Zolpidem

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Fatal overdose may occur when GABAergic substances are combined with other depressants such as opiates, benzodiazepines, barbiturates, gabapentinoids, thienodiazepines or alcohol.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Summary sheet: Zolpidem
Zolpidem
Zolpidem.svg
Chemical Nomenclature
Common names Ambien, Intermezzo, Edluar, Zolpimist
Substitutive name Zolpidem
Systematic name N,N-dimethyl-2-(6-methyl-2-p-tolylimidazo[1,2-a]pyridin-3-yl)acetamide
Class Membership
Psychoactive class Depressant / Hallucinogen
Chemical class Imidazopyridine
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold 5 mg
Light 10 - 20 mg
Common 20 - 30 mg
Strong 30 - 50 mg
Heavy 50 mg +
Duration
Total 5 - 10+ hours
Onset 15 - 45 minutes
Come up 30 - 45 minutes
Peak 3 - 6 hours
Offset 4 - 5 hours
After effects 2 - 4 hours









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Interactions


Zolpidem (also known as Ambien, Intermezzo, Edluar, Stilnoct, Stilnox, Zolpimist[2], and others) is a non-benzodiazepine hypnotic of the imidazopyridine chemical class which is primarily used in the treatment of insomnia.[2][3]

When taken at recreational doses, it reportedly produces powerful and notoriously bizarre atypical hallucinogenic, dissociative, deliriant and even psychedelic effects.

Zolpidem is a member of a family colloquially known as a "Z-drug." Other Z-drugs include zaleplon (Sonata) and zopiclone (Imovane). These drugs were initially thought to be less addictive and/or habit-forming than benzodiazepines. However, this evaluation has shifted in the last few years as cases of addiction and habituation have accumulated.[citation needed]

Zolpidem should not be taken on a full stomach and it is recommended on a short-term basis only. Daily or continuous use of the drug is not usually advised.

Chemistry

Zolpidem is a hypnotic nonbenzodiazepine drug of the imidazopyridine class. This class of drugs is named for having an imidazole constituent, a five-membered ring with two non-adjacent nitrogen constituents fused to a pyridine ring, a six-membered nitrogenous ring which shares a nitrogen with the imidazole group.

GABAA-agonizing imidazopyridines such as zolpidem are often grouped with pyrazolopyrimidines, and cyclopyrrones under the label "nonbenzodiazepines" for their similar effects.

Three syntheses of zolpidem are common. 4-methylacetophenone is used as a common precursor. This is brominated and reacted with 2-amino-5-methylpyridine to give the imidazopyridine. From here the reactions use a variety of reagents to complete the synthesis, either involving thionyl chloride or sodium cyanide. These reagents are challenging to handle and require thorough safety assessments.[4] Though such safety procedures are common in industry, they make clandestine manufacture difficult.

A number of major side-products of the sodium cyanide reaction have been characterised and include dimers and mannich products.[5]

Pharmacology

Zolpidem interacts with the GABA-BZ receptor system[6] and shares some of the pharmacological properties of traditional benzodiazepines.

In contrast to benzodiazepines, which non-selectively bind to and activate all BZ receptor subtypes among others, zolpidem binds to the BZ1 receptor preferentially with a high affinity ratio of the α1/α5 subunits. It's this selective binding in comparison to traditional benzodiazepines that gives zolpidem very weak anxiolytic, muscle relaxant, and anticonvulsant properties but very strong hypnotic or sedative properties.[7]

As the GABA site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming) effects of zolpidem on the nervous system.

In regards to how the consumption of this compound results in its bizarre hallucinations, the pharmacological mechanics behind this are not understood and do not seem to have been directly studied. It is worth noting, however, that zolpidem may share similar mechanisms as a GABAA receptor agonist to that of muscimol, which is the active compound within the hallucinogenic amanita muscaria mushroom.

Subjective effects

The subjective effects of zolpidem seem to vary wildly between individuals with certain users experiencing a complete lack of hallucinations whilst others experience them even at lower dosages. Generally, a recreational zolpidem dose has features comparable to DXM, DPH, alprazolam and psilocin.

It contains many of the physical and cognitive effects of benzodiazepines with a moderately dissociated headspace most similar to that of DXM. This occurs alongside bizarre thought patterns and external hallucinations similar to those of deliriants and visual distortions most similar to those of psychedelics. Overall, this makes zolpidem an extremely unique and unpredictable hallucinogen which requires a trip sitter.

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

Physical effects
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Disconnective effects
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Visual effects
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Cognitive effects
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Auditory effects
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Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

Additional experience reports can be found here:

Toxicity and harm potential

Zolpidem has a low toxicity relative to dose.[11] However, it is potentially lethal when mixed with depressants like alcohol or opioids.

Zolpidem has been reported to cause psychosis, delusions and delirium at a significantly higher rate than other hallucinogens like LSD, ketamine, or DMT. There are a large number of experience reports online which describe states of delirium, amnesia, bizarre behavior,[12] sleep walking,[13] driving while impaired[13][14] and other serious consequences after abusing the drug. In many cases this has resulted in hospitalization, arrests,[15] car crashes,[16] lengthy court cases and even death.[17]

It is strongly recommended that one use harm reduction practices and have a trip sitter when using this drug.

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.[18]

Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.[19] 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;[19] it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of hypertension, seizures, and death.[20] 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, benzodiazepines)- 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 status

Internationally, zolpidem is a Schedule IV substance under the Convention on Psychotropic Substances.[21]

  • Australia: Zolpidem is only available by prescription.[citation needed]
  • Canada: Zolpidem is only available by prescription.[citation needed]
  • Germany: Zolpidem is a controlled substance under Anlage III of the BtMG. It can only be prescribed on a narcotic prescription form. There is an exception for oral preperations, containing up to 8,5mg zolpidem per unit, which can be prescribed on a regular prescription form.[22]
  • Netherlands: Zolpidem is only available by prescription.[citation needed]
  • Russia: In Russia, since 2013, zolpidem is a Schedule III controlled substance.[23]
  • Switzerland: Zolpidem is a controlled substance specifically named under Verzeichnis B. Medicinal use is permitted.[24]
  • United Kingdom: Zolpidem has been a class C drug in the UK since 2003.[25] It is illegal to possess (without a legitimate prescription), supply, produce or import.[citation needed]
  • United States: Zolpidem is listed as a Schedule IV drug due to evidence that the drug has addictive properties similar to benzodiazepines.[citation needed]

See also

External links

References

  1. Risks of Combining Depressants - TripSit 
  2. 2.0 2.1 http://www.drugs.com/zolpidem.html | Zolpidem (Drugs.com)
  3. Du, B., Shan, A., Zhong, X., Zhang, Y., Chen, D., Cai, K. (March 2014). "Zolpidem Arouses Patients in Vegetative State After Brain Injury: Quantitative Evaluation and Indications". The American Journal of the Medical Sciences. 347 (3): 178–182. doi:10.1097/MAJ.0b013e318287c79c. ISSN 0002-9629. 
  4. Johnson, D. S., Li, J. J., eds. (2007). The art of drug synthesis. Wiley-Interscience. ISBN 9780471752158. 
  5. Sumalatha, Y., Reddy, P. P., Reddy, R., Satyanarayana, B. (7 April 2009). "Synthesis and spectral characterization of zolpidem related substances - hypnotic agent". Arkivoc. 2009 (7): 143–149. doi:10.3998/ark.5550190.0010.714. ISSN 1551-7012. 
  6. Kovacic, P., Somanathan, R. (2009). "Zolpidem, a clinical hypnotic that affects electronic transfer, alters synaptic activity through potential GABA receptors in the nervous system without significant free radical generation". Oxidative Medicine and Cellular Longevity. 2 (1): 52–57. ISSN 1942-0900. 
  7. Salvà, P., Costa, J. (September 1995). "Clinical pharmacokinetics and pharmacodynamics of zolpidem. Therapeutic implications". Clinical Pharmacokinetics. 29 (3): 142–153. doi:10.2165/00003088-199529030-00002. ISSN 0312-5963. 
  8. DeNoon, D. J., Ambien Linked to “Sleep Eating” 
  9. Ambien, delusions, and violence: Is there a link?, Psychology Today 
  10. Side Effects of Ambien (Zolpidem Tartrate), Warnings, Uses 
  11. PubChem, Zolpidem 
  12. /r/ambien (reddit) | https://www.reddit.com/r/ambien/top/
  13. 13.0 13.1 Hoque, R., Chesson, A. L. (15 October 2009). "Zolpidem-Induced Sleepwalking, Sleep Related Eating Disorder, and Sleep-Driving: Fluorine-18-Flourodeoxyglucose Positron Emission Tomography Analysis, and a Literature Review of Other Unexpected Clinical Effects of Zolpidem". Journal of Clinical Sleep Medicine : JCSM : Official Publication of the American Academy of Sleep Medicine. 5 (5): 471–476. ISSN 1550-9389. 
  14. http://www.nhcriminaldefense.com/auto_accident_injury.html
  15. Passengers recount horror as Air Force vet threatens to bring down transatlantic Delta flight 
  16. News, A. B. C., Kerry Kennedy Says Ambien “Overtook” Her, Causing Car Crash 
  17. The Disturbing Side Effect Of The No. 1 Prescription Sleep Aid, 2014 
  18. Hajak, G., Müller, W. E., Wittchen, H. U., Pittrow, D., Kirch, W. (October 2003). "Abuse and dependence potential for the non-benzodiazepine hypnotics zolpidem and zopiclone: a review of case reports and epidemiological data: Abuse and dependence of zolpidem and zopiclone". Addiction. 98 (10): 1371–1378. doi:10.1046/j.1360-0443.2003.00491.x. ISSN 0965-2140. 
  19. 19.0 19.1 Sethi, P. K., Khandelwal, D. C. (February 2005). "Zolpidem at supratherapeutic doses can cause drug abuse, dependence and withdrawal seizure". The Journal of the Association of Physicians of India. 53: 139–140. ISSN 0004-5772. 
  20. Lann, M. A., Molina, D. K. (June 2009). "A fatal case of benzodiazepine withdrawal". The American Journal of Forensic Medicine and Pathology. 30 (2): 177–179. doi:10.1097/PAF.0b013e3181875aa0. ISSN 1533-404X. 
  21. "List of psychotropic substances under international control (Green List)" (PDF) (23rd ed.). International Narcotics Control Board (INCB). August 2003. Archived from the original (PDF) on March 2, 2007. 
  22. Anlage III BtMG - Einzelnorm 
  23. Постановление Правительства РФ от 04.02.2013 N 78 “О внесении изменений в некоторые акты Правительства Российской Федерации” - КонсультантПлюс 
  24. "Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien" (in German). Bundeskanzlei [Federal Chancellery of Switzerland]. Retrieved January 1, 2020. 
  25. The Misuse of Drugs Act 1971 (Modification) Order 2003