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Flunitrazolam

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Revision as of 19:39, 28 September 2021 by >Dextromethorphan (Natzki moved page Talk:Flunitrazolam to Flunitrazolam: hope its okay seems finished)
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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: Flunitrazolam
Flunitrazolam
Chemical Nomenclature
Common names Flunitrazolam
Substitutive name Flunitrazolam
Systematic name 1-methyl-8-nitro-6-(2-fluorophenyl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Class Membership
Psychoactive class Depressant
Chemical class Benzodiazepine
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 0.1 mg
Light 0.1 - 0.2 mg
Common 0.2 - 0.3 mg
Strong 0.3 - 0.5 mg
Heavy 0.5 +
Duration
Total 4 - 8 hours
Onset 20 - 40 minutes
Peak 1 - 2 hours
Offset 2 - 4 hours
After effects 1 - 12 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.

Interactions


Flunitrazolam is a novel synthetic depressant substance of the benzodiazepine class which reportedly produces primarily hypnotic effects, among others such as muscle relaxant, anxiolytic, disinhibiting, sedative, , and memory suppressing or even amnesic effects when administered. It has been noted for its unusual potency for a benzodiazepine compound, being active in the low microgram range. This trait is also shared by compounds such as flubromazolam and clonazolam.

Flunitrazolam first appeared on the research chemicals market in 2016.[citation needed] It typically appeared in the form of pressed pellets along with other novel benzodiazepines such as clonazolam and flubromazolam. Of these, this compound is entirely novel and has no precedent in the scientific literature before being made available on online. As a result, information regarding dosage, effects, and toxicity should be regarded with caution. Any comments regarding its pharmacology are purely speculation based upon the subjective effects it induces and its structural similarity to funitrazolam and other benzodiazepines, with very little research done for far with this particulr compound.

It should be noted that there have been reports of seizues on high doses of this compound, without any contributing cause or withdrawal that might have triggered this. Only r05-4864 has this property, although to a greater extent.

It is worth noting that the sudden discontinuation of benzodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death.[2] 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 usage abruptly.[3]

Very little data exists about the pharmacological properties, metabolism, and toxicity of flunitrazolam in humans. Currently, it being sold as a gray-area research chemical by online vendors. Due to the high dependence-forming and addiction potential that this substance shares with other members of the benzodiazepine class, as well as its alcohol-like ability to induce dangerous disinhibitory and especially reported black-out states, it is highly advised to use proper harm reduction practices if choosing to use this substance, especially concurrently with other depressants and also by using volumetric liquid dosing carefully.

Chemistry

This chemistry section is incomplete.

You can help by adding to it.

Flunitrazolam is a chemical of the benzodiazepine class. Flunitrazolam is named for the fluorine, bromine, and triazole substitutions on its core benzodiazepine skeleton (FLUorine-NITro-AZOLe-AM). Flunitrazolam is a member of the benzodiazepine class as it contains a 1,4 diazepine ring fused to a substituted benzene ring. Bromine is bound to this bicyclic structure at R7. Additionally, a fluorine substituted phenyl ring is bound to this structure at R5.

Flunitrazolam also contains a methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring. Flunitrazolam belongs to a class of benzodiazepines containing this fused triazole ring, 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.[4] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of flunitrazolam on the nervous system.

The anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.[5]

Experimental results for Flunitrazolam often yield findings of sedation, disinhibition, dream potentiation, residual sleepiness, thought deceleration, and muscle relaxation.[6]

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 ☠.

Flunitrazolam has distict effects which range from barely noticeable to complete memory loss, depending strongly on dosage and physical differences in metabolism. It shares some common traits among many people, including mild or threshold effects at lower dosage levels before quickly turning into very amnesic or black-out states over a certain dosage (some people report 300mg). It predominantly has hypnotic effects and notable muscle relaxation, while lacking anxiety suppression or sedating effects.


Physical effects

Paradoxical effects

Cognitive effects

After 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:

Preparation methods

  • Volumetric liquid dosing - If one's benzodiazepines are in powder form, they are unlikely to weigh out accurately without the most expensive of scales due to their extreme potency. To avoid this, one can dissolve the benzodiazepine volumetrically into a solution and dose it accurately based upon the instructions linked within this tutorial.

Due to Flunitrazolam's extreme potency compared to even other ultrapotent benzodiazepines it should be used even more carefully when making and using a volumetric liquid solution. One should weigh at least 30mgs or Flunitrazolam which requires a bit bigger dropper bottles. The bottle should be shaked everytime before usage.

Toxicity and harm potential

Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.[11]

Flunitrazolam likely has a low toxicity relative to dose.[12] However, it is [[Toxicity::potentially lethal when mixed with depressants like alcohol or opioids]].

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

Tolerance and addiction potential

Flunitrazolam 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 benzodiazepines in a controlled manner, please see this guide.

Benzodiazepine 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 hypertension, seizures, and death.[13] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Flunitrazolam presents cross-tolerance with [[Cross-tolerance::all benzodiazepines]], meaning that after its consumption all benzodiazepines will have a reduced effect.

Overdose

Benzodiazepine overdose may occur when a benzodiazepine 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. Benzodiazepines 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[14]. Benzodiazepine 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 benzodiazepine overdose may include severe thought deceleration, slurred speech, confusion, delusions, respiratory depression, coma or death. Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Benzodiazepine overdoses are sometimes treated with flumazenil, a GABAA antagonist,[15] however care is primarily supportive in nature.

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 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 ("pulmonary aspiration"). If extreme sleepiness or loss of consciousness occur, 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 mask 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.

This legality section is a stub.

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

Flunitrazolam is currently a gray area compound within most (if not all) 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.

  • Switzerland: Flunitrazolam is legal in Switzerland as of September 2021.[16]

See also

References

  1. Risks of Combining Depressants - TripSit 
  2. A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812
  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. Benzodiazepines, but not beta carbolines, limit high-frequency repetitive firing of action potentials of spinal cord neurons in cell culture. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2450203
  6. https://pubmed.ncbi.nlm.nih.gov/29462316/
  7. http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
  8. Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
  9. Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms, and therapeutic implications | CNS Drugs
  10. Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
  11. Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  12. Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614
  13. A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812
  14. Twyman, R. E., Rogers, C. J., & Macdonald, R. L. (1989). Differential regulation of γ‐aminobutyric acid receptor channels by diazepam and phenobarbital. Annals of Neurology, 25(3), 213-220. https://doi.org/10.1002/ana.410250302
  15. Amrein, R., Leishman, B., Bentzinger, C., & Roncari, G. (1987). Flumazenil in benzodiazepine antagonism. Medical Toxicology and Adverse Drug Experience, 2(6), 411-429. PMID: 8306565
  16. https://fedlex.data.admin.ch/filestore/fedlex.data.admin.ch/eli/cc/2011/363/20161201/de/pdf-a/fedlex-data-admin-ch-eli-cc-2011-363-20161201-de-pdf-a.pdf