Flubromazolam

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Please be aware of the high incidence of deaths due to respiratory depression when benzodiazepines are combined with depressants such as opiates, alcohol or other GABAergic substances.

Flubromazolam
Flubromazolam1.png
Chemical Nomenclature
Common names Flubromazolam
Systematic name 8-bromo-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Class Membership
Psychoactive class Depressant
Chemical class Benzodiazepine
Routes of Administration



Oral
Dosage
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity.
Threshold 80 ug
Light 100 - 200 ug
Common 200 - 400 ug
Strong 400 - 600 ug
Heavy 600 ug +
Duration
Total 12 - 18 hours
Onset 30 minutes
Afterglow 24+ hours









Summary sheet: Flubromazolam

Flubromazolam is a long-lasting psychoactive drug of the benzodiazepine class which produces anxiolytic, sedative, muscle relaxant, anti-nausea and amnesic effects.

This compound has potential use for the short-term treatment of anxiety, insomnia, acute seizures, and the sedation of hospitalized patients. However, it is currently exclusively sold by online research chemical vendors for use as a recreational psychoactive substance and has not been formally studied. This means that any comments regarding its pharmacology are purely speculation based upon the subjective effects it induces and its structural similarity to triazolam, pyrazolam and other benzodiazepines.

It is important to note that before ingesting this compound, careful consideration should be taken into ensuring that it is indeed flubromazolam and not flubromazepam. This is extremely important because flubromazepam has a 3 day duration and a 4 hour onset. A mistake could result in one attempting multiple redoses under the assumption that it has not worked and suffering a dangerous overdose.

Chemistry

Flubromazolam is a chemical of the benzodiazepine class. Flubromazolam is named for the fluorine, bromine, and triazole substitutions on its core benzodiazepine skeleton (FLUorine-BROMine-AZOLe-AM). Flubromazolam 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. Flubromazolam also contains a methylated triazole ring fused to and incorporating R1 and R2 of its diazepine ring. Flubromazolam 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.[1] As this site is the most prolific inhibitory receptor within the brain, its modulation results in the sedating (or calming effects) of flubromazolam on the nervous system.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

The physical effects of flubromazolam can be broken down into several components which progressively intensify proportional to dosage.

These are described below and generally include:

  • 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.
  • Motor control loss
  • Respiratory depression
  • Dizziness
  • Muscle relaxation

Cognitive effects

The cognitive effects of flubromazolam can be broken down into several components which progressively intensify proportional to dosage. The general head space of flubromazolam is described by many as one of intense sedation and decreased inhibition. It contains a large number of typical depressant cognitive effects.

The most prominent of these cognitive effects generally include:

Paradoxical effects

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%).[2][3]

These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[4][5]

Toxicity and harm potential

Lethal dosage

The lethal dosage of flubromazolam has not been established; however, (like many benzodiazepines) it has a large therapeutic index and margin of safety. Complications may arise when administered in excess. Intentional overdoses have been reported.

As with all GABAergic drugs, overdose can be lethal when mixed with other depressants including alcohol or opioids.

Tolerance and addiction potential

Tolerance will develop to the sedative-hypnotic effects within a couple of days of repeated administration. Abrupt discontinuation of flubromazolam following regular dosing over several days can result in a withdrawal phase which includes rebound symptoms such as increased anxiety and insomnia. It is possible to gradually reduce the dose over the course of several days, which will lengthen the duration of the withdrawal period, but reduce the perceived intensity.

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 seizure following discontinuation. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

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 also 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.

Legal issues

Flubromazolam is currently a grey 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.

Preparation methods

Preparation methods for this compound within our preparation index include:

See also

References

  1. Benzodiazepine interactions with GABA receptors | http://www.ncbi.nlm.nih.gov/pubmed/6147796
  2. http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
  3. Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
  4. Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
  5. Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev