zolpidem
08 »
zolpidem
ZolpidemSystematic (IUPAC) nameN,N,6-trimethyl-2-(4-methylphenyl)-imidazo(1,2-a)pyridine-3-acetamideIdentifiersCAS number82626-48-0ATC codeN05CF02PubChem5732DrugBankAPRD00095ChemSpider5530Chemical dataFormulaC19H21N3O Mol. mass307.395 g/molSMILESeMolecules & PubChemPharmacokinetic dataBioavailability70% (oral) 92% bound in plasmaMetabolismHepatic CYP34AHalf life2 to 2.6 hoursExcretion56% renal34% fecalTherapeutic considerationsPregnancy cat.B3(AU) B(US)Legal statusSchedule IV(US) Class C / POM (UK)RoutesOralZolpidem is a prescription medication used for the short-term treatment of insomnia, as well as some brain disorders. It is a short-acting nonbenzodiazepine hypnotic that potentiates gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, by binding to gamma-aminobutyric acid (GABAA) receptors at the same location as benzodiazepines. It works quickly (usually within 15 minutes) and has a short half-life (2–3 hours). Some trade names of zolpidem are: Ambien, Hypnogen, Ivadal, Lunata, Myslee, Nimadorm, Nitrest, Sanval, Somit, Stella, Stilnoct, Stilnox, Zoldem, Zodorm, Zolfresh, and Zolt.Its hypnotic effects are similar to those of the benzodiazepine class of drugs, but it is molecularly distinct from the classical benzodiazepine molecule and is classified as an imidazopyridine. Flumazenil, a benzodiazepine receptor antagonist, which is used for benzodiazepine overdose, can also reverse zolpidem's sedative/hypnotic effects.As an anticonvulsant and muscle relaxant, the beneficial effects start to emerge at 10 and 20 times the dose required for sedation, respectively. For that reason, it has never been approved for either muscle relaxation or seizure prevention. Such drastically increased doses are more inclined to induce one or more negative side-effects, including hallucinations and/or amnesia. (See below.)The patent 4382938 in the United States on zolpidem was held by the French pharmaceutical corporation Sanofi-Aventis. On April 23, 2007 the U.S. FDA approved 13 generic versions of zolpidem tartrate. Zolpidem is available from several generic manufacturers in the UK, as a generic from Sandoz in South Africa, as well as from other manufacturers such as Ratiopharm.Recently, zolpidem has been cited in various medical reports mainly in the United Kingdom as waking persistent vegetative state (PVS) patients, and dramatically improving the conditions of people with brain injuries.// UsesZolpidem is approved for the short-term (usually two to six weeks) treatment of insomnia, and it has been studied for nightly use up to six months in a single-blind trial published in 1991, an open-label study lasting 180 days published in 1992 (with continued efficacy in patients who had kept taking it as of 180 days after the end of the trial), and in an open-label trial lasting 179 days published in 1993.The United States Air Force uses zolpidem as a substitute for temazepam, under trade name Ambien, as "no-go pills" to help pilots sleep after a mission; the main drug used for the purpose is temazepam (Normison/Restoril). (Cf. the "go-pills" dextroamphetamine, served under the name Dexedrine, or its recent modafinil (Provigil) replacement, act as a stimulant for the same pilots, the effects of which are reversed by the aforementioned "no-go pills")Zolpidem is also used off-label to treat restless leg syndrome, and, as is the case with many prescription sedative/hypnotic drugs, it is sometimes used by stimulant users to "come down" after the use of stimulants such as amphetamines (including methamphetamine), cocaine, and MDMA (ecstasy).Recently, the drug has been reported anecdotally to have positive effects for patients in persistent vegetative state. Results from phase IIa trials are expected in June 2007. The trials are being conducted by Regen Therapeutics of the UK, who have a patent pending on this new use for Zolpidem.A clinical trial on a single patient performed at the Toulouse University Hospital using PET shows that zolpidem repeatably improves brain function and mobility of a patient immobilized by akinetic mutism caused by hypoxia. Mechanism of actionZolpidem binds with high affinity to the α1 containing GABAA receptors, about 10-fold lower affinity for those containing the α2, α3-GABAA receptor subunits, and with no appreciable affinity for α5 subunit containing receptors.Like the vast majority of benzodiazepine-like molecules, zolpidem has no affinity for α4 and α6 subunit-containing receptors. Zolpidem positively modulates GABAA receptors, probably by increasing the GABAa receptor complexes apparent affinity for GABA, without affecting desensitization or peak current. Zolpidem increases slow wave sleep and caused no effect on stage 2 sleep in laboratory tests.A meta-analysis of the randomised controlled clinical trials that compared benzodiazepines against Z drugs has shown that there are few consistent differences between zolpidem and benzodiazepines in terms of sleep onset latency, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia, and daytime alertness. New researchZolpidem has recently been very strongly related to certain instances of patients in a minimally conscious coma state being brought to a fully conscious state. While it was initially given to these supposed permanent coma patients to put them to sleep, it actually brought them to a fully conscious state in which they were capable of communicating and interacting for the first time in years. CT scans have shown that the use of the drug actually does dramatically increase the activity in the frontal lobe of the brain in some patients in a minimally conscious state. Large-scale studies are currently being done to see whether it has the same universal effect on all or most patients in a minimally conscious state. It may be that zolpidem's ability to stimulate the brain, particularly in the semi-comatose, may be related to one of its side-effects, which sometimes causes sleepwalking and other activity while asleep, that appears to observers to be fully conscious activity. Recreational use and abuseThe neutrality of this section is disputed.Please see the discussion on the talk page. (December 2007)Please do not remove this message until the dispute is resolved.The transition from medicinal use to recreational use of zolpidem can occur when the drug is used without the doctor's recommendation to continue using it, in high doses (more than the usual 5mg or 10 mg), when consumed other than orally (snorting or injecting), or when taken for purposes other than as a sleep aid. Abuse is more prevalent in those that have been dependent on other drugs in the past. Zolpidem effects can increase and intensify if mixed with other substances like alcohol and cannabis.In the U.S., recreational use of this drug is becoming more common in young people. Recreational users claim that "fighting" the effects of the drug by forcing themselves to stay awake will sometimes cause vivid visuals and a body high (see side-effects below). However, others who are already in an anxious state, claim it is not hard to fight the main effect of sedation, experiencing the side-effect of euphoria more than the sedation itself. Thus, some users report decreased anxiety, and even mild euphoria, as well as perceptual changes, visual distortions, and light-based hallucinations. It is also not uncommon for one that has developed a tolerance to the drug to eventually feel such a decrease in the sedation effect that only the euphoric, perceptual, and anxiety decreasing side-effects remain.With regular use at high dosage, there can be a risk of a severe physical dependence on zolpidem, with cases being reported in the medical literature of epileptic seizures forming part of the withdrawal syndrome. One case involved a woman detoxing off a high dose of zolpidem experiencing a generalized seizure. The clinical withdrawal and dependence effects were reported to be similar to those of benzodiazepines in this case report.Zolpidem and other sedative hypnotic drugs are detected frequently in cases of people suspected of driving under the influence of drugs. Other drugs including the benzodiazepines and zopiclone are also found in high numbers of suspected drugged drivers. Many drivers have blood levels far exceeding the therapeutic dose range suggesting a high degree of excessive-use potential for benzodiazepines, zolpidem and zopiclone.As Ambien's patent expired April 21, 2007, new generic versions were approved, which do not have the "protective cover" present on the Sanofi name-brand Ambien they once previously had to prevent users from crushing, snorting, or injecting the drugs. Dependence and withdrawalAlcohol has cross tolerance with GABAa receptor positive modulators such as the benzodiazepines and the nonbenzodiazepine drugs. For this reason alcoholics or recovering alcoholics may be at increased risk of physical dependency on zolpidem. Also, alcoholics and drug abusers may be at increased risk of abusing and or becoming psychologically dependent on zolpidem. Zolpidem should be avoided in those with a history of Alcoholism, drug misuse, or in those with history of physical dependency or psychological dependency on sedative-hypnotic drugs. OverdoseOverdose of zolpidem may present with excessive sedation, pin-point pupils, depressed respiratory function, which may progress to coma and possibly death. Zolpidem combined with alcohol, opiates or other CNS depressants may be even more likely to lead to fatal overdoses. Zolpidem overdosage can be treated with the benzodiazepine receptor antagonist flumazenil, which displaces zolpidem from its binding site the benzodiazepine receptor and therefore rapidly reverses the effects of zolpidem.Long term use of Ambien (or its time-release formula, Ambien CR) may require a dose adjustment. This adjustment helps those using Ambien to minimize or eliminate withdraw effects such as r
Stilnox & Zolpidem appear to be 'bad news' drugs with serious side effects, and should be banned.Buy cheap zolpidem tartrate online zolpidem ONLINE! DISCOUNTS UP TO 70%!!! SPECIAL OFFERS. Here you will see some tips for using ambien zolpidem tartrate if you have insomnia."Stilnox (zolpidem, or Ambien in the US) has been causing weird sleep activity in Australia.Drug zolpidem led to a dramatic improvement in the patient, almost completely disabled due to brain damage after an unsuccessful suicide attempts, reports New Scientist. A man took Stilnox at home and later found himself lying on a woman's couch wearing a dress. (direct link & more detailed than other articles submitted)"The common sleeping pill zolpidem, sold in the US under the name Ambien, can reverse serious brain damage and wake up patients in persistent vegetative states!When given to a man who had been vegetative, "I sat by his bed for 25 minutes, and then he made a sound like 'mmm'. UK and Australian health agencies have released information about 240 cases of odd occurrences, including sleepwalking, amnesia and hallucinations among people taking the drug zolpidem.. One woman woke up with a paintbrush in her hand after having painted the front door. Will drug giant
Even more about zolpidem
zolpidem
Zolpidem is a prescription medication used for the short-term treatment of insomnia, as well as some brain disorders. It is a short-acting nonbenzodiazepine hypnotic that ...
Zolpidem - Wikipedia, the free encyclopedia
Read about the medication zolpidem (Ambien), a drug used as a sleeping pill to treat insomnia. Side effects, drug interactions, warnings, and precautions are included in the ...
zolpidem (Ambien, Sleeping Pill) drug class, medical uses, medication ...
sleep ... This Journal has been read times since its creation on June 20, 2007
zolpidem
Zolpidem ... Why is this medication prescribed? Return to top. Zolpidem is used to treat insomnia (difficulty falling asleep or staying asleep).
MedlinePlus Drug Information: Zolpidem
zolpidem - Safe, Private&Convenient Zolpidem. US ... ... Brand names Why is this medication prescribed? Recycle limitless conditions.
Comment:
