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)

An elderly woman residing in an independent-living retirement community was found dead in the bathtub. She had a history of depression and was prescribed Ambien (generic name zolpidem) for the treatment of insomnia. Two empty prescription bottles of Ambien were found; both were for 10-mg tablets with a total quantity of 60. A postmortem examination was conducted, and blood, urine, and gastric contents were submitted for toxicology screening. The cause of death was drowning. The only remarkable toxicology finding was zolpidem. Quantitative analysis by gas chromatography-mass spectrometry determined the following concentrations of zolpidem: blood, 7.9 micrograms/mL and urine, 4.1 micrograms/mL. A total of 7 mg unabsorbed zolpidem was found in the gastric contents. Our findings report the highest blood concentration of zolpidem reported to date and corroborate other studies that imply that death due solely to overdosage of zolpidem is an unlikely occurrence.
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PMID:A fatality involving zolpidem. 939 27

Zolpidem belongs to a new class of hypnotic agents, chemically distinct from the pre-existing ones, and has a unique neuropharmacological profile. It induces sedative/hypnotic effects in rodents at doses much lower than those for anticonvulsant and myorelaxant activities. Clinically, zolpidem is indicated for the short term treatment of insomnia. It has a short half-life (2.4h), with no active metabolite, and does not accumulate during repeated administration. The pharmacokinetic profile associated with the absence of active metabolites is consistent with the short duration of action and absence of residual effects that have been observed. Polysomnographic experience indicates that zolpidem induces a sleep pattern which is similar to that of physiological sleep, and which produces either no or only minimal effects on sleep architecture after abrupt discontinuation. Aspects of the general safety of zolpidem have been studied in data obtained from healthy volunteers and patients, both adult and elderly, during its clinical development and in post-marketing experience. Zolpidem appears to be well-tolerated in adults and in the elderly, when administered in accordance with prescribing instructions. The available data indicate that, in these circumstances, the risk of abuse or dependence is minimal.
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PMID:The safety and tolerability of zolpidem--an update. 1022 62

Zolpidem, non-benzodiazipine preparation, was used for therapy of 56 patients with insomnia. 4 groups of patients were treated: a) with a prevalence of asthenic symptomatology in psychogenic disorders; b) with polymorphic neurotic symptomatology and autonomic disorders; c) with affective pathology of neurotic level; d) with nervous anorexia and bulimia. Zolpidem was quite effective in all groups of patients in terms of normalization of falling asleep, improvement of quality of sleep without changing of daily activity. A good drug tolerance was found in elderly patients.
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PMID:[Treatment of insomnia in patients with borderline mental diseases]. 1062 29

Zolpidem is one of the newer medications developed for the treatment of insomnia. It is an imidazopyridine agent that is an alternative to the typical sedative-hypnotic agents. Zolpidem use is gaining favor because of its efficacy and its side effect profile, which is milder and less problematic than that of the benzodiazepines and barbiturates used to treat insomnia. Still, side effects are not uncommon with zolpidem use. We report a series of cases in which the patients developed delirium, nightmares and hallucinations during treatment with zolpidem. We will review its pharmacology, discuss previous reports of central nervous system side effects, examine the impact of drug interactions with concurrent use of antidepressants, examine gender differences in susceptibility to side effects, and explore the significance of protein binding in producing side effects.
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PMID:Central nervous system side effects associated with zolpidem treatment. 1068 33

Insomnia is problematic for many individuals, causing them to seek treatment. There is a long history of therapies aimed at restoring normal sleep patterns, each having its advantages and disadvantages. This review traces the history of insomnia drug therapies from chloral hydrate and the barbiturates through the benzodiazepines and explores the newest selective benzodiazepine receptor agonists, including zolpidem and zaleplon. The mechanisms of action of the benzodiazepine receptor agonists are compared and contrasted. A pharmacokinetic comparison is presented showing the importance that parameters such as dose, onset of action, lipophilicity, metabolites, half-life, and receptor-binding affinity have on clinical effects. The possible adverse effects of sleep aids are discussed, including residual sedation and psychomotor impairment, daytime anxiety, anterograde amnesia and cognitive impairment, rebound insomnia, and drug tolerance and dependence. Effects on sleep efficiency and staging are also discussed. Recommendations for the primary care physician on the selection of hypnotics are also provided. Benzodiazepine receptor agonists are often appropriate agents in the treatment of insomnia; however, individual drug and patient considerations are important in matching the most appropriate agent to the individual patient. Zolpidem and zaleplon, newer selective benzodiazepine receptor agonists, offer additional treatment options.
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PMID:Nonselective and selective benzodiazepine receptor agonists--where are we today? 1075 7

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 very frequent complaint /periodically or permanently it affects about 35% of the population/ and is a serious sociological problem. This term covers at least four types of sleep disorders: difficult falling asleep, frequent awakening, too early awakening and impairment of sleep quality--sleep quantitatively sufficient but failing to produce a feeling of rest. Insomnia may be sporadic, short-lasting and chronic. The last type requires particularly medical assistance since impairment of sleep quality can lead to drug dependence. In every case of insomnia it should be tried to explain its cause /neurosis, depression, somatic diseases with symptoms leading to sleep disturbances, toxic factors such as alcohol, drugs, inappropriate sleep hygiene etc./. In the treatment the basic role is played by removal of causes and better observation of sleep hygiene. Hypnotic drugs are indicated in sporadic and short-lasting insomnia, but in chronic insomnia they should be used cautiously and not continuously. Barbiturates have been abandoned recently and benzodiazepines have replaced them. They are, however, fraught with numerous faults. Cyclopyrolones /Zolpidem, Zopiklon/ are the new generation of hypnotic drugs in which the negative features of benzodiazepines have been partly excluded. Their half-life is short, they cause no rebound effect, adverse effects are better tolerated and are less frequent, drug dependence is not produced.
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PMID:[Insomnia and its treatment]. 1110 64

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

(1) Loss of efficacy can occur after a few weeks of treatment with zolpidem and zopiclone. This is not a reason to increase the dose. (2) Zolpidem and zopiclone carry a risk of dependence and of potentially severe disorders (e.g. seizures) during withdrawal. (3) The risk-benefit ratio of benzodiazepines and related drugs (zopiclone and zolpidem) remains more favourable than that of other drugs used in insomnia. However, first-line treatment of sleep disorders should not necessarily be drug-based.
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PMID:Hypnotic dependence: zolpidem and zopiclone too. 1150 51

A recent report showed that zolpidem (CAS 82626-48-0) can lead to the arousal of a semi-comatosed patient. Zolpidem is clinically used for the treatment of insomnia. It belongs to the imidazopyridine chemical class and is a non benzodiazepine drug. It illicits its pharmacological action via the GABA receptor system through stimulation of particularly the omega 1 receptors. In this study, the effect of zolpidem on brain perfusion was examined by 99mTc hexamethyl-propylene amine oxime (HMPAO) split dose brain SPECT on four normal baboons and in one baboon with abnormal neurological behaviour. The global and regional brain perfusion was not significantly affected in the normal brains. In some regions of the abnormal baboon brain, however, there was a disproportionate increase in perfusion after zolpidem.
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PMID:Measurement of cerebral perfusion after zolpidem administration in the baboon model. 1155 20


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