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

Zolpidem is a nonbenzodiazepine hypnotic agent belonging to a new class of psychotropic drugs the imidazopyridines which enhance the GABAA receptor function by interacting with a specific receptor population. Zolpidem binds selectively to the Omega-1 receptor subtype and from a pharmacological point of view differs from benzodiazepines (BZD) by producing a strong sedative and hypnotic profile which predominates over the anticonvulsivant and anxiolytic activity and moreover appears practically devoid of myorelaxant properties. From a pharmacodynamic point of view, these results suggest that zolpidem facilitates more selectively than BZD, GABAA function and produces a selective hypnotic effect. Though if the role played by receptors in tolerance and dependence has not been yet fully elucidated, it could be described as an adaptative process to sustained stimulation of GABA function. Animal data obtained with zolpidem differs substantially from that of the BZD and indicates that repeated zolpidem administration may not lead to phenomena of tolerance and withdrawal syndrome after abrupt drug discontinuation. In human following oral intake, zolpidem is very rapidly (Tmax: 30-40 min) absorbed. The clearance is essentially metabolic and less than 1% is recovered in urine. The apparent plasma half-life is of 2.0-2.5 hours in most adult subjects and metabolites are totally inactive. The hypnotic activity of zolpidem and its effects on sleep architecture have been assessed in polysomnographic studies: 11 studies in 579 healthy volunteers and 12 studies in 202 insomniac patients. From all the patient studies, it emerges clearly that zolpidem at the dose of 10 mg significantly decreases sleep onset latency, the number and the duration of nocturnal awakenings, and concomitantly increases total sleep time. Furthermore, at variance with what observed with reference benzodiazepine hypnotics, zolpidem does not alter patient sleep architecture: it increases only moderately stage 2, it increases, when reduced, stages 3 and 4 (slow wave sleep) and it does not decrease REM sleep. Clinical studies conducted on more than 4,000 insomniac patients have clearly shown that at the dose of 10-20 mg, zolpidem induces from the first night a definite hypnotic effect in all types of insomnia. In elderly subjects an initial dose of 5 mg should be considered. The possible presence of residual effects during the day following administration of zolpidem has been assessed in 535 healthy volunteers and in 133 insomniac patients according to a double blind (versus placebo and/or benzodiazepine) controlled design.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Contribution of zolpidem in the management of sleep disorders]. 136 57

The efficacy and tolerability of the imidazopyridine hypnotic, zolpidem, were investigated in 119 elderly psychiatric in-patients complaining of insomnia in a double-blind, parallel-group, placebo-controlled trial. After a 7-day placebo washout period, patients were randomized to receive 10 or 20 mg/day zolpidem, or placebo for 21 days; thereafter, all patients received placebo for 7 days. Sleep was assessed by patient observation on days 0, 1, 7, 14, 21, 22 and 28. Compared with placebo, 20 mg/day zolpidem significantly improved total duration of sleep between day 0 and day 21, and this was maintained at day 28. After 10 or 20 mg/day zolpidem, there was also a trend towards improvement in all other sleep parameters, which remained above baseline at day 28. Zolpidem was well tolerated with no withdrawal symptoms during the second 7-day placebo treatment period. Daytime drowsiness was reported in three patients receiving 20 mg/day zolpidem and in one receiving 10 mg/day zolpidem, but there was no significant increase in daytime drowsiness between days 0 and 21. Ataxia occurred in two, one and one patient, respectively, treated with 20 mg/day zolpidem, 10 mg/day zolpidem and placebo. The incidences of other adverse events or effects on clinical and laboratory parameters were minimal and similar in all three treatment groups. It is concluded that, in elderly psychiatric patients, 10 mg/day zolpidem can be used to treat insomnia and can be safely added to concomitant psychotropic treatment without inducing daytime drowsiness.
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PMID:A double-blind, comparative study of zolpidem and placebo in the treatment of insomnia in elderly psychiatric in-patients. 152 71

The safety and efficacy of 10 or 20 mg/day zolpidem, a new hypnotic belonging to the imidazopyridine class, were studied over a 180-day period in 96 patients with sleep disorders. The treatment was continued for a further 180 days by 49 of these patients. Follow-up information from 21 patients who discontinued treatment after 180 days showed no rebound insomnia or withdrawal signs. Efficacy of treatment with respect to reduction of sleep onset latency and number of nocturnal wakenings, and improvement in duration of sleep, quality of sleep and morning wakenings was found in nearly 90% of patients and was maintained in those patients who continued treatment for 360 days. This efficacy was achieved with a stable percentage of patients receiving 10 mg/day and 20 mg/day zolpidem from day 30 to the final visit. Zolpidem, therefore, has been shown to be an effective and safe hypnotic, and to be devoid of rebound and withdrawal effects.
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PMID:The safety and efficacy of zolpidem in insomniac patients: a long-term open study in general practice. 152 72

Eighteen non-pregnant woman complaining about insomnia were polysomnographically investigated for 3 nights with weekly intervals. They received placebo, 2 mg flunitrazepam or 10 mg zolpidem according to a cross-over double blind design. The patients were selected by general practitioners on the basis of subjective complaints. Zolpidem is a recently introduced short-acting imidazopyridine hypnotic, binding to a subunit of the benzodiazepine 1 receptor. Flunitrazepam is a well-known hypnotic, binding to both the benzodiazepine 1 and 2 receptor subtypes. Objective recording did not substantiate the subjective complaint of insomnia. Sleep patterns during placebo differed only little from that expected from age matched healthy persons. Both flunitrazepam and zolpidem significantly shortened sleep onset (5 min of continuous sleep beginning with NREM 1 sleep). The sleep composition following flunitrazepam was characterized by an increase in NREM 2, a prolongation of the time of REM sleep, a reduction of REM sleep and an increase in NREM 3-4 sleep during the first 2 h of sleep. The sleep composition following zolpidem resembled more than seen in persons without sleep complaints. However, as compared to placebo, there was a decrease of the time spent awake during sleep and an increase in NREM 3-4 during the first 2 of sleep.
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PMID:Effects of zolpidem and flunitrazepam on nocturnal sleep of women subjectively complaining of insomnia. 157 23

A 3-hour phase advance of sleep time was employed to produce a model of transient insomnia. The degree to which this manipulation was effective varied substantially among young, healthy normal sleepers. Zolpidem, an imidazopyridine hypnotic compound, was effective in reversing the sleep disruption in those individuals displaying transient insomnia in this model.
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PMID:Transient insomnia associated with a 3-hour phase advance of sleep time and treatment with zolpidem. 219 96

Zolpidem is an imidazopyridine, a chemically novel nonbenzodiazepine hypnotic agent which acts at the benzodiazepine omega 1-receptor subtype in the brain. With a rapid onset of action and short elimination half-life, it reduces the latency to and prolongs the duration of sleep in patients with insomnia, yet has no major effects on sleep stages when given in dosages of 5 to 20 mg nightly. Rebound effects on withdrawal of the drug have not been observed. Unlike benzodiazepines, zolpidem has no myorelaxant or anticonvulsant effects and its effects on anxiety appear to be minor. While zolpidem aids sedation, and may reduce memory or psychomotor function within the first 2 hours after administration of single oral doses, its use as a surgical premedicant remains to be established. Adverse effects are predominantly CNS and gastrointestinal in nature. Altered pharmacokinetics may lead to an increase in dose-proportionate adverse effects in the elderly and in patients with renal dysfunction. Limited evidence to date suggests that the dependence liability of zolpidem is minimal. Thus, zolpidem is an interesting alternative to benzodiazepines in the treatment of insomnia, with properties that potentially offer worthwhile advantages in this therapeutic area if they are confirmed with wider clinical experience.
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PMID:Zolpidem. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential. 222 17

The effect of zolpidem 10 mg p.o. on sleep in patients with persistent psychophysiological insomnia was assessed by polysomnographic recordings. An improvement in sleep with no rebound insomnia was observed during treatment for two weeks. Time awake after the onset of sleep was reduced after one week and increased after two weeks, whereas sleep latency remained reduced. Zolpidem markedly increased the duration of Stage 2 sleep without affecting either slow wave sleep or REM sleep. Subjective evaluation of improvement in sleep was well correlated with sleep laboratory findings. Zolpidem did not impair the immediate memory or psychomotor performance of patients on the morning after its administration. Side-effects during the period of drug administration included drowsiness, fatigue, headache, anxiety and irritability. They were mild or moderate and wore off soon after awakening.
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PMID:Effect of zolpidem on sleep in insomniac patients. 266 41

Effects of an imidazo-pyridine (zolpidem: 10, 20 and 30 mg) on overnight sleep and on performance the next day were studied in young adults and in middle aged individuals. The young adults were used particularly as an homogenous group to establish any possible adverse effects of the drug on sleep and on performance the next day, and the middle aged subjects with their less restful sleep were used to study efficacy. In the young adults zolpidem led to a marked increase in slow wave sleep with a reduction in stage 2 sleep. There were no significant changes in REM sleep, though there was a tendency for REM sleep to be delayed. In the middle aged there was a reduction in awake activity and drowsy sleep with an increase in stage 2 sleep. The latency to REM sleep was increased but the duration of REM sleep over the whole night was not reduced. Digit symbol substitution and a complex reaction time task were used to study performance, but there were no residual effects with zolpidem (9 h after ingestion). Zolpidem is likely to prove useful in the management of transient and short-term insomnia in healthy middle aged individuals when impaired performance the next day is to be avoided.
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PMID:Hypnotic activity of an imidazo-pyridine (zolpidem). 395 37

Transient insomnia may be induced by stress, sleep in unfamiliar surroundings, jet lag and other factors. Zolpidem, a novel imidazopyridine hypnotic, has been shown to have hypnotic properties in most patients without significantly affecting next-day performance. Using the first-night effect in a sleep laboratory as a model of transient insomnia, this placebo-controlled, double-blind, parallel-group study evaluated the efficacy and safety of zolpidem in 462 normal volunteers. Zolpidem was tested at doses of 5, 7.5, 10, 15 and 20 mg, and statistical analysis of 7.5 mg and 10 mg was compared with placebo (unbalanced randomization). Compared with placebo, the 7.5 mg and 10 mg doses of zolpidem decreased sleep latency and increased sleep duration and maintenance (i.e. reduced number of awakenings). Zolpidem (7.5 mg or 10 mg) had no significant effect on next-day psychomotor performance. No statistically significant differences in the overall side-effect profiles were found between 7.5-mg and 10-mg zolpidem dose groups and placebo. This study demonstrates that zolpidem at 7.5 mg and 10 mg is effective in the treatment of transient insomnia.
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PMID:Zolpidem in the treatment of transient insomnia: a double-blind, randomized comparison with placebo. 761 22

In a pilot double-blind trial in 21 patients with learned or idiopathic insomnia (DSM-IIIR), patients received placebo for 1 week (nights 1-7), either active (zolpidem, 10 mg) or placebo treatment for 2 weeks (nights 8-21) and then placebo for a further week (nights 22-28). Variables to measure efficacy, rebound and withdrawal were assessed daily from day 1 to day 28. Polysomnographic recordings together with sleep cycle analysis were performed on nights 7, 21 and 28. Patients treated with 10 mg zolpidem for 2 weeks had significantly improved sleep efficiency at the end of the randomised double-blind phase compared with the placebo group. Fractionated sleep-cycle analysis showed an increase in slow-wave sleep during the first 2-hour cycle after sleep onset. During the withdrawal placebo week, most of the main sleep variables remained relatively stable in the zolpidem group (nights 22-28), and deteriorated further in the placebo group. At the end of the withdrawal phase, there was a statistically significant difference between groups, in favour of the zolpidem treatment, in sleep efficiency, total sleep time, absolute and percentage of time awake, and percentage of REM sleep. REM sleep, which was normal in both groups at baseline, decreased significantly in the placebo group between nights 22 and 28 (during the withdrawal placebo week) compared with the zolpidem treatment group, and the number of periods of time awake increased. Minor subjective complaints were recorded under zolpidem and were comparable with those under placebo. Zolpidem seemed to improve some important sleep variables, when assessed both objectively and subjectively. The sleep cycle analysis suggested a possible shift of slow-wave sleep to an earlier period of the night, with a more physiological sleep structure. There was no evidence for withdrawal or rebound after stopping the 2 weeks of zolpidem treatment, but rather signs that the effect of zolpidem outlasted active treatment. The present pilot study justifies a prospective confirmatory comparison of zolpidem with benzodiazepines in an adequate number of patients and withdrawal after 6-8 weeks of treatment.
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PMID:Pilot controlled double-blind study of the hypnotic effects of zolpidem in patients with chronic 'learned' insomnia: psychometric and polysomnographic evaluation. 814 86


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