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'''Fluclotizolam''' is a [[ | {{DepressantOD|benzodiazepines}}<br />{{SummarySheet}} | ||
{{SubstanceBox/Fluclotizolam}} | |||
'''Fluclotizolam''' is a medium-duration [[psychoactive]] substance of the [[chemical class::thienodiazepine]] class which has been shown to produce [[psychoactive class::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).<ref>http://www.google.com/patents/EP0776892A4?cl=en | THIENYLAZOLE COMPOUND AND THIENOTRIAZOLODIAZEPINE COMPOUND. Patent EP 0776892. Yoshitomi Pharmaceuticals, 1997.</ref> 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]], [[Thienodiazepine#Discontinuation|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.<ref>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</ref> | |||
==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Fluclotizolam is a structural relative of [[benzodiazepines]], whereby the benzene ring has been replaced by a thiophene ring, classifying it as a [[thienodiazepine]].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 R<sub>1</sub> and R<sub>4</sub>. 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 R<sub>7</sub>. Additionally, a phenyl ring is bound to this structure at R<sub>5</sub>. Fluclotizolam also contains a methylated triazole ring fused to and incorporating R<sub>1</sub> and R<sub>2</sub> 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== | |||
{{HistoryStub}} | |||
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 R<sub>1</sub> and R<sub>4</sub>. This forms the thienodiazepine core of fluclotizolam . An ethyl chain is bound to this bicyclic structure at R<sub>7</sub>. Additionally, a R<sub>2</sub>' fluorine-substituted phenyl ring is bound to this structure at R<sub>5</sub>. | |||
Fluclotizolam also contains a methylated triazole ring fused to and incorporating R<sub>1</sub> and R<sub>2</sub> 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 [[GABA|gamma aminobutyric acid (GABA)]] by acting on its [[receptor]]s.<ref>Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796</ref> As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the [[sedating]] (or [[anxiety suppression|calming effects]]) of Fluclotizolam on the nervous system. | |||
==Subjective effects== | |||
{{Preamble/SubjectiveEffects}} | |||
{{effects/base | |||
|{{effects/physical| | |||
*'''[[Effect::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. | |||
*'''[[Effect::Respiratory depression]]''' | |||
*'''[[Effect::Muscle relaxation]]''' | |||
*'''[[Effect::Dizziness]]''' | |||
}} | |||
{{effects/paradoxical| | |||
Paradoxical reactions to [[thienodiazepine]]s and [[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%).<ref>http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review</ref><ref>Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf</ref> | |||
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.<ref>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</ref><ref>http://www.ncbi.nlm.nih.gov/pubmed/26256485 | Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev</ref> | |||
}} | |||
|{{effects/cognitive| | |||
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]]s cognitive effects. | |||
The most prominent of these cognitive effects generally include: | |||
*'''[[Effect::Amnesia]]''' | |||
*'''[[Effect::Anxiety suppression]]''' | |||
*'''[[Effect::Thought deceleration]]''' | |||
*'''[[Effect::Analysis suppression]]''' | |||
*'''[[Effect::Disinhibition]]''' | |||
*'''[[Effect::Cognitive euphoria|Euphoria]]''' | |||
*'''[[Effect::Compulsive redosing]]''' | |||
*'''[[Effect::Emotion suppression]]''' - Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but less intensive than that of [[antipsychotic]]s. | |||
*'''[[Effect::Delusions|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 heavy dosages. | |||
*'''[[Effect::Dream potentiation]]''' | |||
}} | |||
}} | |||
===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: | |||
*[https://www.erowid.org/experiences/subs/exp_Deschloroetizolam.shtml Erowid Experience Vaults: Fluclotizolam] | |||
==Toxicity and harm potential== | |||
[[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.<ref>Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644</ref>]] | |||
{{Further|Research chemicals#Toxicity and harm potential}} | |||
Fluclotizolam likely has a [[Toxicity::low toxicity]] relative to dose.<ref>Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614</ref> However, it is [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[opioids]]]]. | |||
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug. | |||
===Tolerance and addiction potential=== | |||
Fluclotizolam is [[Addiction potential::extremely physically and psychologically addictive]]. | |||
Tolerance will develop to the sedative-hypnotic effects [[Time to full tolerance::within a couple of days of continuous use]]. After cessation, the tolerance returns to baseline in [[Time to zero tolerance::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 [http://www.benzo.org.uk/manual/bzcha02.htm this guide]. | |||
[[Benzodiazepine#Discontinuation|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 [[Cross-tolerance::all [[benzodiazepine]]s and [[thienodiazepine]]s]], 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 [[barbiturate |barbiturates]] and [[alcohol]] since they work in a similar fashion, but bind to distinct allosteric sites on the GABA<sub>A</sub> receptor, thus their effects potentiate one another. Thienodiazepine increase the frequency in which the chlorine ion pore opens on the GABA<sub>A</sub> 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<ref>Barbiturates and thienodiazepine effects | https://www.ncbi.nlm.nih.gov/pubmed/2471436</ref>. 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]], [[language suppression |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 GABA<sub>A</sub> antagonist<ref>Flumazenil, a benzodiazepine antagonist | https://www.ncbi.nlm.nih.gov/pubmed/8306565</ref>, however care is primarily supportive in nature. | |||
===Dangerous interactions=== | |||
{{DangerousInteractions/Intro}} | |||
*'''[[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 [[stimulant]]s due to the risk of excessive intoxication. Stimulants decrease the [[sedation|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 [[thienzodiazepine#Subjective effects|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== | |||
{{legalStub}} | |||
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.<ref>http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-15.html#h-34</ref> | |||
*'''Germany''': Fluclotizolam is controlled under the NpSG (''New Psychoactive Substances Act'')<ref>{{cite web|url=https://www.gesetze-im-internet.de/npsg/anlage.html|title=Anlage NpSG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 10, 2019|language=de}}</ref> as of July 18, 2019.<ref>{{cite web|url=http://www.bgbl.de/xaver/bgbl/start.xav?startbk=Bundesanzeiger_BGBl&jumpTo=bgbl119s1083.pdf|title=Verordnung zur Änderung der Anlage des Neue-psychoaktive-Stoffe-Gesetzes und von Anlagen des Betäubungsmittelgesetzes|publisher=Bundesanzeiger Verlag|work=Bundesgesetzblatt Jahrgang 2019 Teil I Nr. 27|publication-date=July 17, 2019|access-date=December 28, 2019|language=de}}</ref> 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.<ref>{{cite web|url=https://www.gesetze-im-internet.de/npsg/__4.html|title=§ 4 NpSG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 10, 2019|language=de}}</ref> | |||
*'''Russia''': Fluclotizolam is a Schedule III controlled substance since 2017.<ref>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</ref> | |||
*'''Switzerland''': Fluclotizolam is a controlled substance specifically named under Verzeichnis E.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref> | |||
*'''Turkey:''' Fluclotizolamis a classed as drug and is illegal to possess, produce, supply, or import.<ref name="Bakanlar Kurulu Kararı - Karar Sayısı : 2016/9712">https://resmigazete.gov.tr/eskiler/2017/01/20170112-8.pdf</ref> | |||
*'''United Kingdom''': It is illegal to produce, supply, or import Fluclotizolam under the Psychoactive Substance Act, which came into effect on May 26, 2016.<ref>Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted</ref> | |||
==See also== | |||
*[[Responsible use]] | |||
**[[Volumetric liquid dosing]] | |||
*[[Depressants]] | |||
*[[Benzodiazepines]] | |||
*[[Etizolam]] | |||
==External links== | |||
*[https://en.wikipedia.org/wiki/Fluclotizolam Fluclotizolam (Wikipedia)] | |||
*[https://isomerdesign.com/PiHKAL/explore.php?id=3331 Fluclotizolam (Isomer Design)] | |||
==References== | |||
<references /> | |||
{{#set:Featured=true}} | |||
[[Category:Substance]] | |||
[[Category:Psychoactive substance]] | |||
[[Category:Depressant]] | |||
[[Category:Anxiolytics]] | |||
[[Category:Thienodiazepine]] | |||
[[Category:Research chemical]] | |||