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)

Zopiclone is a cyclopyrrolone derivative which exerts, in animal and man, an hypnotic activity comparable to that of flurazepam. In healthy adult insomniacs it was well tolerated upon repeated administration for 28 days. In a double-blind, placebo-controlled, crossover study, three dose levels of zopiclone (5, 7.5, and 10 mg) were compared to 15 mg of flurazepam in 30 geriatric insomniacs. The 7.5- and 10-mg doses demonstrated hypnotic potency comparable to that of flurazepam, and the active treatments were superior to placebo. For most sleep indices, 7.5 mg was the optimal therapeutic dose. Few side effects were reported. These were not clinically significant. Zopiclone is efficacious and well tolerated in the treatment of geriatric patients suffering from insomnia. A dosage range of 7.5-10 mg is recommended.
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PMID:Efficacy and tolerance of zopiclone in insomniac geriatric patients. 718 74

Zopiclone, a novel cyclopyrrolone compound has recently become available for the treatment of insomnia in Singapore. Pharmacodynamic and pharmacokinetic studies have shown it to be an effective hypnotic with a good safety profile and minimal side-effects. The efficacy of Zopiclone was studied in a group of patients with insomnia (n = 40). The study group comprised patients with and without a psychiatric diagnosis. About two-thirds (65%) of the patients had been on hypnotics previously without relief of the insomnia. There was improvement in the various sleep parameters studied: sleep latency, sleep duration, night awakening, sleep quality, dreams, "day-after" effects. The drug was well-tolerated and only four patients experienced minor side-effects.
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PMID:A postmarketing surveillance study of zopiclone in insomnia. 789 99

Zopiclone is a cyclopyrrolone which is chemically unrelated to the benzodiazepines and is thought to act on the GABAA receptor complex at a site distinct from, but closely related to, the benzodiazepine binding site. The hypnotic efficacy of zopiclone administered as single oral doses has been demonstrated in patients undergoing next-day surgery and in patients with insomnia, and these studies have established an optimal dose of 7.5mg for elderly patients. Using this dose, clinical studies have shown that zopiclone improved sleep in elderly patients to a similar extent as triazolam 0.125 to 0.5mg, flurazepam 15mg, and nitrazepam 5mg. Studies that also included younger patients have shown that zopiclone 7.5mg is at least as effective as triazolam 0.25 or 0.5mg, and on most sleep parameters is comparable to temazepam 20mg, nitrazepam 5mg, flunitrazepam 2mg, and flurazepam 20mg. Zopiclone causes minimal impairment to psychomotor performance and mental alertness the morning after night-time administration. The drug is generally well tolerated by patients of all ages; the most frequently reported adverse effects being bitter taste and dry mouth. Treatment withdrawal due to adverse effects is seldom required and reports of rebound insomnia after zopiclone withdrawal are rare. While symptoms of physical dependence have not been observed in clinical studies, there have been isolated reports of physical dependence in patients with a history of substance abuse. Although the latter finding should be kept in mind, it appears that zopiclone has a low dependence liability. Thus, with its short duration of action and good tolerability profile, zopiclone is a well established alternative to the benzodiazepine hypnotics and may be particularly beneficial in those patients unable or unwilling to tolerate the residual effects associated with many other hypnotic agents.
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PMID:Zopiclone. A review of its pharmacological properties and therapeutic efficacy as an hypnotic. 824 8

Zopiclone is a new short half-life cyclopyrrolone hypnotic agent acting at the GABA-benzodiazepine receptor complex. In order to characterize its pharmacological profile, the effects of 7.5 mg zopiclone on nocturnal melatonin secretion were investigated under polysomnographic control in 11 healthy subjects following acute and subchronic administration as well as after abrupt discontinuation of the drug. No effect of zopiclone on the melatonin plasma levels could be observed. Regarding both total melatonin production and the temporal pattern of melatonin secretion during the night, there was no difference between placebo baseline condition, acute and subchronic administration, and discontinuation. In contrast, the sleep EEG data demonstrated the hypnotic efficacy of zopiclone under acute administration and indicated a rebound insomnia after abrupt discontinuation. Moreover, alterations of sleep architecture were found under treatment as well as after discontinuation. Whereas, with regard to sleep EEG parameters, zopiclone appears to be comparable with some short-acting benzodiazepines, a discrepancy between the missing effect of zopiclone on pineal function and the suppressing influence of benzodiazepines known from the literature becomes obvious. The fact that zopiclone does not interfere with nocturnal melatonin secretion at pharmacologically active doses as indicated by alterations in sleep EEG parameters might possibly point to a pharmacodynamic difference between the two drug classes.
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PMID:Acute, subchronic and discontinuation effects of zopiclone on sleep EEG and nocturnal melatonin secretion. 888 74

Night sleep was examined in 120 patients with different forms of insomnia. The positive effect of Imovane was shown both on presomnic and intrasomnic disorders. Transitory side effects (dryness, bitter taste in the mouth) were in some cases that didn't need cessation of therapy. Polysomnographic studies confirmed effectivity of Imovane: there were observed either lengthening of the duration of sleep, its 2 stage, delta-sleep, or decrease of the duration of falling asleep. There were no respiratory changes after course of Imovane, meanwhile some indices positive dynamics was revealed in this case.
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PMID:[The effect of Imovane on sleep structure and respiratory indices during sleep in insomnia patients]. 921 91

We report a 55 years old married woman without history of drug dependence. Due to a severe marital conflict she developed a chronic adjustment disorder with depressed mood. Zopiclone, 7.5 mg at night was prescribed for her insomnia and she rapidly became tolerant and dependent to the hypnotic. She was admitted to a psychiatric clinic, slowly detoxified and treated with pharmacotherapy and psychotherapy. Six months later, she has resumed her housekeeping and professional activities and is maintained with a benzodiazepine at night for insomnia.
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PMID:[Zopiclone dependence. Report of one case]. 946 Feb 72

Zopiclone is a non-benzodiazepine hypnotic which was first reviewed in Drugs in 1986. At that time, zopiclone had shown hypnotic efficacy superior to that of placebo, but had not been extensively compared with benzodiazepine hypnotics in patients with insomnia. A much larger body of clinical data is now available, allowing a more detailed evaluation than was previously possible. Together with results from earlier studies, subsequent clinical trials have shown that zopiclone is generally at least as effective as the benzodiazepines (regardless of duration of action) in the treatment of insomnia, although comparisons between zopiclone and flurazepam have produced inconsistent results. Tolerance to the effects of zopiclone was not seen in short term clinical trials (< or = 4 weeks); data from longer term studies are conflicting and the potential for tolerance during long term zopiclone treatment is therefore unclear. Zopiclone has a relatively low propensity to cause residual clinical effects (such as difficulty in waking or reduced morning concentration). Rebound of insomnia to a level below that at baseline can occur after withdrawal of zopiclone, but, on the basis of data from short term studies, does not appear to be common. Data from prescription-event monitoring suggest that zopiclone does not have a high dependence potential (at least in those who are not regular drug abusers/addicts). Zopiclone is well tolerated in both the elderly and younger patients with insomnia. A bitter aftertaste is usually the most common adverse event, but is relatively infrequent (3.6% in the largest available postmarketing study). Thus, zopiclone is now firmly established as an effective and well tolerated hypnotic agent. Although the available data on rebound insomnia and dependence liability are encouraging, potential differences between zopiclone and the benzodiazepines in these respects may have little clinical relevance in the context of short term intermittent use of hypnotics, as it currently recommended. A low propensity for rebound insomnia and dependence might prove valuable during long term hypnotic therapy (which, although not recommended, is a clinical reality). However, the risk-benefit profile of zopiclone in this context remains unknown. Nevertheless, zopiclone is clearly a suitable alternative to the benzodiazepines for the short term treatment of insomnia.
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PMID:Zopiclone. An update of its pharmacology, clinical efficacy and tolerability in the treatment of insomnia. 950 47

For insomniac patients, sleeping drugs are used: in addition, concomitant therapy with other drugs has been tried in an effort to prevent a decrease in the effects due to long-term continuous use. This report presents the results of a study on the sleeping effects in nine aged patients with insomnia associated with cerebrovascular and noncerebrovascular disorders who received concomitant therapy with Zopiclone and Aniracetam. The treatment in 7/9 cases (78%) was found to be effective, showing more than 50% prolongation of sleeping time, and in two cases (22%) was found to be ineffective. We discuss the mechanism of action referring to the literature.
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PMID:Treatment of insomnia by concomitant therapy with Zopiclone and Aniracetam in patients with cerebral infarction, cerebroatrophy, Alzheimer's disease and Parkinson's disease. 962 49

Insomnia, especially when chronic, is associated with disturbances in daytime well-being and performance, resulting in a poor quality of life for those affected. Zopiclone has been proven as a drug that favourably balances sleep induction and maintenance as well as an improvement in daytime well-being (efficacy) with a low potential for adverse effects (safety) in the symptomatic treatment of insomnia. Management of chronic insomnia with zopiclone needs a multidimensional approach involving the proper diagnosis of possible underlying causes, and combined use of causal treatment, general sleep hygiene measures, basic elements of psychological treatment and adjunctive medication. It is recommended that therapy with the nonbenzodiazepine hypnotic zopiclone should conform to the guidelines for the use of hypnotics, which are valid for all benzodiazepine receptor agonists.
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PMID:Clinical management of patients with insomnia. The role of zopiclone. 1016 25

Zopiclone is a cyclopyrrolone hypnosedative that is chemically unrelated to the benzodiazepines but nevertheless potentiates gamma-aminobutyric acid-mediated neuronal inhibition, and has demonstrated proven efficacy and good tolerability in the treatment of insomnia over 15 years of use. Zopiclone is indicated for short term use, and should not be prescribed for more than 4 weeks. This review compares the efficacy of zopiclone with that of a number of commonly used short-, medium- and long-acting benzodiazepines. Zopiclone at dosages of 7.5 mg/day has demonstrated efficacy equivalent and in some cases greater to that of flurazepam 30 mg/day, nitrazepam 5 mg/day, flunitrazepam 1 to 2 mg/day, temazepam 20 mg/day, triazolam 0.125 to 0.5 mg/day and midazolam 15 mg/day. Zopiclone-treated patients reported themselves to be less impaired by daytime sedation than patients treated with the medium- and long-acting hypnosedatives flurazepam, nitrazepam and flunitrazepam. Zopiclone and temazepam showed similar effects on daytime behaviour while zopiclone appeared to have somewhat better effects on daytime well-being than the short-acting triazolam and midazolam. There has been no clinical comparison with the frequently used medium-acting benzodiazepines lormetazepam and brotizolam and the imidazopyridine hypnosedative zolpidem. Data from clinical trials, pooled analyses and postmarketing surveillance including over 30,000 patients showed that with the exception of bitter taste (reported by <10% of zopiclone recipients), the tolerability profile of zopiclone is similar to that of placebo. Clinical trials found no evidence for significant rebound insomnia and indicated that the risk of withdrawal reactions with therapeutic doses of zopiclone is very low. In addition, to date, dependency appears very low, although abuse potential should be considered following a history of addiction or psychiatric illness. Evaluation of the accumulated evidence from over 2.5 billion units dispensed in more than 30 countries indicates that zopiclone is effective, well tolerated and an excellent alternative to benzodiazepines in the short term treatment of insomnia.
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PMID:A comparative assessment of the risks and benefits of zopiclone: a review of 15 years' clinical experience. 1061 70


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