Talk:Flunitrazepam

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It may contain incorrect information, particularly with respect to dosage, duration, subjective effects, toxicity and other risks.

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Death may result 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: Flunitrazepam
Flunitrazepam
Flunitrazepam.svg
Chemical Nomenclature
Common names Rohypnol, Flunitrazepam
Substitutive name Flunitrazepam
Systematic name 5-(2-fluorophenyl)-1-methyl-7-nitro-3H-1,4-benzodiazepin-2-one
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 0.2 - 0.5 mg
Light 0.5 - 1 mg
Common 1 - 3 mg
Strong 3 - 4 mg
Heavy 4 - 6 mg +
Duration
Total 4 - 8 hours
Onset 20 - 30 minutes
After effects 2 - 24 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.


Flunitrazepam (trade name Rohypnol) is a depressant substance of the benzodiazepine class that produces anxiolytic, anticonvulsant, sedative, and amnesic effects when administered.[2]

Flunitrazepam was first synthesized in 1972 by Hoffmann-La Roche. It is used for the short term treatment of insomnia and as a preoperative sedative in some countries. It is approximately 10 times more potent by weight than diazepam.

Users should note 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.[3] 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]

History and culture

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Flunitrazepam was discovered at Roche as part of the benzodiazepine work led by Leo Sternbach. It was first marketed in 1974 and entered the commerical market in Europe in 1975 under the name Rohypnol. In the 1980's it began to be available in other countries. [5]

In 1998, due to the abuse of the drug for date rape and recreation, Roche modified their 1mg tablets to make them less soluble and added a blue dye for easier detection in drinks. [6]

In studies in Sweden, flunitrazepam was the second most common drug used in suicides, being found in about 16% of cases. In a retrospective Swedish study of 1587 deaths, in 159 cases benzodiazepines were found. In suicides when benzodiazepines were implicated, the benzodiazepines flunitrazepam and nitrazepam were occurring in significantly higher concentrations, compared to natural deaths. [7]

Chemistry

Flunitrazepam is a drug of the benzodiazepine class. Benzodiazepine drugs 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.

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.[8] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of Flunitrazepam 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.[9]

Flunitrazepam is known to induce anterograde amnesia in sufficient doses (individuals are unable to remember certain events that they experienced while under the influence of the drug). This effect could be particularly dangerous, if flunitrazepam is used to aid in the commission of sexual assault, because victims may be unable to clearly recall the assault, the assailant, or the events surrounding the assault. [10]

80% of the flunitrazepam that is taken orally is absorbed but the bioavailability in suppository form is closer to 50%. [11]

Subjective effects

The general head space of flunitrazepam is described as one of intense sedation, relaxation, anxiety suppression and decreased inhibition similar to the headspace of higher doses of diazepam and temazepam.

The effects listed below are based on the subjective effect index, which is based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be treated with a healthy amount of skepticism. It is worth noting that these effects will rarely (if ever) occur all at once but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
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Paradoxical effects
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Cognitive effects
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After effects
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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:

Usage

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 methodological instructions linked within this tutorial here.

Toxicity and harm potential

Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.[16]

Flunitrazepam likely has a low toxicity relative to dose.[17] 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.

Lethal dosage

The oral LD50 (lethal dose in 50% of the population) of flunitrazepam is 1200 mg/kg in mice and 415 mg/kg in rats. [18]

Tolerance and addiction potential

Flunitrazepam 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 regularly using to discontinue use without tapering their dose over a period of weeks. There is an increased risk of hypertension, seizures, and death.[19] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Flunitrazepam presents cross-tolerance with all benzodiazepines, meaning that after its consumption, all benzodiazepines will have a reduced effect.

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 small 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. 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.

Overdose

Benzodiazepine overdose may occur when a benzodiazepine is taken in large quantities or concurrently with other depressants. This is particularly dangerous with other GABAergic depressants such as barbiturates and alcohol since they work similarly, 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[20]. Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and appropriately.

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[21]. However, care is primarily supportive in nature.

Legal status

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This legality section is a stub.

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

  • International: Flunitrazepam is a Schedule III drug under the international Convention on Psychotropic Substances of 1971. [citation needed]
  • Australia: Flunitrazepam is a Schedule 8 (S8) or controlled drug.[citation needed]
  • Austria: Flunitrazepam is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).[citation needed]
  • Canada: Flunitrazepam is a Schedule I controlled substance and is available by prescription only. [citation needed]
  • Germany: Since November 2011, flunitrazepam is controlled under Anlage 3 of the BtMG and requires a special prescription. [citation needed]
  • United Kingdom: Flunitrazepam is a Class C, Schedule 4 controlled drug under the Misuse of Drugs Regulations 2001.[22] [citation needed]
  • United States: Flunitrazepam is a Schedule IV drug under the Controlled Substances Act in the U.S but is not medically used. [citation needed]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614
  3. A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | 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. https://en.wikipedia.org/wiki/Flunitrazepam
  6. https://wiki.tripsit.me/wiki/Flunitrazepam
  7. https://en.wikipedia.org/wiki/Flunitrazepam#Suicide
  8. Benzodiazepine interactions with GABA receptors (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/6147796
  9. 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
  10. https://en.wikipedia.org/wiki/Flunitrazepam#Drug-facilitated_sexual_assault
  11. https://en.wikipedia.org/wiki/Flunitrazepam#Pharmacology
  12. http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
  13. Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
  14. Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
  15. Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
  16. Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  17. Benzodiazepine metabolism: an analytical perspective (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18855614
  18. https://toxnet.nlm.nih.gov/cgi-bin/sis/search/a?dbs+hsdb:@term+@DOCNO+6960
  19. A fatal case of benzodiazepine withdrawal. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/19465812
  20. Barbiturates and benzodiazepine effects | https://www.ncbi.nlm.nih.gov/pubmed/2471436
  21. Flumazenil, a benzodiazepine antagonist | https://www.ncbi.nlm.nih.gov/pubmed/8306565
  22. List of drugs currently controlled under the misuse of drugs legislation| https://www.gov.uk/government/uploads/system/uploads/attachment_data/file/164222/controlled-drugs-list.pdf