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

This is a review and update on hypnotics. Insomnia is a symptom of many underlying conditions which have to be evaluated before resorting to medication. Hypnotics are useful for short term treatment. The benzodiazepines have replaced the barbiturates which have a low therapeutic index. The action of benzodiazepines depends on their absorption rate, lipophilicity, half-life and metabolites. They induce sleep, prolonged sleep time and reduced night wakenings. They increase stage 2 sleep, and reduce stage 1, 3, 4 and REM (Rapid Eye Movement) sleep. Flurazepam, triazolam and midaolam are described. The benzodiazepines suffer from many unwanted effects which include tolerance, dependence, withdrawal symptoms, rebound insomnia, hang over effect, alteration of memory process and synergism with ethanol. The ideal hypnotic should be free from these drawbacks. Three new generation hypnotics quazepam, zopiclone and zolpidem are described. Drugs suitable for long term hypnotic medication include antipsychotics, antidepressants and antihistamines.
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PMID:Insomnia: drug treatment. 167 17

Flurazepam, temazepam, and triazolam are compared in terms of initial and short term efficacy, effectiveness during intermediate and long term use, withdrawal effects, and general side effects. The usefulness of temazepam is considerably restricted since the drug is slowly absorbed; peak blood concentrations are not reached until 2 to 3 hours after ingestion. Consequently, while the majority of insomniac patients complain primarily of difficulty falling asleep, temazepam is not effective for this sleep complaint. Further, the drug has an intermediate elimination half-life and induces a significant degree of morning sleepiness (hang-over). Rebound insomnia of a moderate degree occurs with some frequency following withdrawal of temazepam. Triazolam is effective initially and with short term use both for inducing and maintaining sleep. However, much of this effectiveness is lost with continued nightly use over an intermediate period (2 weeks). The drug has a rapid elimination rate; during drug administration, sleep may worsen in the final hours of the night (early morning insomnia), and following drug withdrawal, rebound insomnia is frequent, immediate, and severe. Side effects are frequent and include some morning sleepiness (before tolerance develops) and significant memory impairment and even episodes of amnesia. Triazolam may have a narrow margin of safety in that serious behavioral symptoms have been reported even with a 1-mg dose. Flurazepam is effective both for initiating and maintaining sleep with initial and short term drug administration. Further, its efficacy is maintained not only with intermediate term use but with long term drug use (4 weeks). Flurazepam is a long elimination half-life drug, and there is significant daytime sedation during short term use; with continued use this effect diminishes. Rebound insomnia has not been noted following withdrawal of flurazepam; there is a carry-over effectiveness into the first and second nights of withdrawal, and any withdrawal sleep disturbance would be expected to be infrequent, delayed in appearance, and mild in degree.
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PMID:Sleep laboratory studies of hypnotic drugs: efficacy and withdrawal effects. 613 33

The benzodiazepines are the most effective, safest, and most widely used antianxiety drugs. As a class of drugs, there are few major differences between the various benzodiazepine derivatives. The main distinguishing features are different plasma half-lives and the presence or absence of pharmacologically active metabolites. Plasma half-lives vary considerably, from 2 to 3 hours to more than 100 hours. All benzodiazepines are equally effective in the short term management of anxiety and insomnia, and their classification into 'anxiolytics' and 'hypnotics' is not justified. There are numerous other indications for benzodiazepine use, such as muscle spasm in osteoarthritic conditions, and acute alcohol withdrawal, but the benzodiazepines have no antidepressive or analgesic effects. While there is no good evidence for their long term efficacy in the treatment of anxiety and insomnia, the benzodiazepines are more effective and safer than their main predecessors, the barbiturates. Some of the benzodiazepines, particularly those with long plasma half-lives which are commonly used as hypnotics, have a prolonged duration of action and cause marked 'hang-over' effects. Alcohol enhances the effects of these drugs, and thus can also increase their side effects. Adversely effects such as oversedation, tremor, ataxia and confusion are much more common in elderly patients. Ever since the benzodiazepines were first marketed 20 years ago their use has increased rapidly, and it is now estimated that between 12 and 16% of the adult population in developed countries use tranquillisers at some time each year. However, their overall use has probably diminished somewhat in the last few years. Although their indications are very common, it is possible that some of this extensive usage may be the result of dependence. Until recently, published reports of such dependence were comparatively few. However, withdrawal symptoms have now been demonstrated in a substantial proportion of patients on long term, normal dose benzodiazepine treatment. The abstinence syndrome usually lasts for 8 to 10 days, and is characterised by insomnia, anxiety, loss of appetite and bodyweight, tremor, perspiration, and a host of perceptual disturbances. More serious developments such as epileptic fits and psychosis are probably infrequent during withdrawal from therapeutic doses. The overall incidence of benzodiazepine dependence remains unknown.
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PMID:Rational use of anxiolytic/sedative drugs. 613 9

Current treatment of insomnia with hypnotics, GABA(A) receptor modulators, induces various side effects, including cognitive impairment, motor disturbance, dependence, tolerance, hang-over, and rebound insomnia. Ramelteon (Rozerem) is an orally active, highly selective melatonin MT1/MT2 receptor agonist. Unlike the sedative hypnotics that target GABA(A) receptor complexes, ramelteon is a chronohypnotic that acts on the melatonin MT1 and MT2 receptors, which are primarily located in the suprachiasmatic nucleus. Ramelteon has demonstrated sleep-promoting effects in clinical trials, and coupled with its favorable safety profile and lack of abuse potential or dependence, this chronohypnotic provides an important treatment option for insomnia.
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PMID:[A novel therapeutic drug: ramelteon]. 1976 47