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At least 19 recordsLinked to original sources
PubMed1976

Is the use of hypnotics, sedatives and minor tranquilizers really a major health problem?

An analysis has been made of individual purchases of hypnotics, sedatives and minor tranquilizers made during 1973 by patients who had bought such drugs either only once (group S, n= 417) or regularly (group R, n=76) during a 16-month period five years earlier from pharmacies in the town of Ostersund, county of Jmtland, Sweden. By 1973, 17% of the patients in each group had either died or moved out of the country and were therefore excluded from the comparison. In group S, 81 patients (23%) bought the above drugs once or more in 1973, while the corresponding figure for group R was 55 (87%). Compared with 1968-69, there was a decrease in the number of prescriptions and also in the number of tablets obtained per individual. Furthermore, the number of tablets per prescription was lower in 1973. Among the drugs prescribed, benzodiazepines dominated during both periods, followed by barbiturates. In 1973 there was a substantial increase in the use of nitrazepam, mostly at the expense of diazepam and combined products. One patient in group S and one in group R showed a tendency to decrease the interval between purchases. The latter was already known to be a drug abuser five years earlier. Without knowing the reason why the drugs were prescribed and to what extent they were actually taken, it is impossible to say whether the other patient should be classified as drug abuser or not. Although the number of patients in this study is limited, it might be concluded that the risk of an occasional user of hypnotics, sedatives and minor tranquilizers living in this area becoming an abuser of such drugs within a five-year period is less than 1/345.

Adolescent↗
PubMedDate not supplied

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↗
PubMed1975

Sedative-hypnotic properties of a new benzodiazepine in comparison with flurazepam. Pharmacological and clinical findings.

The sedative-hypnotic effects of a new benzodiazepine, 1-(2-hydroxyethyl)-3-hydroxy-7-chloro-1,3-dihydro-5-(o-fluorophenyl)-2H-1,4-benzodiazepin-2-one (SAS 643), were compared with those of flurazepam in mice and rats as well as in a double-blind clinical trial. It was found that SAS 643 has a potency 2--4 times greater than that of flurazepam while it is about one half less toxic than the latter drug. The results of the clinical trial confirm the greater activity of SAS 643 and indicate that the new benzodiazepine causes a significantly less amount of hangover than flurazepam.

Aged↗
PubMed1979

Pharmacological properties of taglutimide, a new sedative-hypnotic drug.

2-[Bicyclo(2,2,1)heptane-2-endo-3-endo-dicarboximido]-glutarimide (taglutimide, K-2004) proved to be a new sedative-hypnotic drug which did not produce any toxic effects when administered orally to mice even at a very high dosage. Central-nervous depression was demonstrated by a reduction in spontaneous motor activity, potentiation of the central-depressant effect of pentobarbital, antagonism of the central-stimulant effect of amphetamine after oral administration and by narcotic activity after i.v. administration of the drug. Furthermore, oral administration of taglutimide potentiated the analgesic action of morphine without being effective on its own. Only weak potentiation of chlorpromazine-induced catalepsy, but not of reserpine-induced catalepsy was observed after taglutimide pretreatment. The drug influenced neither motor co-ordination nor the toxicity of ethanol. Taglutimide exhibited no anticonvulsant activity with respect to maximum electroshock or strychnine-induced seizures. No effect on heart rate or blood pressure was demonstrable after taglutimide treatment in conscious dogs.

Animals↗
PubMed1978

Comparison of oxazepam, flurazepam and chloral hydrate as hypnotic sedatives in geriatric patients.

In a four-week study, a comparison was made of oxazepam, flurazepam and chloral hydrate as hypnotic sedatives in 17 geriatric patients. Each drug was given alone for six nights, with a two-night placebo interval following each phase. Each patient completed an additional placebo phase (up to six nights) before each drug phase. The number of awakenings per night and the sleep latency (time required to fall asleep) were determined from the patients' reports and from the reports of a nurse-observer. Only for oxazepam was the number of patient-reported awakenings per night significantly less than for placebo, although with both oxazepam and flurazepam the awakenings were fewer than with chloral hydrate. According to the patient-reports, sleep latency was significantly lower with flurazepam than with placebo; for oxazepam and chloral hydrate the latencies were not significantly different from those for flurazepam or placebo. Only for oxazepam were the patients' ratings of sleep quality significantly greater than for placebo. The objective assessment of sleep by the nurse-observer usually confirmed the patients' assessments. Morning drowsiness was the most common side effect, reported equally for placebo and for the active drugs. Drowsiness during the day was reported less frequently for oxazepam than for flurazepam, chloral hydrate or placebo. It is concluded that oxazepam is safe and efficacious for the short-term management of insomnia in the elderly.

Aged↗
PubMed1975

Synthesis of an active hydroxylated glutethimide metabolite and some related analogs with sedative-hypnotic and anticonvulsant properties.

Two synthetic pathways are described for the preparation of 4-hydroxy-2-ethyl-2-phenylglutarimide (2), an active hydroxylated metabolite of glutethimide (1). Fourteen other glutethimide analogs were also synthesized and tested for biological activity. Most of the analogs exhibited sedative-hypnotic properties and compound 2 possessed the greatest activity compared to the parent drug. 4-Amino-2-ethyl-2-phenylglutarimide and 4-hydroxy-2-ethyl-2-phenylglutaconimide (13) exhibited the greatest potential as anticonvulsant agents. The structure-activity relationships of the series are discussed.

Animals↗
PubMed1978

[X-ray examination of the abdomen in hypnotic-sedative drug poisoning--casuistical contribution (author's transl)].

By means of an impressive example the significance of abdominal X-ray examination in cases of intoxication with hypnotic-sedative drugs is pointed out. Apart from the qualitative diagnosis (drug containing bromide) the radiological proof of shadow-giving substances also permits a quantitative clinical assessment and has prognostical as well as therapeutical consequences.

Adult↗
PubMed1979

Barbitone-induced tolerance to the effects of sedative-hypnotics and related compounds on operant behaviour in the rat.

1 Pretreatment doses of barbitone, pentobarbitone, ethanol, and phenytoin (diphenylhydantoin) in non-tolerant rats produced increases in operant responding at low doses and at higher doses resulted in decreases in responding.2 Daily barbitone injections (100 mg/kg, i.p.) resulted in the development of functional tolerance to both the stimulant and depressant effects of barbitone on responding.3 Barbitone tolerance development did not result in any change in the brain or plasma pharmacokinetics of barbitone.4 Barbitone-tolerant rats were cross-tolerant to the behavioural effects of pentobarbitone, ethanol, and phenytoin. The dose-effect curves for all of these drugs were shifted to the right in tolerant rats, compared to non-tolerant rats.5 Comparison of the brain and plasma levels of these drugs in non-tolerant and tolerant rats provided a means of separating functional cross-tolerance from dispositional cross-tolerance. Barbitone-tolerant rats appeared to be functionally cross-tolerant to ethanol in that there was no change in the brain and blood ethanol levels at times when the degree of behavioural impairment was substantially reduced. In contrast to ethanol, cross-tolerance to phenytoin appeared to be due to a decrease in the brain and plasma levels (dispositional tolerance). Cross-tolerance to pentobarbitone appeared to be comprised of both functional and dispositional cross-tolerance.6 The usefulness of a multidisciplinary approach in the analysis of sedative hypnotic tolerance and cross-tolerance is discussed. It is concluded that without the concurrent determination of both brain and plasma drug levels it would not be possible to distinguish between functional and dispositional tolerance.

Animals↗
PubMed1978

Relationship between locus of control and drug effects in users of narcotics, stimulants, hypnotic-sedatives, and hallucinogens.

A test is made of the hypothesis that the subjective effects of narcotics lead to an internal locus of control orientation. No support is evident. Similar findings are given for users of stimulants. As an aside to the major focus of the study, a test of locus of control differences between users of narcotics, stimulants, hypnotic-sedatives, and hallucinogens is given, with no differences being found.

Amphetamines↗
PubMed1977

Purchases of hypnotics, sedatives and minor tranquillizers among 2,566 individuals in the county of Jämtland, Sweden. A 6-year follow-up.

Data from a continuous recording of drug prescriptions to 16,600 individuals in the county of Jämtland, Sweden, revealed that 2,566 patients (15.5%) obtained prescriptions for hypnotics, sedatives and minor tranquillizers in 1970. Occasional use (one purchase only, Group A) was seen in 7.4% of the population, intermediate use (two to six purchases, Group B) in 6.9% whereas 1.2% were regular users (seven purchases or more, Group C). For each group as a whole there was 5 years later a highly significant intraindividual reduction in the purchases of these drugs as well as of other psychotropic drugs. In all groups 10-23% had increased their purchases, most of them insignificantly. Fifteen of 30 patients with a marked increase in consumption developed a regular purchase pattern, but signs of overuse or abuse were seen in only four persons. During the studied period the benzodiazepines increased their share of the total from 45 to 60%. Antihistamines also increased in all groups while the proportion of barbiturates and combined preparations decreased markedly.

Anti-Anxiety Agents↗
PubMedDate not supplied

Comparison of the bromureide sedative-hypnotic drugs, bromvaletone (bromisoval) and carbromal, and their chloro analogues in mice.

1. The central depressant effects of bromvaletone, carbromal and six non-bromo analogues were compared in mice. 2. The chloro analogues of bromvaletone and carbromal were slightly less potent as central depressant agents than the bromo compounds. 3. The chloro analogue of bromvaletone had the greatest margin between central depressant and lethal doses. 4. Lipophilicity (octanol-water partition coefficient) did not provide a unifying relationship for potency within this group of eight acylureas. However, within each of the two subsets of compounds, a linear relationship was found between relative potency and lipophilicity.

Animals↗