Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0917801 (insomnia)
 10,606 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Quazepam and flurazepam share pharmacokinetic properties that result in prevention of early-morning insomnia, daytime rebound anxiety, and withdrawal rebound insomnia. Yet sleep laboratory and performance studies demonstrated that during a 1- to 4-week administration period quazepam had a low potential for causing daytime drowsiness or impairment. This profile may be related to several factors, such as differences in quazepam's metabolic pathways; plasma pharmacokinetics; rate of brain uptake, redistribution, and clearance; as well as differences in receptor binding and kinetics.
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PMID:Quazepam and flurazepam: differential pharmacokinetic and pharmacodynamic characteristics. 168 Jan 20

Quazepam is a benzodiazepine hypnotic that can be useful in the adjunctive pharmacologic treatment of insomnia. It is slowly eliminated due to the long elimination half-lives of the parent compound and its two active metabolites, 2-oxoquazepam and N-desalkyl-2-oxoquazepam. This drug is recommended in doses of 15 mg for adults and 7.5 mg for geriatric patients. Sleep laboratory studies and clinical trials have shown that the 15 mg dose is quite efficacious for inducing and maintaining sleep not only with initial and short-term use but also with continued use. The 7.5 mg dose which has been studied less extensively has also been shown to be effective for inducing and maintaining sleep. There is considerable evidence of carryover effectiveness both during drug administration and after withdrawal. Thus, rebound phenomena are not observed during administration (early morning insomnia and daytime anxiety) and after withdrawal (rebound insomnia). Furthermore, certain behavioral side effects that have occurred with certain benzodiazepines (triazolam) have not been reported with quazepam. The only notable side effect seen with quazepam is a variable degree of daytime sedation, which can be minimized by intermittent use of the 15 mg dose when necessary and use of the 7.5 mg dose in the elderly. In comparison to triazolam and temazepam, quazepam is more effective with short-term use, and with continued use it maintains its efficacy in contrast to both of these drugs which show rapid development of tolerance. Most important, quazepam lacks the frequent and severe side effects increasingly reported with triazolam use or following its withdrawal.
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PMID:Quazepam: hypnotic efficacy and side effects. 196 51

Quazepam (QZP), a new long half-life benzodiazepine, seems to have a more specific hypnotic activity and a "physiological" mechanism of action. This study assessed its clinical efficacy and any withdrawal symptoms occurring after the treatment with QZP and triazolam (TRZ). Sixty-five patients (mean age 41.4 yrs +/- 12.43 SD) with sleep disorders were included in the study. The patients were treated with placebo for 4 days (run-in period) and if no amelioration of insomnia was observed, were then randomly allocated to 15 mg QZP (33 patients) or TRZ (32 patients) for 8 weeks and finally placebo for another week. Sleep quality, efficiency, side-effects and withdrawal effects were assessed by specific rating scales. In comparing data obtained from the two treatments, the following conclusions were drawn: 1) both drugs showed a hypnoinductive efficacy but patients treated with QZP had significantly fewer night awakenings; 2) at the end of treatment only patients treated with TRZ had longer awakenings and rebound symptoms; 3) a lower withdrawal symptom incidence was observed in patients treated with QZP. Therefore, QZP seems to have a good hypnotic effect without inducing withdrawal symptoms. In contrast TRZ turned out to be a merely hypno-inducing drug presenting higher risks of rebound effects after withdrawal.
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PMID:[Controlled clinical study on the effect of quazepam versus triazolam in patients with sleep disorders]. 269 8

Two benzodiazepine hypnotics, one with an intermediate elimination t1/2 (temazepam, 15 mg) and the other with a long t1/2 (quazepam, 15 mg), were evaluated in 22- night sleep laboratory studies. The effectiveness and side effects of these benzodiazepines were assessed during short- and intermediate term use. Subjects were also assessed for the presence of rebound insomnia after abrupt withdrawal. Quazepam, 15 mg, was significantly effective in improving sleep both with short- and intermediate-term use, but the effectiveness of temazepam was considerably less. Although temazepam was effective for maintaining sleep with short-term use, there was rapid development of tolerance for this effect with intermediate-term use. Temazepam did not produce any behavioral side effects during either drug condition. The only side effect associated with quazepam was a significant degree of daytime sleepiness. After its withdrawal, temazepam was associated with some sleep and mood disturbance on the first withdrawal night, whereas quazepam had carryover effectiveness.
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PMID:Quazepam and temazepam: effects of short- and intermediate-term use and withdrawal. 286 23

Quazepam is a trifluoroethyl benzodiazepine hypnotic with a half-life of 27 to 41 hours, which has been shown to induce and maintain sleep in the short to long term (up to 4 weeks) treatment of patients with chronic or transient insomnia. Although its hypnotic efficacy has been well characterised against placebo, there are few clinical studies in comparison with established hypnotics, particularly over long term administration. However, preliminary evidence suggests that quazepam 15 to 30 mg is as effective as flurazepam and triazolam in usual therapeutic doses, and causes minimal rebound insomnia following its withdrawal, unlike rapidly eliminated benzodiazepines such as triazolam. The lack of rebound phenomena is likely to be attributable to the 'carryover' effects occurring after discontinuation of quazepam, which has pharmacologically active metabolites with half-lives of elimination similar to or longer than that of the parent drug. Probably because of the long half-lives of quazepam's metabolites, daytime sedation, fatigue and lethargy are the most frequently reported side effects. These side effects are most intense with the 30 mg dose and least with the 7.5mg dose, which has not been studied extensively. Hence, quazepam is an effective hypnotic which may be particularly suitable for short or medium term use in patients in whom withdrawal effects or rebound insomnia may be especially bothersome. Further definition of certain characteristics of its profile--such as its long term use and potential for development of tolerance or dependence, effects on psychomotor skills, efficacy of the 7.5mg dose, and suitability in elderly patients and patients with chronic organic diseases--will assist in more clearly defining its ultimate place in therapy.
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PMID:Quazepam. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in insomnia. 289 93

Two benzodiazepine hypnotics, triazolam, 0.25 mg, with a short elimination t1/2, and quazepam, 15 mg, with a long t1/2, were evaluated in 22-night sleep laboratory studies. Quazepam improved sleep significantly during both short- and intermediate-term use. Daytime sleepiness, which decreased with continued use, was the side effect most often associated with quazepam dosing. In contrast, triazolam dosing did not significantly improve any of the major sleep efficiency parameters, and there was a rapid development of tolerance for the drug's slight initial effectiveness. In addition, there were a number of behavioral side effects including amnesia, confusion, and disinhibition. Withdrawal of triazolam was associated with sleep and mood disturbances (rebound insomnia and rebound anxiety), whereas quazepam exerted carryover effectiveness. Thus the data in this study show that the 0.25 mg dose of triazolam, which is being prescribed increasingly, has a profile of side effects that is similar to that of the 0.5 mg dose.
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PMID:Comparison of short and long half-life benzodiazepine hypnotics: triazolam and quazepam. 353 May 86

Quazepam, an investigational benzodiazepine, was evaluated in doses of 7.5, 15, and 30 mg in a 12-night protocol including four nights of drug trial. All three doses were effective in inducing and maintaining sleep, with the highest degree of effectiveness after the first drug night. Carry-over effectiveness, which was seen after withdrawal of all three doses, persisted throughout the withdrawal period after the 30-mg dose. Quazepam's effects during both drug use and withdrawal appeared to be dose related; 15 mg induced a greater reduction in wake time after sleep onset than the 7.5-mg dose, and 30 mg induced even greater differences in both wake time after sleep onset and total wake time. Subjective reports of improved sleep were in general agreement with the objective data at each dose level. Side effects appeared to be dose related in terms of severity. The efficacy and comparatively less severe side effects of the 7.5- and 15-mg doses of quazepam suggest that these doses may be optimal when the drug is considered for the adjunctive treatment of insomnia.
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PMID:Dose-response studies of quazepam. 611 10

The efficacy and safety of 15 mg quazepam was compared with placebo in 57 geriatric outpatients with insomnia. The study was double-blind, with treatments randomly assigned to patients. Placebo was taken by all patients for the first 3 nights followed by either placebo or quazepam for 5 nights. Post-sleep questionnaires were completed each day and the physician and patients rated the treatment at the end of the study. Quazepam was significantly better than placebo on all measures of efficacy. Indices of sleep quantity and quality showed that 15 mg quazepam produced significantly greater improvement in sleep than placebo on the first night of treatment and for the treatment period as a whole. There were no reports of unexpected or serious adverse experiences, and quazepam did not cause ataxia or impairment of motor co-ordination in any patient.
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PMID:Short-term quazepam treatment of insomnia in geriatric patients. 612 41

The hypnotic efficacy and safety of quazepam 15 mg was compared with placebo in thirty-six out-patients with insomnia. The study was double-blind, with two comparable groups of patients established by random allocation. Following a placebo baseline period, patients took placebo or quazepam for 5 consecutive nights and completed sleep questionnaires the next day. Quazepam was rated better than placebo in terms of sleep quality, sleep induction time, total sleep time, and early morning awakenings. Quazepam treatment was rated as good or excellent by the physician and the patients who received it almost three times more often was placebo. Quazepam was proved to be safe, with no reports of unexpected or serious adverse experiences.
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PMID:Short-term study of quazepam 15 milligrams in the treatment of insomnia. 634 48

Quazepam, a benzodiazepine hypnotic, was studied in normal subjects to evaluate steady-state kinetics of quazepam and of its major active plasma metabolites, 2-oxoquazepam and N-desalkyl-2-oxoquazepam, after 15 mg once daily by mouth for 14 days. The kinetics of quazepam and 2-oxoquazepam can be best described by a two-compartment open model with first-order absorption/formation kinetics. Quazepam was rapidly absorbed and its two major plasma metabolites appeared very quickly in systemic circulation. The elimination t 1/2s of quazepam, 2-oxoquazepam, and N-desalkyl-2-oxoquazepam were 41, 43, and 75 hr. Steady-state levels were predictable from the kinetic data and were reached by the seventh dose for quazepam and 2-oxoquazepam and by the thirteenth dose for N-desalkyl-2-oxoquazepam. These kinetic profiles may explain the clinical hypnotic effect of quazepam--rapid induction of sleep and long duration of clinical action without appreciable rebound insomnia.
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PMID:Multiple-dose quazepam kinetics. 670 50


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