone as preoperative hypnotics.

Adult↗
PubMed1992

Calcium channels are involved in the hypnotic-anesthetic action of dexmedetomidine in rats.

Our study examined whether calcium channels are involved in the anesthetic action of dexmedetomidine (100-300 micrograms/kg), a highly selective alpha 2-adrenoceptor agonist. To investigate this, we studied the effects of verapamil (1.25 or 2.5 mg/kg), a calcium channel blocker, and BAY K8644 (0.5 or 1 mg/kg), a calcium channel agonist, on the hypnotic-anesthetic effect of dexmedetomidine in rats. Loss of the righting reflex was used to determine the presence of anesthesia, and its length in minutes was referred to as the duration of hypnosis. Verapamil significantly enhanced the duration of the hypnotic-anesthetic action of dexmedetomidine (P less than 0.05). In contrast, BAY K8644 caused a significantly increased onset of hypnosis (P less than 0.001) and attenuated the anesthetic property of dexmedetomidine. These results suggest that the hypnotic-anesthetic action of dexmedetomidine is influenced by the activation/gating of calcium channels.

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy↗
PubMed2000

Cortical evoked response audiometry thresholds and neuroleptic, sedative, hypnotic drugs.

Cortical evoked response audiometry is adequate for approximating hearing threshold levels with frequency specificity when the psychoacoustic responses lack reliability and reproducibility (compensation claim). It is well-known that control of wakefulness is essential for the reliability of slow vertex responses (SVR). Therefore, sedative, hypnotic, and neuroleptic drugs are supposed to have possible adverse effects on the detection of SVR. In contrast, brainstem evoked responses (BER) have proved not to be significantly affected by therapeutic doses of these compounds. The purpose of our study was to assess the reliability of SVR-threshold definition in subjects taking neuroleptic, sedative, and hypnotic drugs. Fifteen subjects examined for occupational hearing loss at the Fund for Occupational Diseases in Brussels and regularly taking one or several of these drugs were compared with 27 comparable controls. In each subject the auditory thresholds were defined with both techniques: SVR (1, 2, and 3 kHz) and BER (clicks). A highly significant difference is observed between the two groups: In the group receiving drugs, the SVR threshold for 3 kHz is 12.1 dB (average) higher than the BER threshold, whereas in the group without drugs, the SVR threshold for 3 kHz is 7.77 dB (average) lower than the BER threshold. In the drug group, large interindividual differences are observed. It may be concluded that the use of neuroleptics, sedatives, and hypnotics renders the auditory threshold definition with SVR completely unreliable. In using SVR for medicolegal threshold definition, controlling the 3-kHz threshold with BER always is necessary.

Adult↗
PubMed2004

[Sleep disorders in elderly patients who take hypnotics on a regular basis].

BACKGROUND: Several studies have shown that the prevalence of sleep disorders such as sleep apnoea and periodic limb movements in sleep increases significantly with age. The assessment capacity is limited and there is a paucity of knowledge in this field among health professional, hence we hypothesise that these disorders are to a considerable extent under-diagnosed in the elderly, as the symptoms are often conceived of as insomnia. MATERIAL AND METHODS: Using ambulant clinical polysomnography, we investigated 19 patients aged 55 years or above who had been taking hypnotics on a daily basis (5 to 7 days a week) for at least one year. RESULTS: Among these 19 patients, the prevalence of sleep apnoea (AHI > 10) as well as periodic limb movements in sleep (PLM index > 10) was 42%; 74% had either sleep apnoea, periodic limb movements in sleep, or both. INTERPRETATION: Seen in relation to the fact that these elderly patients were given hypnotics for insomnia, the prevalence rates of sleep apnoea and periodic limb movements in sleep were high. We suggest that non-pharmacological alternatives should be considered and careful sleep assessment carried out before long-term prescription of hypnotics is instituted.

Aged↗
PubMed2006

[Are z-hypnotics better and safer sleeping pills than benzodiazepines?].

Benzodiazepines and the benzodiazepine-like z-hypnotics (zopiclone, zolpidem, and zaleplon) have the same mode of action and many of the same effects. The use of z-hypnotics has had a steady and large increase since their introduction in Norway, and sales data suggest extensive use among the elderly. The relatively short half-lives of these drugs may cause less hangover effects, but z-hypnotics are hardly more effective or safer than benzodiazepines. The two classes of drugs should be prescribed with similar caution.

Acetamides↗
PubMed2006

GPs' attitudes to benzodiazepine and 'Z-drug' prescribing: a barrier to implementation of evidence and guidance on hypnotics.

Zaleplon, zolpidem, and zopiclone ('Z-drugs') prescribing is gradually rising in the UK, while that of benzodiazepine hypnotics is falling. This situation is contrary to current evidence and guidance on hypnotic prescribing. The aim of this study was to determine and compare primary care physicians' perceptions of benefits and risks of benzodiazepine and Z-drug use, and physicians' prescribing behaviour in relation to hypnotics using a cross-sectional survey. In 2005 a self-administered postal questionnaire was sent to all GPs in West Lincolnshire Primary Care Trust. The questionnaire investigated perceptions of benefits and disadvantages of benzodiazepines and Z-drugs. Of the 107 questionnaires sent to GPs, 84 (78.5%) analysable responses were received. Responders believed that Z-drugs were more effective than benzodiazepines in terms of patients feeling rested on waking (P<0.001), daytime functioning (P<0.001), and total sleep time (P = 0.03). Z-drugs were also thought to be safer in terms of tolerance (P<0.001), addiction (P<0.001), dependence (P<0.001), daytime sleepiness (P<0.001), and road traffic accidents (P = 0.018), and were thought to be safer for older people (P<0.001). There were significant differences between GPs' perceptions of the relative benefits and risk of Z-drugs compared with benzodiazepines. The majority of practitioners attributed greater efficacy and lower side effects to Z-drugs. GPs' beliefs about effectiveness and safety are not determined by current evidence or national (NICE) guidance which may explain the increase in Z-drug prescribing relative to benzodiazepine prescribing.

Acetamides↗
PubMed1991

The nucleoside derivatives possessing sedative and hypnotic effects.

N3-Substituted oxopyrimidines and their related compounds were synthesized. The central nervous system (CNS) depressant activities of the compounds such as hypnotic activity and barbiturate-induced narcosis have been evaluated. N3-Benzyl, o,m,p-xylyl, alpha-phenylethyl, phenacyl substituted and related oxopyrimidine nucleosides exhibited potent hypnotic activity by intracerebroventricular (i.c.v.) administration to mice. The results indicate that hypnotic action of oxopyrimidine nucleoside derivatives might relate to functional group at the N3 position on oxopyrimidine ring and stereospecificity of sugar moiety.

Animals↗
PubMed1991

Sedative-hypnotic drug use in Canada.

Although many studies of sedative-hypnotic drug use have been performed in Canada, there has been no national study of the use of these drugs. We have attempted to correct this deficit in our knowledge by using data from an international survey of health care utilization performed in 1968-9 and from the Canada Health Survey (1978-9), the Health Promotion Survey (1985) and the National Alcohol and Other Drugs Survey (1989) to examine sedative-hypnotic use among individuals aged 15 or more. The results suggest that the use of these drugs in Canada is about average for an industrialized society. Several socioeconomic and health care correlates of sedative-hypnotic use were found. The rate of use of these drugs was higher among women, the elderly, separated, divorced or widowed individuals, those who had a secondary school education or less, individuals with a low family income, the retired, and the unemployed. Among women, higher rates of use were reported by those whose main activity was keeping house (as compared with those who were employed outside the home) and by those who lived alone. Higher rates of use were also found for individuals who had consulted a physician or been hospitalized recently, individuals taking multiple drugs, those who scored highly on an anxiety scale, persons in whom negative feelings predominated, and those who had experienced a high frequency of psycho-physiological symptoms of anxiety and depression. From a regional point of view, the highest rates of use for women were consistently reported from Quebec, while the lowest were consistently found in the Prairie provinces. No consistent pattern was found for men.

Adolescent↗
PubMed1976

[The effect of previous administration of adrenaline or isoprenaline on the activity of several hypnotics in mice].

Previous administration of adrenaline (0.5 mg/kg i.p.) and isoprenaline (10 mg/kg i.p.) enhances activity of several hypnotic drugs (pentobarbital, barbital, chloral hydrate) in mice but is without effect upon hypnotic activity of ethanol. This potentialisation is blocked by previous administration of pindolol, but not by phentolamine. Administration of SKF 525 A demonstrates that metabolism of pentobarbital is modified by this enzymatic inhibitor, which is not the case for other hypnotics.

Animals↗
PubMed1990

[Hypnotics and sleep].

An overview of substances with hypnotic properties and of genuine hypnotics is provided. Desired and undesired properties of benzodiazepine hypnotics are discussed. Although several endogenous sleep-promoting substances are being intensively investigated, their application in therapy is not yet in view.

Anti-Anxiety Agents↗
PubMed1991

The beneficial and adverse effects of hypnotics.

Findings from a four-city study of the beneficial and adverse effects of hypnotics are reported. The study employed a new volunteer call-in method for monitoring drug effects outside of the clinical setting. Respondents were recruited through newspaper advertisements. They were invited to complete a short telephone interview if, during the past 12 months, they (1) had significant trouble with insomnia or (2) had taken a medication to induce sleep. Comparison groups were flurazepam, temazepam, triazolam, and over-the-counter (OTC) sleep medications. An untreated insomnia group also was included. Results indicate that most users of prescription hypnotics attributed positive effects to their sleep medications and that adverse effects were infrequent. OTC hypnotics were less effective and more likely to produce negative effects. The untreated insomnia group was more symptomatic than any of the medication groups.

Adolescent↗
PubMed1990

Actions and interactions of hypnotics on human performance: single doses of zopiclone, triazolam and alcohol.

Actions and interactions with ethanol (0.8 g/kg) of triazolam (TRZ, 0.25 mg) and zopiclone (ZOP, 7.5 mg) on performance and memory were studied with 12 healthy young subjects. The randomized double-blind and crossover test sessions were carried out at 1-week intervals. Each time a set of performance tests and self-assessments on visual analogue scales were done before the treatment and 1.5, 3, 4.5, 6 and 8 h after it. The clinical test for drunkenness (CTD) was done 2 and 5 h after drug intake. Venous blood was sampled after each set of tests. Both TRZ and ZOP impaired coordinative and reactive skills, but not peripheral attention or body balance. They also impaired cognitive test performance (digit substitution, symbol copying), and lowered flicker fusion threshold. The psychomotor effects of the two hypnotics and measures of subjective sedation peaked at 1.5 and 3 h. Spatial memory was impaired by TRZ at 4.5 h. Cognitive tests and tracking were most sensitive to alcohol. Furthermore alcohol impaired both motor and vestibular aspects of the CTD while both ZOP and TRZ alone had only minor effects. Alcohol enhanced and prolonged the effects of both hypnotics without modifying their plasma concentrations. Drug-alcohol interactions were mainly additive though more obvious with TRZ. Interactions were evident also on the CTD. The hypnotics were free from residual psychomotor and cognitive effects at 8 h even after the coadministration of alcohol. It is concluded that ZOP and TRZ have a mainly additive interaction with alcohol but pharmacokinetic mechanisms do not seem to contribute essentially to this.

Adult↗
PubMed1977

Long term study of hypnotic medication in geriatric patients. A study of dixyrazine, nitrazepam and amylobarbitone.

The hypnotic effect of dixyrazine (a phenothiazine derivate), nitrazepam and amylobarbitone was studied during six months in 52 geriatric inpatients (17, 16 and 19 in each group, respectively) with a mean age of 78 years. The variables registered were the percentage of patients asleep at 10 pm and 6 am and the observed number of awakenings. Certain mental and somatic variables were rated according to a schedule for geriatric behaviour. The observations were made every two to three weeks. No systematic significant change with time was observed for any of the three drugs for the percentage of patients asleep at 10 pm or 6 am or for the number of awakenings. Nor was any difference found between the three drugs in respect of these variables. There was no significant change in somatic or mental variables according to the geriatric rating schedule. The results indicate that dixyrazine, nitrazepam and amylobarbitone retain their hypnotic effect in geriatric patients during continuous use for a six-month period. No side effects were observed that influenced the patient' behaviour. The results do not support the view that barbiturates, i.e. amylobarbitone are inappropriate as hypnotics in the elderly patient.

Aged↗
PubMed1985

Paradoxical excitement to sedative-hypnotics in mentally retarded clients.

The relationships among "paradoxical" excitement to sedative--hypnotic medication, self-injurious behavior, and perinatal trauma were evaluated. Mentally retarded patients were classified as either paradoxical or normal responders to sedative-hypnotics. Paradoxical responders to these medications have a lower MA, a history of perinatal trauma, self-injurious behavior (SIB), and aggressive behavior when compared to normal responders. These findings confirmed and extended previous reports that a type of SIB may be indexed by paradoxical response to sedative-hypnotics. Results also suggested that perinatal trauma may be of etiological importance in the development of SIB. Because perinatal trauma or fetal distress results in excessive levels of B-endorphin, in utero, an impaired endogenous opiate system may be a critical factor maintaining a syndrome of SIB. Thus, these data may indicate psychopharmacological markers of SIB that may have both treatment and etiological significance.

Adolescent↗
PubMed1984

Use of hypnotics in the elderly.

Nearly 40 percent of Americans complain about insomnia. Such complaints are even more common among the elderly, possibly because sleep efficiency decreases with age. As a result, the use of hypnotics in this age group is high--sometimes too high. Hypnotics can be addictive, and many have a low therapeutic index. The benzodiazepine agents are safest for use in the elderly. Many elderly patients exhibit a marked increase in sensitivity to these hypnotics.

Age Factors↗
PubMed1983

Hypnotic drug prescribing and consumption in a New Zealand teaching hospital.

The relationship between hypnotic drug choice and consumption was investigated with respect to eight variables for eight of the most commonly prescribed hypnotics in Wellington Hospital. The overall prescribing rate was 27% but the dispensing rate was 89.1%, attributable to the high incidence of PRN charting. Consumption of hypnotics increased with increasing patient age and duration of hospital stay. Consumption was higher for medical compared to surgical patients. Drug choice, ward preference and prescribing rate did not influence consumption, highlighting the fundamental discretionary role of the nurse-dispenser, determining the level of consumption.

Adolescent↗