Talk:Fluclotizolam - PsychonautWiki

Talk:Fluclotizolam

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

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


Summary sheet: Fluclotizolam
Fluclotizolam
Fluclotizolam Structure.svg
Chemical Nomenclature
Common names Fluclotizolam
Systematic name 2-chloro-4-(2-fluorophenyl)-9-methyl-4H-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.












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


Fluclotizolam is a medium-duration psychoactive substance of the thienodiazepine class which has been shown to produce depressant, anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant and amnesic effects. Fluclotizolam, like benzodiazepines, binds to modulatory sites on the GABA receptors. Fluclotizolam is closely related to etizolam (Etilaam), Deschloroetizolam, 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.

Fluclotizolam has a relatively fast onset of action and symptomatic relief (especially when administered sublingually). There are conflicting reports on its potency, but it is claimed to be somewhere between 2 to 3 times half as potent as its parent compound etizolam with a slightly shorter duration. The dosage chart assumes this compound to have 3 times the potency of etizolam.

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

Fluclotizolam 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 replacement of the chlorine atom with a fluorine atom at the 2' position on the phenyl ring, as well as a replacement of the ethyl side chain with a chlorine atom at the thiophene ring.

Fluclotizolam 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 Fluclotizolam. An ethyl chain is bound to this bicyclic structure at R7. Additionally, a phenyl ring is bound to this structure at R5. Fluclotizolam also contains a methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring. Fluclotizolam shares this fused triazole ring substitution with certain benzodiazepine drugs, called triazolobenzodiazepines, distinguished by the suffix "-zolam".

History and culture

 

This History and culture section is a stub.

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

Etizolam first appeared on the online research chemical market at least before 2015.[citation needed]

Chemistry

Fluclotizolam 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. fluclotizolam 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 fluclotizolam . An ethyl chain is bound to this bicyclic structure at R7. Additionally, a R2' fluorine-substituted phenyl ring is bound to this structure at R5.

Fluclotizolam also contains a methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring, classifying it as a thienotriazolodiazepine. Fluclotizolam 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 Fluclotizolam on the nervous system.

Subjective effects

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
 

Paradoxical effects
 

Cognitive effects
 

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Toxicity and harm potential

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

Fluclotizolam 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

Fluclotizolam 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.

Fluclotizolam 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

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.

  • 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

 

This legality section is a stub.

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

Fluclotizolam 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 Fluclotizolam and 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]
  • Germany: Fluclotizolam is controlled under the NpSG (New Psychoactive Substances Act)[14] as of July 18, 2019.[15] Production and import with the aim to place it on the market, administration to another person and trading is punishable. Possession is illegal but not penalized.[16]
  • Russia: Fluclotizolam is a Schedule III controlled substance since 2017.[17]
  • Switzerland: Fluclotizolam is a controlled substance specifically named under Verzeichnis E.[18]
  • Turkey: Fluclotizolamis a classed as drug and is illegal to possess, produce, supply, or import.[19]
  • United Kingdom: It is illegal to produce, supply, or import Fluclotizolam under the Psychoactive Substance Act, which came into effect on May 26, 2016.[20]

See also

External links

References

  1. Risks of Combining Depressants - TripSit 
  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. "Anlage NpSG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved December 10, 2019. 
  15. "Verordnung zur Änderung der Anlage des Neue-psychoaktive-Stoffe-Gesetzes und von Anlagen des Betäubungsmittelgesetzes" (PDF). Bundesgesetzblatt Jahrgang 2019 Teil I Nr. 27 (in German). Bundesanzeiger Verlag. July 17, 2019. Retrieved December 28, 2019. 
  16. "§ 4 NpSG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved December 10, 2019. 
  17. Постановление Правительства РФ от 12.07.2017 N 827 | https://www.consultant.ru/cons/cgi/online.cgi?req=doc&base=LAW&n=220067&dst=1000000001&date=02.12.2019
  18. "Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien" (in German). Bundeskanzlei [Federal Chancellery of Switzerland]. Retrieved January 1, 2020. 
  19. https://resmigazete.gov.tr/eskiler/2017/01/20170112-8.pdf
  20. Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted
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