Zolpidem

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Summary sheet: Zolpidem

Zolpidem (Brand names Ambien, Intermezzo, Edluar, and Zolpimist) is a non-benzodiazepine hypnotic used in the treatment of insomnia. It is an imidazopyridine agonist of the GABA_A receptor.

However, when this compound is taken at doses which far exceed the prescriptions nightly dose, this compound can become a powerfully and notoriously bizarre a-typical hallucinogen with subjective properties comparable to that of dissociatives, deliriants and psychedelics

Zolpidem is known colloquially as a "Z-drug." Other Z-drugs include zaleplon (Sonata) and zopiclone. They were initially thought to be less addictive and/or habit-forming than benzodiazepines. However, this appraisal has shifted somewhat in the last few years as cases of addiction and habituation have been presented. Zolpidem is recommended to be taken on a short-term basis. Daily or continuous use of the drug is not usually advised.

Chemistry

This chemistry section is incomplete. You can help by adding to it.

Pharmacology

This pharmacology section is incomplete. You can help by adding to it.

Zolpidem is an agonist at the GABA A α 1 subunits. Due to its selective binding, zolpidem has very weak anxiolytic, muscle relaxant, and anticonvulsant properties but very strong hypnotic properties.[45] Zolpidem binds with high affinity and acts as a full agonist at the α1-containing GABAA receptors, about 10-fold lower affinity for those containing the α2- and α3- GABAA receptor subunits, and with no appreciable affinity for α5 subunit-containing receptors.[46][47] ω1 type GABAA receptors are the α1-containing GABAA receptors and ω2 GABAA receptors are the α2-, α3-, α4-, α5-, and α6-containing GABAA receptors. ω1 GABAA receptors are found primarily in the brain, whereas ω2 receptors are found primarily in the spine. Thus, zolpidem has a preferential binding for the GABAA-benzodiazepine receptor complex in the brain but a low affinity for the GABAA-benzodiazepine receptor complex in the spine.[48]

Like the vast majority of benzodiazepine-like molecules, zolpidem has no affinity for α4 and α6 subunit-containing receptors.[49] Zolpidem positively modulates GABAA receptors, it is presumed by increasing the GABAA receptor complex's apparent affinity for GABA without affecting desensitization or peak current.[50] Like zaleplon (Sonata), zolpidem may increase slow wave sleep but cause no effect on stage 2 sleep.[51]

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

The physical effects of zolpidem can be broken down into several components.

These are described below and generally include:

• Nausea
• Motor control loss
• Dizziness
• Sedation
• Tactile suppression
• Respiratory depression
• Appetite enhancement
• Muscle relaxation

Cognitive effects

The cognitive effects of zolpidem can be broken down into several components.

It contains cognitive effects which generally include:

• Disinhibition
• Anxiety suppression
• Language suppression
• Information processing suppression
• Thought deceleration
• Amnesia
• Compulsive redosing - Zolpidem may provoke compulsive redosing in equal or greater strength than benzodiazepines. Caution is advised as damaging behaviour has been reported following compulsive redosing.
• Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others. It most commonly occurs at heavy dosages. Experience reports indicate that zolpidem may provoke these delusions in equal or greater strength than benzodiazepines.

Visual effects

The visual effects of zolpidem can be broken down into several components.

• Double vision
• Acuity suppression
• Visual disconnection
• Vaguely defined hallucinations

Auditory effects

• Auditory hallucinations

Toxicity and harm potential

Zolpidem has a low toxicity relative to dose. However, it is [[Toxicity::potentially lethal when mixed with depressants like alcohol or opioids]].

It is strongly recommended that one use harm reduction practices when using this drug.

The acute oral LD50 in rats is 695 mg/kg.

Tolerance and addiction potential

Zolpidem is moderately addictive. A review of 36 human case reports found that reported dependence to zolpidem was lower than that of benzodiazepines.

Withdrawal symptoms or rebound symptoms may occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction. For more information on tapering from zolpidem in a controlled manner, please see this guide while keeping in mind it is intended for benzodiazepines.

Although dependence builds up more slowly than in benzodiazepines, discontinuation from regular recreational doses of zolpidem appear to be as difficult as benzodiazepine discontinuation; it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is also an increased risk of hypertension, seizures, and death. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

• Depressants (1,4-Butanediol, 2-methyl-2-butanol, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - It is dangerous to combine zolpidem with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of zolpidem, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of zolpidem will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of zolpidem per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.

Legal issues

This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it.

• U.S.: Zolpidem is a Schedule IV drug due to evidence that the drug has addictive properties similar to benzodiazepines.
• U.K.: The drug is prescription only.
• Australia: Zopiclone is prescription only.

See also

• Responsible use
• Zopiclone
• Zolpidem (Wikipedia)
• The Ambien Walrus Collection