Deschloroetizolam

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

Taking large amounts of these substances together is strongly discouraged.

Deschloroetizolam
The skeletal formula of Deschloroetizolam.
Deschloroetizolam.png
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



Oral
Dosage
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is a summary of data gathered from users and resources. It is not a recommendation and should be verified with other sources for accuracy.
Threshold < 2 mg
Light 2 - 4 mg
Common 4 - 6 mg
Strong 6 - 12 mg
Heavy 12 mg +
Duration
Total 3 - 8 hours
Onset 15 - 60 minutes
Peak 1 - 2 hours
Offset 2 - 3 hours
Afterglow 3 - 6 hours









Summary sheet: Deschloroetizolam

Deschloroetizolam is a short-acting psychoactive drug of the thienodiazepine class which has been shown to produce depressant, anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, and amnestic effects. Deschloroetizolam, like benzodiazepines, binds to modulatory sites on the GABA gamma-aminobutyric acid 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. For anxiety disorders associated with depression, 2mg may be administered a couple of times over the course of a day. Smaller doses may alleviate symptoms of panic and it can be used before bed for relief of insomnia.

Similar to benzodiazepines, sudden withdrawal from extended thienodiazepine use can result in hypertension, seizures, and death.[3] When suspending long-term use, 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.[4]

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

Benzodiazepines 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.[5] As this site is the most prolific inhibitory receptor 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. 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 deschloroetizolam can be broken down into several components which progressively intensify proportional to dosage.

The most prominent of these cognitive effects generally include:

  • Sedation - In terms of energy level alterations, this drug has the potential to be extremely sedating and often results in an overwhelmingly lethargic state. At higher levels, this causes 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.
  • Respiratory depression
  • Muscle relaxation
  • Dizziness

Cognitive effects

The cognitive effects of deschloroetizolam can be broken down into several components which progressively intensify proportional to dosage. The general head space of deschloroetizolam is described by many as one of intense sedation and decreased inhibition. It contains a large number of typical depressant cognitive effects.

The most prominent of these cognitive effects generally include:

Paradoxical effects

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%).[6][7]

These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[8][9]

Toxicity and harm potential

Lethal dosage

The lethal dosage of deschloroetizolam has not been established; however, (like many benzodiazepines) it has a large therapeutic index and margin of safety. Complications may arise when administered in excess. Intentional overdoses have been reported.

As with all GABAergic drugs, overdose can be lethal when mixed with other depressants including alcohol or opioids.

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

Tolerance and addiction potential

Tolerance will develop to the sedative-hypnotic effects within a couple of days of repeated administration. Abrupt discontinuation of deschloroetizolam following regular dosing over several days can result in a withdrawal phase which includes rebound symptoms such as increased anxiety and insomnia. It is possible to gradually reduce the dose over the course of several days, which will lengthen the duration of the withdrawal period, but reduce the perceived intensity.

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 an increased risk of seizure following discontinuation of deschloroetizolam. 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 also 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 benzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of benzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of benzodiazepines 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 benzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.

Legal issues

Deschloroetizolam is currently thought to be 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.

Preparation methods

Preparation methods for this compound within our preparation index include:

See also

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. A fatal case of benzodiazepine withdrawal. | http://www.ncbi.nlm.nih.gov/pubmed/19465812
  4. 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
  5. Benzodiazepine interactions with GABA receptors | http://www.ncbi.nlm.nih.gov/pubmed/6147796
  6. http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
  7. Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
  8. 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
  9. http://www.ncbi.nlm.nih.gov/pubmed/26256485 | Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev