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Query: UMLS:C0917801 (insomnia)
 10,606 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Zaleplon (Sonata) is an original hypnotic derived from the pyrazolopyrimidine with a full agonistic activity on central benzodiazepine receptors B21 type. Zaleplon is characterized by an extremely short half-life (about 1 hour). At the 10 mg dose, it is an affective sleep inducer with limited risks of disturbances in morning performance. It is particularly suitable for the treatment of initial insomnia when the prescription of an hypnotic is justified.
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PMID:[Pharma-clinics. Drug of the month. Zaleplon (Sonata)]. 1054 1

The present randomized, double-blind, placebo and active-drug controlled, crossover study assessed residual sedation after zaleplon 10 mg, flurazepam 30 mg (as an active control), and placebo, taken during a nocturnal awakening in patients with sleep maintenance insomnia. Twenty-two healthy sleep maintenance insomniacs (11 men; mean age, 42 y) received zaleplon, flurazepam, or placebo after an experimental awakening 3.5 hours after bedtime on two consecutive nights in each of three conditions. Residual sedation was measured with sleep latency testing (5 and 6.5 h postdrug), digit symbol substitution, symbol copying, and subjective sleepiness by visual analog scale, each twice each morning. Zaleplon did not differ from placebo on any measure of residual sedation; flurazepam showed significant sedation on all measures. No residual sedative effects were detected 5 or 6.5 hours after ingestion of zaleplon during the middle of the night by sleep maintenance insomniacs.
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PMID:Lack of residual sedation following middle-of-the-night zaleplon administration in sleep maintenance insomnia. 1068 26

Objective: To examine the hypnotic efficacy of zaleplon 10 mg, a selective benzodiazepine receptor agonist, over a period of 35 nights in primary insomniacs.Methods: A double-blind, parallel-group, placebo-controlled design was employed. Subjects were 113 men and women, ages 18 to 65 years. Polysomnographic and subjective sleep data were collected during baseline, on two nights during each of five treatment weeks, and on the first two nights after discontinuation of active medication.Results: Sleep latency was significantly shortened with zaleplon 10 mg for all 5 weeks of treatment as assessed by polysomnography and by subjective sleep measures. Total sleep time, whether evaluated with polysomnography or with subjective estimates, was inconsistently affected. Sleep architecture was similar with zaleplon and placebo. There was no evidence of tolerance to the sleep promoting effects of zaleplon during the five weeks of administration, and there was no rebound insomnia upon discontinuation. Adverse events occurred with equal frequency in the zaleplon and placebo groups.Conclusions: Zaleplon 10 mg is effective in the treatment of sleep onset insomnia over a period of 35 nights, with minimal evidence of undesired effects.
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PMID:A five week, polysomnographic assessment of zaleplon 10 mg for the treatment of primary insomnia. 1073 19

The elderly are known to have a high prevalence of insomnia. Causes of insomnia include: medical, psychiatric, and drug issues; circadian rhythm changes; sleep disorders; and psychosocial factors. The elderly frequently use sleeping aids. Risks associated with elderly patients' use of hypnotic drugs are attributable to concomitant comorbid conditions, use of multiple medications, altered pharmacokinetics, and increased central nervous system sensitivity to these drugs. Treatment options for insomnia include behavior modification and pharmacotherapy. The choice of hypnotics is based on matching the nature of the insomnia to the hypnotic agent. Benzodiazepine receptor agonists are common hypnotics prescribed for insomnia in the elderly. The ideal agent has rapid onset, duration of action that lasts through the night but no residual daytime effects, and no adverse effects. The longer-acting agents have been shown to result in a higher risk of falls and hip fractures in the elderly. This relationship is not apparent with short-acting agents. Zaleplon, the newest benzodiazepine receptor agonist, has the shortest half-life of available agents. Studies have demonstrated that zaleplon is effective in improving sleep latency, duration, and sleep quality in the elderly. Zaleplon does not appear to cause rebound insomnia, residual sedation, or adversely affect psychomotor function. The key for the healthcare professional is finding the appropriate treatment or treatment combination, including behavioral modification and pharmacotherapy. When hypnotics are indicated, the most appropriate short-acting agent should be considered.
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PMID:Insomnia in the elderly: a review for the primary care practitioner. 1075 5

The efficacy and safety of three doses of zaleplon, a novel non-benzodiazepine hypnotic, were compared with those of placebo in outpatients with insomnia in this 4-week study, using zolpidem 10 mg as active comparator. Postsleep questionnaires were used to determine treatment effects on the patient's perception of sleep, as well as any development of pharmacological tolerance during therapy or rebound insomnia or withdrawal symptoms upon discontinuation of therapy. During week 1, sleep latency was significantly shorter with zaleplon 5, 10, and 20 mg compared to placebo. The significant decrease in sleep latency persisted through week 4 with zaleplon 20 mg, and was again evident with zaleplon 10 mg at week 3. Zaleplon 20 mg also had significant effects on sleep duration, number of awakenings, and sleep quality compared to placebo. No pharmacological tolerance developed during treatment with zaleplon and there were no indications of rebound insomnia or withdrawal symptoms after treatment discontinuation. Zolpidem 10 mg had significant effects on sleep latency, sleep duration, and sleep quality compared to placebo. However, a significantly greater incidence of withdrawal symptoms and a suggestion of sleep difficulty after treatment discontinuation (rebound insomnia) for all sleep measures was seen with zolpidem compared to placebo. There was no significant difference in the frequency of adverse events with active treatment compared to placebo. These results show that zaleplon provides effective treatment of insomnia with a favourable safety profile.
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PMID:Zaleplon improves sleep without producing rebound effects in outpatients with insomnia. Zaleplon Clinical Study Group. 1087 Aug 72

Insomnia is a frequent complaint in the elderly population. Hypnotic agents, including benzodiazepines, with longer pharmacological half-lives have been associated with side effects, including residual sedation, memory impairment, and discontinuation effects. Zaleplon is a short-acting (elimination half-life of 1 hour), non-benzodiazepine hypnotic that acts on the benzodiazepine type 1 site of the gamma-aminobutyric acid type A (GABA(A)) receptor complex. The pharmacology and pharmacokinetics of Zaleplon suggest a safety profile that is improved over other hypnotics. The objective of this placebo-controlled study was to evaluate the efficacy and safety of Zaleplon (5 and 10 mg) in elderly (> or =65 years) outpatients with primary insomnia. This was a multicenter, double-blind, randomised, placebo-controlled 2-week outpatient study. Postsleep questionnaires were used to record subjective sleep variables: sleep latency, sleep duration, number of awakenings, and sleep quality. Zaleplon significantly reduced subjective sleep latency during both weeks of the study with both 5- and 10-mg doses. Subjective sleep quality was improved for significantly more patients treated with zaleplon 10 mg than those treated with placebo during both weeks of treatment. There was a weak indication of rebound insomnia after discontinuation of treatment with the 10-mg dose, but no significant difference in common treatment-emergent adverse events across treatment groups. Zaleplon is an effective and safe hypnotic for the treatment of insomnia in the elderly.
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PMID:Zaleplon shortens subjective sleep latency and improves subjective sleep quality in elderly patients with insomnia. The Zaleplon Clinical Investigator Study Group. 1096 Aug 82

Zaleplon is a pyrazolopyrimidine hypnotic agent which is indicated for the short term (2 to 4 weeks) management of insomnia. Zaleplon 5 and 10 mg at bedtime (usual recommended doses) significantly reduced sleep latency compared with placebo in clinical trials in nonelderly and elderly patients with insomnia. In general, sleep maintenance (sleep duration and number of awakenings) and sleep quality were not significantly different from placebo with zaleplon 5 and 10 mg/night. Zaleplon 20 mg/night significantly improved sleep latency and duration in nonelderly patients, but effects on number of awakenings were inconsistent and sleep quality generally did not improve. The relative hypnotic efficacy of zaleplon compared with that of triazolam and zolpidem is not yet clearly established. Tolerance to the hypnotic effects of zaleplon generally did not occur during 5 weeks' treatment, or during long term treatment (6 or 12 months) according to a small number of studies presented as abstracts. Zaleplon was well tolerated in clinical trials. The most common event was headache but the incidence was similar to that observed with placebo. Zaleplon 5 and 10 mg did not impair psychomotor function or memory even immediately after the dose in studies in volunteers or patients with insomnia. Zaleplon 20 mg, however, impaired psychomotor function and memory immediately after the dose but next-day effects were not observed. The psychomotor profile of zaleplon appears to be better than that of comparator agents. Rebound insomnia was not observed after sudden discontinuation of up to 12 months' treatment with zaleplon 5 and 10 mg/night and up to 4 weeks' treatment with zaleplon 20 mg/night. In addition, the potential for withdrawal syndrome with zaleplon appears to be low according to limited data. In conclusion, zaleplon 5, 10 and 20 mg administered at bedtime, or later if patients have difficulty sleeping, is an effective and well tolerated hypnotic agent. There was no evidence of next-day residual effects with the 5 and 10 mg dosages, and the incidence of withdrawal effects with zaleplon 5, 10 and 20 mg did not differ significantly to that observed with placebo. In addition, tolerance to the effects of zaleplon is unlikely to develop when administered for the recommended treatment period. The comparative efficacy and tolerability of zaleplon with other short acting nonbenzodiazepine hypnotics is difficult to establish. However, on the basis of current efficacy evidence and the lower incidence of residual effects with zaleplon 5 and 10 mg relative to comparator agents, this drug represents a useful option in the management of patients with insomnia who have difficulties initiating sleep.
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PMID:Zaleplon: a review of its use in the treatment of insomnia. 1098 40

Sleep is an active process consisting of macro- and microarchitectural rhythms, chronobiology, and neurochemical changes. Disruptions in sleep chronobiology, which may occur in shift workers and the elderly or due to jet lag, often respond to exogenous melatonin. Insomnia requires careful evaluation to determine contributions of comorbid medical conditions and drug effects. Treatment options include sleep hygiene principles and sedative hypnotic therapy. Zaleplon and zolpidem, short-acting benzodiazepines selective for omega-1 GABA receptors, are effective first-line agents for initiating sleep.
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PMID:Sleep disorders: assisting patients to a good night's sleep. 1102 66

Zaleplon (N-[3-(3-cyanopyrazolo[1,5-a] pyrimidin-7-yl) phenyl]-N-ethyl acetamide) is a non-benzodiazepine recently introduced for clinical use. This agent is indicated for the short-term treatment of insomnia. Preclinical studies have shown that the benzodiazepines triazolam and Ro17-1812 can substitute for zaleplon in animals trained to distinguish zaleplon from saline. The benzodiazepine antagonist flumazenil can antagonise the discriminative stimulus effect of zaleplon. These findings suggest that zaleplon is recognised by animals as a benzodiazepine agent. Zaleplon is active after ip. and oral administration in a variety of motor performance tests, including locomotor activity, rotarod and the loaded grid. Zaleplon has been shown to be active in a number of different anticonvulsant models, including the pentylenetetrazole, isoniazid and electroshock models. The compound is also reported to be active against convulsions induced by bicuculline, picrotoxin and strychnine. Studies in anxiolytic models suggest that zaleplon may have weak anxiolytic activity. From preclinical studies, it appears zaleplon possesses a reduced risk of tolerance compared to triazolam, is less likely to potentiate the effects of ethanol and is unlikely to produce amnestic effects. In man, zaleplon is rapidly absorbed and undergoes extensive presystemic metabolism. The compound has a plasma half-life of approximately one hour and is metabolised primarily via the aldehyde oxidase system to form 5-oxo-zaleplon. This metabolite, along with other minor metabolites formed in vivo, do not appear to contribute to the activity of zaleplon. Metabolites of zaleplon are excreted primarily via the urine. Phase I studies suggest that single daytime doses of zaleplon up to 15 mg are well-tolerated. Short-term impairment of performance occurs when zaleplon is administered during the day at doses epsilon 20 mg. However, given the short half-life of the compound, significant impairment of daytime performance is unlikely if zaleplon is administered at bedtime or shortly after retiring for the evening. Results from Phase II/III studies suggest that zaleplon (5 - 20 mg) produces a dose-dependent reduction in sleep latency in patients suffering from primary insomnia. The clinical efficacy of zaleplon persists for at least four weeks at doses of 10 mg and 20 mg. Studies in patients with a history of drug abuse suggest that the abuse potential of zaleplon (at doses above the therapeutic dose range) is similar to that seen with the benzodiazepine triazolam.
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PMID:Zaleplon - a review of a novel sedative hypnotic used in the treatment of insomnia. 1106 Jul 14

Insomnia is common among the primary care patient population, 1.3 times more common in women than men, and the prevalence increases with age. Until recently, benzodiazepines (BZs) were the only first-line hypnotics, but with the availability of non-BZ sleep agents, the management of insomnia is changing. Zolpidem and zopiclone have adverse-effect profiles similar to BZs but lack next-day residual effects with bedtime dosing. Zaleplon is a fast-onset, rapidly eliminated medication that allows for dosing at bedtime or during the night with minimal concern for residual effects. In addition, the BZ-associated problems of tolerance and rebound effects are not evident with long-term zaleplon use. The pharmacokinetic profile of zaleplon has the potential to allow for the treatment of symptoms of sleeplessness when they occur, an approach that could replace the standard practice of always treating in anticipation of a problem.
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PMID:Implications of hypnotic flexibility on patterns of clinical use. 1121 27


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