CONTAINS ETIZOLAM 0.5 MG
|Molecular structure of Etizolam.|
|Common names||Etizolam, “Etilaam”, “Etizest”|
|Routes of Administration|
Etizolam (also known by the trade names Etilaam, Etizest, among many others) is a synthetic, fast-acting depressant substance of the thienodiazepine chemical class that produces benzodiazepine-like anxiety suppressing, disinhibiting, muscle relaxing, sedating, and memory suppressing effects when administered. Etizolam is commonly administered orally and sublingually due to the efficiency of these routes.
Etizolam is not commonly prescribed and is not recognized as a controlled substance in many parts of the world, which has led to its rise as a popular research chemical substitute for pharmaceutical benzodiazepines, typically those that are sought after for their recreational effects. It is commonly found in pellet or pill form, laid on a blotter sheet, or as a powder.
Anecdotal reports suggest that in terms of its relative potency, 1 mg of etizolam is approximately equivalent to 0.5 mg of alprazolam(common trade name “Xanax”), 0.5 mg of clonazepam (common trade name “Klonopin”), or 10 mg of diazepam (common trade name “Valium”). It is often compared to a less potent and sedating version of alprazolam in terms of the speed of its onset, total duration, and recreational potential.
It should be noted that that as with benzodiazepines, the sudden discontinuation of thienodiazepines can be potentially dangerous or even life-threatening for individuals who have been using the substance regularly for extended periods of time, as it can result in fatal seizures. As a result, individuals who find themselves physically dependent on this substance are highly advised to taper their dose by gradually lowering the amount taken each day over a prolonged period of time instead of stopping their intake abruptly.
Due to the high dependence-forming and addiction potential that this substance shares with members of the closely related benzodiazepine class, as well as its alcohol-like ability to induce dangerous disinhibitory black-out states, it is highly advised to use proper harm reduction practices if choosing to use this substance.
- 1History and culture
- [+]4Subjective effects
- 5Preparation methods
- [+]6Toxicity and harm potential
- 8See also
- 9External links
History and culture
|This History and Culture section is a stub.
As such, it may contain incomplete or wrong information. You can help by expanding it.
Etizolam first appeared as a gray market research chemical in 2011. Since then its popularity has steadily increased. This likely owes itself to both its low cost and its abundance, and the highly dependence-forming and addictive nature that it shares with recreationally-oriented benzodiazepines.
Alhough it is a relatively new research chemical, etizolam differs from most other research chemicals in that it is approved and actively prescribed as a medical treatment for anxiety in many countries around the world, commonly under brand names like Etilaam and Etizest. Its origins as a medical drug are unclear, although medical papers citing its use in the treatment of anxiety have been documented as early as the 1990s.
Etizolam is a structural relative of benzodiazepines, whereby the benzene ring has been replaced by a thiophene ring, classifying it as a thienodiazepine. Thiophene is a five membered aromatic ring with one sulfur atom. Etizolam contains a thiophene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R1 and R4. This forms the thienodiazepine core of etizolam. An ethyl chain is bound to this bicyclic structure at R7. Additionally, a R2‘ chlorine-substituted phenyl ring is bound to this structure at R5.
Etizolam also contains a methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring. Etizolam shares this fused triazole ring substitution with certain benzodiazepine drugs, called triazolobenzodiazepines, distinguished by the suffix “-zolam”.
Thienodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors. As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of etizolam on the nervous system.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include injury or death.
- Sedation– In terms of energy level alterations, this substance has the potential to become very sedating in a rapid-acting fashion. At higher doses, this can lead users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
- Muscle relaxation
- Physical euphoria
- Motor control loss
- Respiratory depression
- Increased libido
- Seizure suppression
- Appetite enhancement– This effect is not particularly prominent, but is reported to occur in some people. It can have a synergistic effect when combined with cannabis.
- Temporary erectile dysfunction
- Note:The following references benzodiazepines specifically, but due to the close structural and pharmacological similarities they share, can be taken to apply to thienodiazepines like etizolam as well.
Paradoxical reactions to benzodiazepines such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).
- Anxiety suppression
- Cognitive euphoria– This effect is generally produced only at high doses, and is thought to arise largely from the release of pre-existing anxiety in the user. Many users report not feeling any pleasurable or euphoric sensations from benzodiazepines or thienodiazepines like etizolam at all.
- Compulsive redosing– This component is likely due to the rapid way in which the substance produces its anxiety-relieving, relaxing and sometimes euphoric effects before quickly dropping off. It can be made worse due to the memory suppression it produces which can lead the user forgetting they have taken any at all, which can lead to a cycle that leads to a dangerous amnesicblackout state.
- Memory suppression
- 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 high to heavy dosages.
- Analysis suppression
- Ego inflation
- Thought deceleration
- Motivation suppression
- Emotionality suppression– Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but less intensive than that of antipsychotics.
- Rebound anxiety– Rebound anxiety is a commonly observed effect with anxiety relieving substances like benzodiazepines and etizolam. It typically corresponds to the total duration spent under the substance’s influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction.
- Dream potentiationor Dream suppression
- Residual sleepiness– While etizolam can be used as an effective sleep-inducing aid, its effects may persist into the morning afterwards, which may lead users to feeling “groggy” or “dull” for up to a few hours.
- Thought deceleration
- Thought disorganization
There are currently anecdotal reports which describe the effects of this compound within our experience index.
- Experience:20mg Etizolam – Smoking Etizolam
- Experience:2mg Etizolam – Here be dragons
- Experience:3mg Etizolam – A Comedown Drug
. Additional experience reports can be found here:
- Volumetric liquid dosing– If one’s thienodiazepines are in powder form, it is unlikely to be able to be weighed out accurately without expensive, lab-grade analytical scales due to their milligram-range potency. To avoid the risks of overdose, one can dissolve the thienodiazepine into a carrier solution (such as propylene glycol or vegetable glycerin) to ensure a more accurate administration of the intended dose.
Toxicity and harm potential
Further information: Research chemicals § Toxicity and harm potential
It is strongly recommended that one use harm reduction practices when using this substance.
Tolerance and addiction potential
Etizolam is extremely physically and psychologically addictive. When multiple doses of etizolam, or lorazepam, were administered to rat neurons, lorazepam caused downregulation of alpha-1 benzodiazepine binding sites (tolerance/dependence), while etizolam caused an increase in alpha-2 benzodiazepine binding sites (reverse tolerance to anti-anxiety effects). Tolerance to the anticonvulsant effects of lorazepam was observed, but no significant tolerance to the anticonvulsant effects of etizolam was observed. Etizolam therefore has a reduced liability to induce tolerance, and dependence when compared with classic benzodiazepines.
Tolerance will, however, develop to the sedative-hypnotic effects within a couple of days of continuous use. After cessation, the tolerance returns to baseline in 7 – 14 days. However, in certain cases this may take significantly longer in a manner which is proportional to the duration and intensity of one’s long-term usage.
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. For more information on tapering from thienodiazepines in a controlled manner, please see this guide.
Thienodiazepine discontinuation is notoriously difficult; 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 seizure following discontinuation of thienodiazepines. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.
Thienodiazepine overdose may occur when it is taken in extremely heavy quantities or concurrently with other depressants. This is particularly dangerous with other GABAergic depressants such as barbiturates and alcohol since they work in a similar fashion, but bind to distinct allosteric sites on the GABAA receptor, thus their effects potentiate one another. Thienodiazepine increase the frequency in which the chlorine ion pore opens on the GABAA receptor while barbiturates increase the duration in which they are open, meaning when both are consumed, the ion pore will open more frequently and stay open longer. Thienodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly.
Symptoms of a thienodiazepine overdose may include severe thought deceleration, slurred speech, confusion, delusions, respiratory depression, coma or death. Thienodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Thienodiazepine overdoses are sometimes treated with flumazenil, a GABAAantagonist, however care is primarily supportive in nature.
Although many psychoactive substances 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 thienzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants mask the sedative effect of thienzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of thienzodiazepines will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dose a certain amount of thienzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.
|This legality section is a stub.
As such, it may contain incomplete or wrong information. You can help by expanding it.
- United States:In August 2014, a Connecticut man was charged with driving under the influence and the possession of etizolam. In the same month, the state of Arkansas listed etizolam as a Schedule I drug under their drug scheduling guidelines.
- Germany:Phenazepam and etizolam were controlled in Germany in July 2013.
- Poland:Etizolam may be scheduled under the Act on Counteracting Drug Addiction and the State Sanitary Inspection -Article 27c.
- Switzerland:Etizolam is controlled in Switzerland.
- United Kingdom– Etizolam is a Class C drug in the UK as of 31st May 2017, making it illegal to possess, produce, or supply.
- Canada– Although etizolam is not scheduled in Canada, it is only legal to import for research purposes.
- Sanna, E., Pau, D., Tuveri, F., Massa, F., Maciocco, E., Acquas, C., … & Biggio, G. (1999). Molecular and neurochemical evaluation of the effects of etizolam on GABAA receptors under normal and stress conditions.Arzneimittelforschung, 49(02), 88-95. https://doi.org/10.1055/s-0031-1300366
- Altamura, A. C., Moliterno, D., Paletta, S., Maffini, M., Mauri, M. C., & Bareggi, S. (2013). Understanding the pharmacokinetics of anxiolytic drugs.Expert Opinion on Drug Metabolism & Toxicology, 9(4), 423-440. https://doi.org/10.1517/17425255.2013.759209
- Fracasso, C., Confalonieri, S., Garattini, S., & Caccia, S. (1991). Single and multiple dose pharmacokinetics of etizolam in healthy subjects. European Journal of Clinical Pharmacology, 40(2), 181-185. https://doi.org/10.1007/BF00280074
- Jump up↑Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
- Jump up↑Canadian Guideline for Safe and Effective Use of Opioids for Chronic Non-Cancer Pain – Appendix B-6: Benzodiazepine Tapering | http://nationalpaincentre.mcmaster.ca/opioid/cgop_b_app_b06.html
- Jump up↑ (n.d.). Etizolam. In TripSit Wiki. Retrieved May 11, 2017, from https://wiki.tripsit.me/wiki/Etizolam
- Jump up↑Sanna, E., Pau, D., Tuveri, F., Massa, F., Maciocco, E., Acquas, C., … & Biggio, G. (1999). Molecular and neurochemical evaluation of the effects of etizolam on GABAA receptors under normal and stress conditions. Arzneimittelforschung, 49(02), 88-95. https://doi.org/10.1055/s-0031-1300366
- Jump up↑Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796
- Jump up↑http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
- Jump up↑Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
- Jump up↑Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
- Jump up↑Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
- Jump up↑Etizolam and benzodiazepine induced blepharospasm. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/14966178
- Jump up↑Etizolam-induced superficial erythema annulare centrifugum (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/11952667
- Jump up↑Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614
- ↑ Jump up to:013.1 13.2 Sanna, E; Busonero, F; Talani, G; Mostallino, MC; Mura, ML; Pisu, MG; MacIocco, E; Serra, M; Biggio, G (2005). “Low tolerance and dependence liabilities of etizolam: Molecular, functional, and pharmacological correlates”. European Journal of Pharmacology 519 (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/16107249
- Jump up↑Barbiturates and thienodiazepine effects | https://www.ncbi.nlm.nih.gov/pubmed/2471436
- Jump up↑Flumazenil, a benzodiazepine antagonist | https://www.ncbi.nlm.nih.gov/pubmed/8306565
- Jump up↑http://m.ctpost.com/blogs/article/Man-charged-with-DUI-after-crash-5701091.php
- Jump up↑http://www.healthy.arkansas.gov/aboutADH/RulesRegs/ControlledSubstanceListSummary.pdf
- Jump up↑http://www.bundesgesundheitsministerium.de/fileadmin/dateien/Downloads/B/Betaeubungsmittelgesetz/27_BtMAEndV.pdf
- Jump up↑http://www.gesetze-im-internet.de/btmg_1981/index.html
- Jump up↑http://web.archive.org/web/20170329020935/https://www.admin.ch/opc/de/classified-compilation/20101220/index.html
- Jump up↑The Misuse of Drugs (Amendment) (England, Wales and Scotland) Regulations 2017 | http://www.tihs.org.uk/timeline/resources/2017-631.pdf