Flualprazolam
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.
Flualprazolam | |||||||||||||||||||||||||||||||
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Chemical Nomenclature | |||||||||||||||||||||||||||||||
Common names | Flualprazolam | ||||||||||||||||||||||||||||||
Substitutive name | Flualprazolam | ||||||||||||||||||||||||||||||
Systematic name | 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-benzo[f] [1,2,4]triazolo[4,3-a] [1,4]diazepine | ||||||||||||||||||||||||||||||
Class Membership | |||||||||||||||||||||||||||||||
Psychoactive class | Depressant | ||||||||||||||||||||||||||||||
Chemical class | Benzodiazepine | ||||||||||||||||||||||||||||||
Routes of Administration | |||||||||||||||||||||||||||||||
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Interactions | |||||||||||||||||||||||||||||||
Stimulants | |||||||||||||||||||||||||||||||
Depressants | |||||||||||||||||||||||||||||||
Dissociatives |
Flualprazolam is a novel depressant substance of the benzodiazepine class. It is a structural analog of alprazolam (Xanax), a widely used prescription benzodiazepine with high recreational potential. The mechanism is unknown, but it likely acts as a GABA receptor agonist.
Flualprazolam appears to have first become available for sale in 2017 on the online research chemical market.[2] The origins of its development is not clear. It has been marketed or deceptively sold as a replacement for alprazolam despite differing in substantive ways, according to some reports.
Subjective effects include sedation, muscle relaxation, disinhibition, anxiety suppression, memory suppression, and euphoria. Its effects are somewhat similar to alprazolam; however, it is reported to be more hypnotic and sedating than anxiolytic, and not as recreational. It appears to be more potent-by-weight than alprazolam.
Limited data exists on the pharmacological properties, metabolism, and toxicology of this compound. It likely possesses high abuse potential due to its similarity to alprazolam. The health risks of forming physical dependence to this compound are not known, and may possess additional risks relative to traditional benzodiazepines.
Additionally, it should be noted that the sudden discontinuation of benzodiazepines can be dangerous or even life-threatening for individuals for heavy or long-term users. As a result, individuals who are physically dependent on this substance are advised to taper their dose by gradually lowering the amount taken each day over a prolonged period instead of stopping use abruptly.[3]
Flualprazolam has been reported by users to dramatically and rapidly increase benzodiazepine cross-tolerance. It is strongly advised to only use Flualprazolam for short periods of time, and if used as an emergency substitute to avoid benzodiazepine withdrawal, to avoid compulsive redosing and minimize the administered dose as much as possible.
The potency of Flualprazolam compared to Alprazolam has been reported to vary dramatically by users (ranging anywhere between 1.5x and 5x stronger than Alprazolam).
It is strongly advised to use harm reduction practices if using this substance.
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. |
Flualprazolam first appeared on the research chemical market around 2017[2]
Chemistry
Flualprazolam belongs to a class of synthetic organic compounds called benzodiazepines. Benzodiazepines contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R1 and R4.
The benzyl ring of flualprazolam is substituted at R8 with a chlorine group. Further, the diazepine ring is bonded at R5 to a phenyl ring. The only difference to alprazolam is a fluorine group located at R2'.
Flualprazolam also contains a 1-methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring. Flualprazolam belongs to a class of benzodiazepines containing this fused triazole ring, called triazolobenzodiazepines, distinguished by the suffix "-zolam".
It can be described as the 2'-fluoro derivative of alprazolam, which it might share some of its effects[4], though some users report that it subjectively feels different than alprazolam in most aspects.
Pharmacology
This pharmacology section is incomplete. You can help by adding to it. |
Flualprazolam can be described as the 2'-fluoro derivative of alprazolam, or the fluoro instead of chloro analogue of triazolam, and has similar sedative and anxiolytic effects.[4]
Subjective effects
This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it. |
Flualprazolam is reported to to be more hypnotic, have a longer duration, and a significantly longer elimination half-life than its parent compound alprazolam.
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
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- Sedation - Reported to be stronger than many benzodiazepines. It has been described as a very forceful hypnotic, inducing sleep by force at high doses. This effect is dangerously hard to predict independent of any previous benzodiazepine tolerance.[citation needed]
- Muscle relaxation - Reportedly stronger than Alprazolam.
- Physical euphoria - Short-lasting, encouraging compulsive redosing.
- Motor control loss - More common at higher doses.
- Respiratory depression,
- Increased libido - Uncommon but noticeable effect, especially for first-time users.
- Seizure suppression
- Dizziness - Strong at higher doses.
- Temporary erectile dysfunction - Can sometimes be very strong and last for a few hours.
Cognitive effects
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If applicable, a brief paragraph summary of the substance's cognitive effects may be included here.
You may select from a list of cognitive effects to add below here.
- Anxiety suppression - Somewhat effective, but outweighed by hypnotic & sedative effects.
- Disinhibition - More prominent at high doses.
- Cognitive euphoria - Reportedly short lasting (1-2h after dosing), encouraging compulsive redosing while still intoxicated.
- Compulsive redosing
- Memory suppression - Quite strong at high doses.
- Delusions of sobriety - Present but manageable with some of the effect being imperceptible until the following day, depending on the dosage.
- Analysis suppression
- Ego inflation
- Thought deceleration
- Emotion suppression - This effect seems to be more pronounced than other benzodiazepines.
- Sleepiness - Noticeably more sedating than Alprazolam.
- Irritability - See paradoxical effects section
Visual effects
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- Visual acuity suppression - Like many depressants, flualprazolam may cause blurred or otherwise suppressed visual acuity, especially at high doses.
After effects
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- Rebound anxiety - Rebound anxiety is a commonly observed effect with anxiety relieving substances like benzodiazepines. 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 potentiation[5]
- Residual sleepiness - While benzodiazepines can be used as an effective sleep-inducing aid, their effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours.
- Thought deceleration
- Thought disorganization
- Irritability
Paradoxical effects
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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%).
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[8][9]
Experience reports
There are currently 0 experience reports which describe the effects of this substance in our experience index.
Additional experience reports can be found here:
Toxicity and harm potential
This toxicity and harm potential section is a stub. As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it. |
Flualprazolam likely has a low toxicity relative to dose. 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 substance.
Dependence and abuse potential
Like most benzodiazepines, Flualprazolam is considered to be highly addictive with a high potential for abuse.
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.
Benzodiazepine discontinuation is notoriously difficult and potentially life-threatening for heavy or long-term users. There is an increased risk of seizure following discontinuation of benzodiazepines. 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. Substances which lower the seizure threshold such as Tramadol should be avoided during withdrawal.
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, 2M2B, alcohol, benzodiazepines, barbiturates, GHB/GBL, methaqualone, opioids) - This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration. There is also an increased risk of suffocating on one's vomit while unconscious. If nausea or vomiting occurs before a loss of consciousness, users should attempt to fall asleep in the recovery position or have a friend move them into it.
- Dissociatives - This combination can unpredictably potentiate the amnesia, sedation, motor control loss and delusions that can be caused by each other. It may also result in a sudden loss of consciousness accompanied by a dangerous degree of respiratory depression. If nausea or vomiting occurs before consciousness is lost, users should attempt to fall asleep in the recovery position or have a friend move them into it.
- Stimulants - Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states. This combination can also potentially result in severe dehydration if one's fluid intake is not closely monitored. If choosing to combine these substances, one should strictly limit themselves to a pre-set schedule of dosing only a certain amount per hour until a maximum threshold has been reached.
Legal status
This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it. |
Internationally, Flualprazolam was added to the UN Convention on Psychotropic Substances as a Schedule II controlled substance in March 2020.[6][7]
- Germany: Flualprazolam is controlled under Anlage II BtMG (Narcotics Act, Schedule II) [8] as of January 21, 2021.[9]
- Poland: Flualprazolam is under the IV-P group as of March 11, 2021.[10] It is illegal to own, possess, and sell in Poland.[11]
- Turkey: Flualprazolam is a classed as drug and is illegal to possess, produce, supply, or import.[12]
- United Kingdom: Flualprazolam is controlled under the Psychoactive Substances Act.[citation needed]
- United States: Flualprazolam is a Schedule I controlled substance as of January 23, 2023.[13]
See also
External links
References
- ↑ Risks of Combining Depressants - TripSit
- ↑ 2.0 2.1 Flualprazolam - Google Trends | https://trends.google.com/trends/explore?date=all&geo=US&q=Flualprazolam
- ↑ Kahan, M., Wilson, L., Mailis-Gagnon, A., Srivastava, A. (November 2011). "Canadian guideline for safe and effective use of opioids for chronic noncancer pain. Appendix B-6: Benzodiazepine Tapering". Canadian Family Physician. 57 (11): 1269–1276. ISSN 0008-350X.
- ↑ 4.0 4.1 Waters, L., Manchester, K. R., Maskell, P. D., Haegeman, C., Haider, S. (May 2018). "The use of a quantitative structure-activity relationship (QSAR) model to predict GABA-A receptor binding of newly emerging benzodiazepines". Science & Justice. 58 (3): 219–225. doi:10.1016/j.scijus.2017.12.004. ISSN 1355-0306.
- ↑ Goyal, S. (14 March 1970). "Drugs and dreams". Canadian Medical Association Journal. 102 (5): 524. ISSN 0008-4409.
- ↑ "WHO: World Health Organization recommends 12 NPS for scheduling". December 2019. Retrieved October 16, 2020.
- ↑ "CND accepts all WHO recommendations on the control of several psychoactive substances from the 42nd ECDD meeting". World Health Organization (WHO). March 18, 2020. Retrieved October 16, 2020.
- ↑ "Anlage II BtMG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved August 30, 2021.
- ↑ "Einundzwanzigste Verordnung zur Änderung von Anlagen des Betäubungsmittelgesetzes". Bundesgesetzblatt Jahrgang 2021 Teil I Nr. 2 (in German). Bundesanzeiger Verlag. January 20, 2021. Retrieved August 30, 2021.
- ↑ "Rozporządzenie Ministra Zdrowia z dnia 11 marca 2021 r. zmieniające rozporządzenie w sprawie wykazu substancji psychotropowych, środków odurzających oraz nowych substancji psychoaktywnych". DZIENNIK USTAW 2021 R. POZ. 518 (in Polish). 2021-03-22.
- ↑ "Rozporządzenie Ministra Zdrowia z dnia 11 marca 2021 r. zmieniające rozporządzenie w sprawie wykazu substancji psychotropowych, środków odurzających oraz nowych substancji psychoaktywnych" (PDF). DZIENNIK USTAW 2021 R. POZ. 518 (in Polish). 2021-03-22.
- ↑ "Cumhurbaşkanı Kararı: Karar Sayısı: 1335" (PDF). Resmî Gazete, Sayı: 30837 (in Turkish). Başbakanlık Mevzuatı Geliştirme ve Yayın Genel Müdürlüğü [General Directorate of Legislation Development and Publication] (published July 20, 2019). July 19, 2020.
- ↑ Schedules of Controlled Substances: Temporary Placement of Etizolam, Flualprazolam, Clonazolam, Flubromazolam, and Diclazepam in Schedule I | https://www.federalregister.gov/documents/2022/12/23/2022-27278/schedules-of-controlled-substances-temporary-placement-of-etizolam-flualprazolam-clonazolam