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PubMed2000

Acute effects of zopiclone on blood glucose level and serum lipids in hyperlipidemic rats. Interactions with PK 11195 and flumazenil.

UNLABELLED: Intraperitoneal administration of 5 mg/kg zopiclone a cyclopyrolone acting on the central benzodiazepine receptors was found to produce significant reduction of total lipids, total cholesterol and triglyceride in rats randered hyperlipidemic by intraperitoneal injection of Triton W-1339. Blood glucose level was also reduced. Flumazenil (10 mg/kg) potentiated the hypoglicemic effect of zopiclone but had no additional effect on serum lipids. PK 11195 (25 mg/kg) antagonized the hypolipidemic effects of zopiclone. IN CONCLUSION: 1. The central benzodiazepine receptors are not involved in the hypolipidemic activity of zopiclone. 2. The peripheral type benzodiazepine receptors are partly responsible, for the hypolipidemic activity of this cyclopirrolone. 3. The changes of blood glucose level induced by these drugs does not seem to be related to benzodiazepine receptors.

Animals↗
PubMed2000

Acute effects of zopiclone on blood glucose level and serum lipids in hyperlipidemic rats.

In rats rendered hyperlipidemic by ip administration of Triton WR-1339, the ip administration of zopiclone at doses of 1.25, 2.5, 5.0, 7.5, 10.0 and 15.0 mg/kg, a cyclopyrrolone acting upon the central benzodiazepine receptors, induces very significant reductions of total lipids, total cholesterol, and triglycerides, at nearly all of the doses. The most active dose was 5.0 mg/kg. The blood glucose level was diminished by doses of 1.25, 2.5, 7.5 and 15.0 mg/kg and it was not changed by the rest of the other doses.

Animals↗
PubMed2000

The effects of zolpidem and zopiclone on daytime sleepiness and psychomotor performance.

Zolpidem (ZLP), which has selective affinity to the BZ1 (omega 1) receptor and a short half-life, is a novel hypnotic. The objective of this study is to compare the residual effects of standard clinical doses of ZLP and zopiclone (ZPC), a short-acting hypnotic marginally selective for the BZ1 (omega 1) receptor, given in a single dose on daytime sleepiness and psychomotor function. This study was carried out as a double-blind cross-over study with 10 mg ZLP, 7.5 mg ZPC and a placebo in 12 healthy male adults. In the multiple sleep latency test, sleep latency was not reduced but increased by ZLP and ZPC as well as the placebo when drug plasma levels had nearly reached the peak. Subjects administered ZLP were significantly more feeble, lethargic and antagonistic in mood rating scales than those administered ZPC. The incidence of severe behavioral side effects was higher in the case of ZLP than in the case of ZPC over the same period. Sleep latency the next morning was significantly shorter in the case of ZPC than in the case of ZLP or the placebo. The tapping test performed at the same time demonstrated that the number of taps was significantly less in the case of ZPC than in the case of ZLP or the placebo. The results of the present study suggest that ZLP acts more rapidly than ZPC. On the other hand, ZLP has less residual effect on sleepiness and psychomotor function the next morning.

Adult↗
PubMed2001

Fatal overdose of zopiclone in an elderly woman with bronchogenic carcinoma.

The death of a 72-year-old woman with respiratory debilitation due to bronchogenic carcinoma is described. She overdosed herself with probably 200 to 350 mg of zopiclone. Zopiclone, quantitated by HPLC in femoral postmortem blood, was found to be 1.9 mg/L (4.8 micromol/L). This level is higher than many other zopiclone fatalities reported. We report a case where only zopiclone was detected.

Aged↗
PubMedDate not supplied

[Homeopathic specialties as substitutes for benzodiazepines: double-blind vs. placebo study].

The objective of this study was to compare the efficacy of homeopathic drugs Homéogène 46 and Sédatif PC with a placebo as substitute for benzodiazepines in patients treated for at least 3 months with low doses (less than 10 mg/d of diazepam equivalents). A double-blind randomized trial was carried out in general practice. The treatment lasted one month. Several rating scales were used. The main outcome was success/failure defined according to the doctor's clinical judgement and interruption of treatment. A total of 61 patients were randomized, and 19 interrupted their treatment. Comparability between the groups was good. No statistically significant difference between homeopathic drugs and placebo was observed for the main outcome or for the secondary outcomes. The lack of statistical power due to accrual difficulties limits the conclusions of this trial which did not confirm the efficacy of homeopathic drugs in this indication.

Adult↗
PubMed2001

[Clinical and psychological characteristics and therapy of patients with cluster (bunch) headache].

The paper presents a discussion on clinical psychological peculiarities of patients with cluster headache (CHA), an analysis of these data in dependence on CHA form (episodically or chronically), on the sex of the patients, on the side of the headache localization (right-sided, left-sided). Taking into consideration a correlation of the headache attacks and the quality of the night sleep, the therapy with imovan (zopiclone) preparation was proposed. Such therapy resulted in positive changes including disappearance of the night attacks and the decrease of the intensitivity of the algesic attacks during daily time.

Adult↗
PubMed2001

Melatonin and zopiclone as pharmacologic aids to facilitate crew rest.

PURPOSE: In response to mission imperatives, transport aircrews must often sleep at inappropriate circadian times resulting in inadequate sleep. This study was undertaken to determine whether either melatonin or zopiclone could facilitate early circadian sleep, and to assess whether either of these medications would result in a psychomotor performance decrement which would preclude their use in aircrew. METHOD: Thirteen subjects from DCIEM completed a double-blind cross-over protocol. All subjects were assessed for psychomotor performance during 3 drug conditions (placebo, 10 mg melatonin, and 7.5 mg zopiclone), which were separated by one week. Each of these conditions involved 2 nights of sleep, back-to-back, with the first night being a normal circadian control sleep (23:00 h bedtime, arising at 06:45 h), and the second night being an early circadian drug sleep (drugs at 16:45 h, 17:00 h bedtime, arising at 23:45 h). All subjects were tested for psychomotor performance, on both nights of each of the 3 drug conditions, pre- and post-sleep. Further, during the early circadian drug night, all subjects were tested every hour after arising at 23:45 h (24:00 h until 07:00 h. At the beginning of each psychomotor test session, subjects were asked for their subjective levels of sleepiness and fatigue. RESULTS: Relative to placebo (339.5 min) the subjects slept more on melatonin (370.2 min, p < 0.01), and zopiclone (373.3 min, p < 0.01). Performance in serial reaction time (SRT) task (p < 0.001), logical reasoning task (LRT) (p < 0.001), serial subtraction task (SST) (p < 0.02), and Multitask (MT) (p < 0.03) were impaired for all 3 drug conditions immediately on awakening, compared with pre-sleep performance, as a result of a sleep-inertia effect. With respect to the subjective data, sleep inertia effects were evident for sleepiness (p < 0.001), mental fatigue (p < 0.002), and physical fatigue (p < 0.05). For SRT, LRT, and SST, performance recovered to pre-sleep levels within 1.25 h of awakening, and for MT recovery occurred 2.25 h after awakening. There were no differences in performance or subjective measures between placebo, melatonin and zopiclone. CONCLUSIONS: Both zopiclone and melatonin improved sleep relative to placebo. After sleep inertia, performance recovered to pre-sleep levels for all tasks and was sustained at that level throughout the balance of the testing period. There was no impact of melatonin or zopiclone on performance measures compared with placebo.

Adult↗
PubMed2001

(S)-Zopiclone Sepracor.

(S)-Zopiclone, a cyclopyrrolone sharing activity with benzodiazepines in the CNS, is a short-acting sedative being developed by Sepracorfor the potential treatment of sleeping disorders. In August 2000, the company had completed phase II trials of (S)-zopiclone for insomnia [380377]; by September 2000, patient enrollmentfor phase III studies for insomnia was completed and the trial initiation was planned for October 2000 [381361]. Merrill Lynch expects US filing to take place in the second half of 2001 [383230]. Sepracor was granted US-05786357 in August 1998 covering methods and compositions of (S)-zopiclone in the treatment of sleeping disorders [342938]. In August 2000, Merrill Lynch predicted (S)-zopiclone sales of US $30 million in 2002, rising to US $150 million in 2004 [383230].

Animals↗
PubMed2002

Differential residual effects of zaleplon and zopiclone on actual driving: a comparison with a low dose of alcohol.

STUDY OBJECTIVES: To compare residual effects of zaleplon 10 mg, zopiclone 7.5 mg, and placebo, and a social dose of alcohol on car driving, memory, and psychomotor performance. DESIGN: Two-part placebo controlled, crossover study. Part 1 was single blind, Part 2 double blind. SETTING: University research institute. PARTICIPANTS: Thirty healthy volunteers (15 men and 15 women, mean age 32 +/- 7 years) INTERVENTIONS: In Part 1 alcohol and alcohol-placebo drinks were administered around noon. In Part 2 single oral doses of zaleplon 10 mg, zopiclone 7.5 mg and placebo were administered at bedtime. MEASUREMENT AND RESULTS: A highway driving test, laboratory tests of word learning, critical tracking and divided attention, and subjective assessments of sleep, mood, and effects of treatments on driving. Driving started 40 minutes after a second alcohol dose in Part 1, and 10 hours after drug intake in Part 2. The results demonstrated that alcohol, at average plasma concentrations of approximately 0.030 g/dl, significantly impaired performance in all tests. Zaleplon's residual effects did not differ significantly from those of placebo in any test. In contrast, zopiclone had significant residual effects on driving, divided attention, and memory. The magnitude of impairment in the driving test observed the morning after zopiclone 7.5 mg was twice that observed with alcohol. CONCLUSION: Zaleplon 10 mg has no residual effects on driving when taken at bedtime, 10 hours before driving. In contrast, zopiclone 7.5 mg can cause marked residual impairment. Patients should be advised to avoid driving the morning after zopiclone administration.

Acetamides↗
PubMed2001

[Effectiveness of zopiclone in disorders of initiating and maintaining sleep. Results of a drug monitoring study in 811 general practices].

BACKGROUND AND METHOD: In a drug monitoring study with 811 participating general practitioners, safety and tolerability of zopiclone were studied in 2416 patients with disorders of initiating and maintaining sleep. RESULTS: In general, zopiclone was efficient in all forms of insomnia; the subjective sleep duration was prolonged for 2 hours on average. Patients without somatic complaints or comorbidity showed the greatest benefit. Daytime well-being and vigilance were in general not impaired. Drug related adverse events occurred rarely; the great majority of the participating physicians rated the treatment with zopiclone as efficient and acceptable. CONCLUSION: In this drug monitoring study, zopiclone proved an efficient hypnotic for the treatment of disorders of initiating and maintaining sleep.

Adult↗
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↗
PubMed2002

[Comparison of zopiclone and midazolam premedication for preoperative anxiolysis].

To compare the anxiolysis property of zopiclone (ZPC) and midazolam (MDZ), 117 patients were given zopiclone 7.5 mg p.o. or midazolam 0.05 mg.kg-1 i.m. as premedication. In the study 1, patients were randomly allocated to 4 groups: ZZ group (n = 16) received ZPC in the night before operation and 2 h before operation, ZM group (n = 18) received ZPC in the night before operation and MDZ 1 h before operation, Z group (n = 18) received ZPC 2 h before operation, and M group (n = 24) received MDZ 1 h before operation. The degree of anxiety was evaluated using the state-trait anxiety inventory (STAI) on the day before operation and after receiving premedication. ZPC showed a significant reduction in the STAI score in the ZZ and Z group, but premedication with MDZ showed no changes in the STAI score. In the study 2, patients were randomly allocated to 2 groups: ZPC group (n = 22) received ZPC 2 h before operation, and M group (n = 19) received MDZ 1 h before operation. The degree of anxiety was evaluated using the visual analog scale (VAS) on the day before operation and after receiving premedication. ZPC showed a significant reduction in the VAS score, but MDZ showed no changes in the VAS. It is concluded that ZPC (7.5 mg p.o.) is suitable to reduce the preoperative anxiety in patients who are to undergo surgery as compared to MDZ (0.05 mg.kg-1 i.m.).

Adult↗
PubMed2002

[Study of the real situation of improvement by Zopiclone in treatment of insomnia among persons working during night shifts].

UNLABELLED: We investigated the effect of adapted management of sleep on the duration and quality of sleep in shift workers working the night shift. Twenty-nine shift workers suffering from insomnia were included and treated with zopiclone (7.5mg/day) or placebo according to a random double-blind protocol. Patients completed a sleep diary and a wrist actigraph was used to evaluate episodes of rest/activity. A self-administered subjective sleep questionnaire was filled out just after awakening. Zopicone was found to increase the duration of sleep significantly (p<0.05) over the baseline duration after the first and second night on duty. Subjective estimation of sleep was better in patients taking zopiclone who exhibited a smaller number of shorter awakening episodes. IN CONCLUSION: zopiclone improves the quality and duration of sleep in shift workers suffering from insomnia.

Adult↗
PubMed2002

Insomnia. Diagnosis and management.

BACKGROUND: Insomnia is a complaint of perceived poor sleep quality resulting in impairment of daytime function. It is the commonest clinical sleep disorder with approximately 6-12% of adults complaining of chronic insomnia. OBJECTIVE: To review current knowledge on causes and effects of insomnia and to provide a brief evidence based review of management options for the family practitioner. DISCUSSION: Patients with insomnia are characterised by excessive arousal and an inability to sleep despite reported reduced sleep hours and poor sleep quality. Current management approaches are focussed on reducing this 'hyperarousal' and its behavioural manifestations by a range of behavioural treatments. Good evidence exists for the efficacy of hypnotics for short term insomnia but long term data is currently lacking. Nonbenzodiazepine hypnotics (zopiclone, zolpidem) have less adverse effects and similar efficacy to benzodiazepines.

Anti-Anxiety Agents↗