Deschloroetizolam

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

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

Summary sheet: Deschloroetizolam
Deschloroetizolam
Deschloroetizolam.svg
Chemical Nomenclature
Common names Deschloroetizolam
Systematic name 2-ethyl-9-methyl-4-phenyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
Class Membership
Psychoactive class Depressant
Chemical class Thienodiazepine
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 Common Heavy
1 - 2 - 4 - 6 - 12 mg
Light Strong
Threshold 1 - 2 mg
Light 2 - 4 mg
Common 4 - 6 mg
Strong 6 - 12 mg
Heavy 12 mg +
Duration
Total 8 - 10 hours
Onset 1 - 5 minutes
Peak 1 - 2 hours
Offset 2 - 3 hours
After effects 3 - 6 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.

Deschloroetizolam is a short-acting psychoactive substance of the thienodiazepine class which has been shown to produce depressants, anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, depressant and amnesic effects. Deschloroetizolam, like benzodiazepines, binds to modulatory sites on the GABA receptors. Deschloroetizolam is closely related to etizolam (Etilaam), triazolam (Halcion), and alprazolam (Xanax).[2] It is not prescribed and is not recognised as a controlled substance in many parts of the world, leading to its appearance within grey market research chemical vendors in 2014.

Deschloroetizolam has a relatively fast onset of action and symptomatic relief. It is half as potent as its parent compound etizolam with a duration which is twice as long. It also has a similar bioavailibility and a similar time to onset in comparison to the parent drug. 2mg of deschloroetizolam is thought to be of similar potency to 10mg of diazepam.

Similar to benzodiazepines, the sudden discontinuation of thienodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. It is highly recommended to taper one's dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping abruptly.[3]

Chemistry

Deschloroetizolam is a structural relative of benzodiazepines, whereby the benzene ring has been replaced by a thiophene ring, classifying it as a thienodiazepine. It differs structurally from its parent compound etizolam through removal of the chlorine atom at the 2' position on the phenyl ring.

Deschloroetizolam contains a thiophene ring fused to a diazepine ring, which is a seven member ring with the two nitrogen constituents located at R1 and R4. Thiophene is a five member aromatic ring with one sulfur atom. This forms the thienodiazepine core of deschloroetizolam. An ethyl chain is bound to this bicyclic structure at R7. Additionally, a phenyl ring is bound to this structure at R5. Deschloroetizolam also contains a methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring. Deschloroetizolam shares this fused triazole ring substitution with certain benzodiazepine drugs, called triazolobenzodiazepines, distinguished by the suffix "-zolam".

Pharmacology

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.[4] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of deschloroetizolam on the nervous system.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These 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 of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
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Paradoxical effects
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Cognitive effects
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Toxicity and harm potential

Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.[9]

Deschloroetizolam likely has a low toxicity relative to dose.[10] However, it is potentially lethal when mixed with depressants like alcohol or opioids.

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

Tolerance and addiction potential

Deschloroetizolam is extremely physically and psychologically addictive.

Tolerance will 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.

Deschloroetizolam presents cross-tolerance with all benzodiazepines and thienodiazepines, meaning that after its consumption all thienodiazepines will have a reduced effect.

Overdose

Thienodiazepine overdose may occur when a thienodiazepine 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[11]. 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 GABAA antagonist[12], however care is primarily supportive in nature.

Dangerous interactions

Although many psychoactive substances are safe to use on their own, they can become dangerous or even life-threatening when taken with other substances. The list below contains some potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses but still increase the possibility of injury of death. Independent research should always be conducted 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 decrease 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 dosing a certain amount of thienzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.

Legal status

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This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

Deschloroetizolam is a grey area compound within most parts of the world. This means that it is not known to be specifically illegal within any country, but people may still be charged for its possession under certain circumstances such as under analogue laws and with intent to sell or consume.

  • Canada: Thienodiazepines like deschloroetizolam are not scheduled in Canada. However, it is illegal to sell or give someone it for human consumption because it is not an approved medical drug.[13]
  • United Kingdom: It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.[14]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. http://www.google.com/patents/EP0776892A4?cl=en | THIENYLAZOLE COMPOUND AND THIENOTRIAZOLODIAZEPINE COMPOUND. Patent EP 0776892. Yoshitomi Pharmaceuticals, 1997.
  3. 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
  4. Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796
  5. http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
  6. Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
  7. http://link.springer.com/article/10.2165/00023210-199809010-00005#page-1 | Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
  8. http://www.ncbi.nlm.nih.gov/pubmed/26256485 | Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
  9. Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  10. Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614
  11. Barbiturates and thienodiazepine effects | https://www.ncbi.nlm.nih.gov/pubmed/2471436
  12. Flumazenil, a benzodiazepine antagonist | https://www.ncbi.nlm.nih.gov/pubmed/8306565
  13. http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-15.html#h-34
  14. Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted