Flubromazepam |
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There is a high incidence of death due to respiratory depression when benzodiazepines are combined with depressants such as opiates, alcohol or other GABAergic substances.[1] |
| Flubromazepam | |||||||||||||||||||||||
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| The skeletal formula of flubromazepam | |||||||||||||||||||||||
| Chemical Nomenclature | |||||||||||||||||||||||
| Common names | Flubromazepam | ||||||||||||||||||||||
| Systematic name | 7-Bromo-5-(2-fluorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one | ||||||||||||||||||||||
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| Psychoactive class | Depressant | ||||||||||||||||||||||
| Chemical class | Benzodiazepine | ||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||
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| Summary sheet: Flubromazepam |
Flubromazepam is a long-lasting psychoactive drug of the benzodiazepine class which produces anxiolytic, sedative, muscle relaxant, anti-nausea and amnesic effects. It is important to note before ingesting this compound that it has an unusually long half life with a 3 day duration and a 4 hour onset.
This compound was first made in 1960,[2] but was never marketed and did not receive any further attention or study until late 2012. It 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.
Contents
Chemistry
Flubromazepam, or 7-Bromo-5-(2-fluorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one, is a chemical of the benzodiazepine class. Flubromazepam is named for the fluorine and bromine substitutions on its core benzodiazepine skeleton (FLUorine-BROMine-azepam). Flubromazepam 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 flourine substituted phenyl ring is bound to this structure at R5. Flubromazepam also contains an oxygen group double bonded to R2 of its diazepine ring to form a ketone. This oxygen substitution at R2 is shared with other benzodiazepine drugs with the suffix -azepam.
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.[3] As this site is the most prolific inhibitory receptor within the brain, its modulation results in the sedating (or calming effects) of flubromazepam 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 flubromazepam 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 flubromazepam can be broken down into several components which progressively intensify proportional to dosage. The general head space of flubromazepam 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:
- Amnesia
- Anxiety suppression
- Thought deceleration
- Disinhibition
- Information processing suppression
- Compulsive redosing
- 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.
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%).[4][5]
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[6][7]
Toxicity and harm potential
Lethal dosage
The lethal dosage of flubromazepam 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 flubromazepam 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
Flubromazepam 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.
- Germany: On November 21, 2015 flubromazepam was added to the controlled substance act ("BtMG"), making it illegal to produce, sell or possess.[8]
Preparation methods
Preparation methods for this compound within our preparation index include:
See also
- Responsible use
- Flubromazepam (Wikipedia)
- Flubromazolam
- Benzodiazepines
- Depressants
- Volumetric liquid dosing
References
- ↑ https://tripsit.me/combining-depressants/ | Tripsit - Risks of Combining Depressants
- ↑ http://worldwide.espacenet.com/publicationDetails/biblio?CC=US&NR=3136815&KC=&FT=E&locale=en_EP
- ↑ Benzodiazepine interactions with GABA receptors | http://www.ncbi.nlm.nih.gov/pubmed/6147796
- ↑ http://www.ncbi.nlm.nih.gov/pubmed/18922233 | Saïas T, Gallarda T | Paradoxical aggressive reactions to benzodiazepine use: a review
- ↑ Paton C | Benzodiazepines and disinhibition: a review | Psychiatr Bull R Coll Psychiatr | http://pb.rcpsych.org/cgi/reprint/26/12/460.pdf
- ↑ Bond AJ | Drug-induced behavioural disinhibition: incidence, mechanisms and therapeutic implications | CNS Drugs
- ↑ Drummer OH | Benzodiazepines—effects on human performance and behavior | Forensic Sci Rev
- ↑ 30. BtMÄndVO in Kraft getreten | http://blog.beck.de/2015/11/23/30-btm-ndvo-in-kraft-getreten-6-neue-stoffe-wurden-ins-btmg-aufgenommen-0