Flubromazolam

Flubromazolam

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Flubromazolam

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Description

some other prescription benzodiazepines, it is easy to overdose on flubromazolam alone.

The threshold dose for flubromazolam is 80 micrograms (about 1/12 of a milligram). A common recreational dose of flubromazolam is 200-400 ug (or 0.2-0.4 mg). Because it’s difficult to accurately measure such doses, I recommend using a milligram scale to prepare a 1mg/mL solution of flubromazolam in propylene glycol (More on this below!).

According to anecdotal reports [1], flubromazolam has more pronounced hypnotic, amnesic, and sedative effects than anxiolytic (anti-anxiety) effects. Consider this experience report from one UKChemicalResearch forum member:

Onset is 20 minutes and it hits hard and fast. Immediate hypnotic feeling and the eyes are like lead weights. Pure hypnotic but pronounced anti-anxiety effect as well. 1.5 mg had me asleep if compared to Temazepam 0.5 mg is around 25 mg. If introduced here it would have to be 0.25 mg. I would like to see it because it’s the most effective hypnotic i have seen and the shortish duration would mean no next day fogginess. But you would have to ration use to once every ten days or less, its potency has to be respected and frequent dosing would lead to inevitable problems. Possibly it could be introduced in advanced sections of sites.

Note that 1.5 mg flubromazolam would be a dangerous dose for someone without considerable tolerance to benzodiazepines.

A few users [1] have reported that flubromazolam has the greatest recreational value of any analog they’ve tried. That’s because, like alcohol, flubromazolam provides a distinctive “buzz.” But it will cause you problems if not treated with the respect it deserves.

Skeptical? Consider the flubromazolam safety section below, where I comment on a case report of a man in his twenties who took 3.0 mg of flubromazolam, resulting in profound and long-lasting hypotension, coma, and cerebral ischemia [2].

In contrast, if you took 20x the prescribed dose of Xanax (alprazolam) in isolation (without mixing it with other CNS depressants), you’d likely be fine [3]. Typical prescription benzodiazepines are relatively safe in overdose when other drugs aren’t involved, but flubromazolam is an entirely different animal.

A Brief History of Designer Benzodiazepines

​In 2012, the first designer benzodiazepines were offered online as alternatives to prescription-only benzodiazepines [4].

Most benzodiazepines are tightly regulated in the US since they’re frequently abused. Physicians are also becoming more reluctant to prescribe benzodiazepines.

All these factors contributed to the development of gray market benzodiazepine analogs, which are readily available online.

This stringent regulatory environment has made gray market benzodiazepine analogs so popular. It’s tricky to safely buy Xanax online. But designer benzodiazepines like Etizolam? Because many of these new analogs are unscheduled, they’re much more widely available.

However, technically some of the original benzodiazepine derivatives that became available in 2012 are now scheduled (regulated) in different countries. For example, Eetizolam is scheduled in five US states as well as Germany [4.5]. This first wave of designer benzodiazepines was largely Pphenazepam and Eetizolam.

When Pphenazepam and Eetizolam became more tightly regulated by government agencies, clandestine labs began synthesizing other benzodiazepines analogs as legal substitutes.

This lead to the emergence of Cclonazolam, Ddeschloroetizolam, Fflubromazolam, Fflubromazepam, and Mmeclonazepam.

A Primer on Benzodiazepines

​In this section, I’ll discuss the pharmacology of benzodiazepines and how they affect the brain.

Benzodiazepines play an essential function in forensic and clinical toxicology [5]. They’re widely used for the treatment of sleep and anxiety disorders [6], seizures [7], and as drugs of abuse [8].

Benzodiazepines are central nervous system (CNS) depressants. They depress our CNS by binding to GABA-A receptors in the brain. GABA is an inhibitory neurotransmitter; it inhibits brain activity. Under normal conditions, GABA binds to its receptor, GABA-A. This tonically helps decrease anxiety, prevent excess neural activity, and regulate neuronal excitability.

Flubromazolam is a designer benzodiazepine that behaves kind of (but not exactly) like GABA – it binds and activates the GABA-A receptor. However, an important difference between these two molecules is that Flubromazolam is remarkably potent. The threshold dose for flubromazolam is a mere 80 ug (micrograms). That’s about 1/12 of a milligram.

Later, I’ll discuss what chemical modifications make flubromazolam so potent. Spoiler: it’s the Triazole group.

The first such benzodiazepine, chlordiazepoxide (Librium), was found accidentally by Leo Sternbach in 1955 and made available in 1960 by Hoffmann-La Roche – which, since 1963, has also marketed the benzodiazepine diazepam (Valium) [9]. In 1977, benzodiazepines were globally the most prescribed medications [10].

Benzodiazepines enhance the effect of the neurotransmitter GABA at the GABA(A) receptor, leading to sedative, hypnotic (sleep-inducing), anxiolytic (anti-stress), anticonvulsant, and muscle relaxant properties.

High doses of many shorter-acting benzodiazepines (e.g., Xanax) can also cause anterograde amnesia and dissociation [11]. These properties make benzodiazepines useful in treating anxiety, sleeplessness, agitation, seizures, muscle spasms, alcohol withdrawal and as a premedication for surgical or dental procedures [12].

Benzodiazepines are categorized as either short-, intermediate-, or long acting. Short- and intermediate-acting benzodiazepines are favored for treating sleeplessness; longer-acting benzodiazepines are advocated for treating stress [13]. Short-acting benzodiazepines tend to be more addictive since the user feels a psychological compulsion to redose if the effect doesn’t last very long.

Benzodiazepines are by and large viewed as safe and effective for short-term use, although cognitive impairment and paradoxical effects like behavioral disinhibition or aggression sometimes occur.happen.

Rarely, people experience paradoxical reactions to benzodiazepines, such as worsened agitation or panic [14]. Long-term use is controversial due to because of concerns about adverse emotional and physical effects, diminishing falling effectiveness, and physical addiction and withdrawal [15][16].

Given the adverse effects associated with benzodiazepine dependence, discontinuing from benzodiazepines often leads to enhanced physical and mental health [17][18]. The elderly are at a higher danger of suffering from both short- and long-term adverse effects [17][18]. Therefore, all benzodiazepines are recorded in the Beers List of improper drugs for senior adults [20].

Flubromazolam’s Profile

Flubromazolam has hypnotic, anxiolytic and tranquilizing effects. It also acts as a skeletal muscle relaxant at very low oral doses (0.1-0.2 milligrams). A dosage of 3.0 milligrams (about 0.043 mg/kg b.w.) can cause acute, long-lasting cardiorespiratory depression and CNS failure, complicated with brain hypoxic-ischemic changes [2].

Flubromazolam is an analog of flubromazepam. Flubromazolam has a remarkably high affinity for benzodiazepine receptors. It is immediately absorbed with peak effects normally within an hour. Flubromazolam hasn’t been screened for off-target effects and its wide availability online makes it a potentially dangerous and potent new designer drug.

In the literature, very little data can be found regarding flubromazolam. Nonetheless, it seems plausible that the inspiration for this molecule came from flubromazepam.

The effects of flubromazolam are unmistakable. Physically, flubromazolam ingestion causes sedation, dizziness, muscle relaxation, and impaired motor control.

The cognitive effects of flubromazolam include disinhibition, amnesia, anxiolytsics (decreased anxiety), and suppression of overall brain activity.

Flubromazolam Dosage

The threshold dose is 80 ug – this is the smallest dose where you’d expect to start feeling the effects of the drug. In this respect, flubromazolam is like LSD – another substance that is active in microgram quantities.

A common recreational flubromazolam dosage is 200-400 ug, but even the higher end of this spectrum may be too much for some people to handle.

Why is Flubromazolam So Potent?

As always, the dose makes the poison.

Very low doses of flubromazolam can be poisonous. In at least one case report, 3.0 mg of flubromazolam resulted in profound respiratory depression and coma [2].

Without turning this post into a chemistry lesson, flubromazolam’s potency is related to its chemical structure.

Fig 1. Flubromazolam                    Fig 2. Triazolam

Flubromazolam (fig. 1) is structurally very similar to triazolam (fig. 2). Triazolam (Halcion) is actually a prescription benzodiazepine that’s still used in the United States to treat insomnia. Like flubromazolam, triazolam is also extremely potent. For example, a typical dose of triazolam is 0.125mg or 0.250mg.

Halcion (triazolam) was banned in the UK in 1991 due to its potency and propensity to cause amnesia and sedation [21].

What makes triazolam and bromazolam more potent than your standard, run-of-the-mill benzodiazepine?

The triazole group. A triazole refers to heterocyclic compounds that have 3 nitrogens atoms in the ring with molecular formula C2H3N3.

Although flubromazolam is structurally most similar to triazolam, it was actually derived from flubromazepam (fig. 3) by adding a triazole functional group.

Fig. 3 Flubromazepam

How To Synthesize Flubromazolam

Flubromazepam and flubromazolam have fluorine and bromine atoms in the same positions. To synthesize flubromazepam, clandestine labs took flubromazepam and added a triazole functional group, making it very similar to triazolam.

Fig. 4 Triazolam Synthetic Route

The synthesis of flubromazolam can be accomplished by adding by adding 1-Acetyl-1,2,4-triazole to flubromazepam. I’m referring to step 3 in the above synthetic route.

Given flubromazolam’s potency, the ability to measure precise quantities is of paramount importance. Consider this statement published in the literature:

Due to their high potency, compounds like clonazolam or flubromazolam can cause strong sedation and amnesia at oral doses as low as 0.5 mg. Such low doses are extremely difficult to measure for users handling bulk materials, and tablets often vary greatly in the content of the active ingredient. This can lead to unintended overdosing, and could also be of concern in drug-facilitated crimes [22].

I recommend picking up a milligram scale. A microgram scale is preferable but prohibitively expensive in many cases.

The best way to deliver small doses of a substance is by preparing a solution. This decreases the chance that you’ll accidentally measure out too large of a dose.

The protocol entails dissolving a relatively large amount of fluobromazolam in an ounce of water. Next, titrate an appropriate dose by consuming a few drops of the solution.

This brings us to my next point, which is about flubromazolam’s solubility.

Flubromazolam Solubility

Flubromazolam is a fairly hydrophobic molecule [23]. This means that it’s insoluble in water – it will only dissolve in lipids or fats. As

This means that it’s essentially insoluble in water – it’s not polar enough to hydrogen bond with water.

If you’re wondering about flubromazolam’s solubility, then you’re probably trying to make a solution – which is the right idea. Preparing a solution will help you stay safe and avoid accidentally taking too high of a dose.

Flubromazolam’s approximate solubility in propylene glycol (PG) is 2.5 mg/mL.

Propylene glycol is a common solvent used in skincare products and things like vape juice. It’s safe to consume small quantities of propylene glycol. Due to its lack of oral toxicity, the United States Food and Drug Administration classified propylene glycol as “generally recognized as safe” (GRAS) for use as a food additive. Consequently, it’s found in ice cream, frozen desserts, and other consumables.

It’s fairly difficult to prepare a flubromazolam solution that’s as concentrated as 2.5 mg/mL. But it’s possible if the solution is gently warmed, stirred, and given sufficient time to solvate the flubromazolam.

For this reason, I recommend preparing a 1 mg/mL flubromazolam solution. Some supplies you’ll need to include (all of which are available on Amazon):

  • Dropper bottle
  • Food grade propylene glycol
  • Graduated cylinder.
  • Milligram scale
  • Spatula (optional)
  • Weighing papers (optional)

​Preparing A 1mg/mL Flubromazolam Solution

​1. Transfer propylene glycol (PG) to your dropper bottle
Most standard dropper bottles are 1 oz or 30 mL. I recommend using a graduated cylinder to measure out a known volume of propylene glycol (e.g. 30 mL), and then transferring the solvent to the dropper bottle.2. Measure out 30 mg flubromazolam
Since we’re aiming for a solution with a final concentration of 1 mg/mL and the volume of our vessel is 30 mL, we’ll need to add 30 mg of flubromazolam.

For this step, make sure you use an accurate milligram scale.

Take a weighing paper and fold it twice, so that you’ve made four squares. Now unfold/flatten the weighing paper. This will come in handy later.

Add the formerly folded weighing paper to your scale, zero the scale, and transfer the flubromazolam to the weighing paper with a spatula.

Measure out X mg of flubromazlam and transfer it to the dropper bottle. For the sake of this example, we’re measuring out 30 mg to add it to 30 mL propylene glycol and yield a 1 mg/mL solution.

3. Titrating the right dose
Next, you’d want to determine the volume of a drop of solution. Usually, there are about 20 drops per mL, but you should verify the volume of the drops using your graduated cylinder (count how many drops it takes to fill 1 mL in the graduated cylinder).

For a 1 mg/mL solution of flubromazolam, assuming a drop volume of 0.05 mL, one drop of the solution will correspond to 0.05 mg or 50 ug.

As a starting dose, I’d administer 4 drops, corresponding to 200 ug and wait a few hours to see how I feel. Don’t forget that anecdotal reports about flubromazolam indicate that the subjective effects of the drug peak after about 4 hours.

Don’t make the classic mistake drug-naive people make with say, cannabis edibles, pot brownies, where you’re impatient about not feeling anything immediately, and then end up consuming way too much. With pot brownies, the risks associated with overdosing on THC are minimal, but not so with flubromazolam: it’s markedly lethal in overdose (and overdose is only a few milligrams of the stuff).

Flubromazolam Duration

The half-life and duration of flubromazolam haven’t yet been fully characterized.Users report that the approximate duration of effects flubromazolam is 11-17 hours. The onset is 30 minutes, and an afterglow effect can persist days after dosing.

Flubromazolam Drug Tests

Does flubromazolam show up on standard drug screens for benzodiazepines?

The answer is yes. For example, one case report describes a 27-year-old man who was found unconscious [2]. He was intubated and mechanically ventilated (due to hypoventilation). The patient had ingested 3.0 mg flubromazolam. A positive benzodiazepine result was noted in urine obtained on admission 19 hours after flubromazolam ingestion.

It’s also likely that flubromazolam is metabolized to other more common benzodiazepines that are readily detectable in urine samples. At this point, there’s no evidence that flubromazolam is undetectable in standard drug test panels.

Flubromazolam Experience Reports

Flubromazolam users have frequently noted the potency and intensity of the drug. Such first-hand accounts also underscore of trialing low doses and being as safe as possible.

Consider the following account on Erowid, which cautions that flubromazolam “will fuck up your life.”

Male, 180 lbs, no current benzo tolerance before this but occasionally I occasionally take 2-5mg of alprazolam and remember most of the night. I have also tried flunitrazepam, diazepam, and clonazepam and have good times with these substances.

So on Monday (3 days ago) I was excited to see I’d gotten my 10ml bottle 1mg/ml flubromazolam liquid and 90 count tablets of clonazolam (.5-.7mg each).

Started with one tablet, took another 25 minutes later and that’s when things got blurry. I remember ingesting maybe .5ml of the flubromazolam liquid after that as well (using a .25ml segmented pipette). So a total of 1mg clonazolam and .5mg flubromazolam (ASKING FOR TROUBLE, I KNOW).

Anyways, I wake up the next day about 26 hours later to find the flubromazolam liquid completely empty. I believe I spilled it because if 9.5mg if flubromazolam was actually ingested I believe I would have still been asleep or much less coherent.

Anyways, because of my lowered inhibitions, I start popping the tablets like candy. I gave some to friends, maybe a total of 20 but even that’s a maximum overstatement. Between tuesday and wednesday I either dropped on the floor or consumed over 75 pellets of clonazolam.

During one of the nights, my step dad found me on the kitchen floor, covered in bed sheets with a big mess everywhere including food all over the ground.

Using my longboard as transportation, my friends mom who owns a coffee/ice cream shop said I stopped by and was outside the shop eating a latte, ice cream, texting and longboarding at the same time looking super fucked up. She said a car almost hit me and had to slam on the brakes.

I do vaguely remember to recall a car honking at me very closely and I’m lucky I’m still alive. That was a 45mph road.

I also vaguely remember breaking a bunch of glass, stepping on it and leaving blood stains all over the floor where I was stepping around in my room (I had absolutely no pain so I didn’t give a fuck at the time). I cleaned a lot of broken glass and blood off of the carpet yesterday.

I woke up today without a longboard, went out looking for it for a while and gave up. I had just bought this longboard two weeks ago for $190 and just got new bearings for it in the mail today. So yeah that’s gone.

One of my friends I gave 1 tablet too blacked out for the entire day and missed his date with his girlfriend.

I wouldn’t recommend these benzos to anyone unless you already have like a 12mg a day alprazolam habit or something crazy like that (I’m serious, no exaggeration). These will fuck up your life.

Flubromazolam SafetyBecause illicit benzodiazepine derivatives are readily obtainable online, forensic toxicologists and policymakers have their hands full with overdose cases.

Illicit compounds have various effects: euphoric, stimulating, or hallucinogenic. This marketplace also supplies benzodiazepine analogs, which are sometimes used in combination with stimulants to reduce their side effects.

One might think that benzodiazepine derivatives shouldn’t cause major toxicological issues because common prescription benzodiazepines typically have a low acute toxicity. Nevertheless, many new designer benzodiazepines can pose the danger of life-threatening intoxications. This include:

Deschloroetizolam
Etizolam
Pyrazolam
Diclazepam
Nifoxipam
Clonazolam
Flubromazolam

Cases of deadly overdose from prescription benzodiazepines (e.g., Xanax) without the involvement of other CNS depressants is actually rare. Adverse reactions usually occur when benzodiazepines and other sedatives are co-ingested. Unlike traditional benzodiazepines, flubromazolam is dangerous by itself in overdose.

I’ve summarized a case report of flubromazolam overdose for your benefit:

A patient was found unresponsive at home, with no indication of how long he had been unconscious.

The family denied any history of injury or chronic diseases. The patient reportedly experimented with new psychoactive substances for several years. Lately, he was using various research chemicals from an unknown source.

Upon arrival to The Department of Toxicology at Municipal Hospital, he was in a deep coma, score 3 in Glasgow Coma Scale (GCS). He was intubated and mechanically ventilated because of hypoventilation (respiratory rate of 6-8 breaths/min) and respiratory failure.

No spontaneous involuntary or voluntary movement was noted. A physical examination revealed paleness with livedo Reticularis and cyanosis of hands and feet. The existence of Bedsores on the right side of the body – on his cheek, shoulder, forearm, and hip as well as on the interior of the knee and ankle joints, suggested prolonged immobilization. His eyes were deviated upwards, and the exam revealed generalized hypotonia, decreased reflexes, and absent plantar reaction.

Neither pathological neurological symptoms nor meningeal signs were noticed. Intravenous fluid resuscitation was started, without any improvement. Intravenous administration of 25 mg of ephedrine failed to increase blood pressure (the patient had hypotension from flubromazolam).

The physicians suspected an opioid overdose and, therefore, administered 0.4 mg IV naloxone – which is a mu-opioid receptor antagonist that reverses some of the effects of opioid toxicity.

Treatment with naloxone had no effect. A continuous infusion of 0.12 mg/kg/min norepinephrine was started, which succeeded in raising blood pressure.

Diagnostic and lab tests were performed in tandem with treatment. Head computed tomography (CT) and the chest X-ray results were unremarkable.

The patient woke up and opened his eyes, moved in response to painful stimulation but failed to respond to voice. His pupils dilated and vertical nystagmus was found. An impulsive, insufficient breathing with the respiratory rate of 4-6/minutes returned. After about 30 minutes the consciousness of the patient returned to a GCS of 3.

Due to the positive reaction after the flumazenil administration, benzodiazepine derivative poisoning was diagnosed. The following day the patient was still unconscious, made non-purposeful movement in response to a noxious stimulus, and achieved a GCS of 6. His pupils reacted to the light and dilated to about 2 millimeters. He was still mechanically ventilated. A minor improvement in circulatory parameters was detected. Blood pressure was maintained at the level 110-120/70-80 mmHg and the dose of noradrenaline reduced to 0.04 mg/kg/min.

Following an intravenous dose of 0.5 mg of flumazenil, the patient awakened (GCS 9-10) for 30 min.

On the 3rd day of therapy, due to consistent disturbances of consciousness, a second computed tomography was performed that revealed hypoxic-ischemic changes inside the internal capsules bilaterally in both frontal and left the temporal area.

Neurological examination revealed Babinski sign, a weaker defense reaction of the right leg and bilateral hyperreflexia of an ankle and a knee on the correct side. A significant improvement of the state of consciousness took place just after the fourth day of treatment when it was possible to extubate the patient. He underwent physical rehabilitation and continued antibiotic treatment (8 d). On the ninth day of the treatment, he was moved to the Department of Neurology for further treatment.

The clinical interview was completed after conversing with the patient. The patient reported that he purchased flubromazolam online and had about 3 milligrams the previous evening, around 19 h before being discovered unconscious. He stated that 48 h before admission, he also ingested 2 mg of flubromazolam with phencyclidine in conjunction.

At that time, he felt very drowsy and woke up after about 10 h, without any unexpected symptoms.

​Actionable Tips For Using Flubromazolam Safely

Despite its high potency, flubromazolam can be used safely if certain precautions are taken.

Avoid redosing completely. Don’t fall into the trap of trying a little bit of flubromazolam, waiting a few hours, and then taking more because the effects weren’t very pronounced the first time. Since drug absorption time is variable, how you feel now won’t reliably predict how intoxicated you’ll be later. The best practice is choosing a reasonable dose from the outset and sticking with it for the evening without redosing.

Don’t combine CNS depressants. Combining a benzodiazepine with an opioid is an admission ticket to the ER. This is even more true with high-potency benzodiazepines like flubromazolam.

Prepare a solution. Don’t try to measure out microgram quantities of flubromazolam on a $20 pocket scale from Amazon. Instead, prepare a 1 mg/mL solution by dissolving flubromazolam in propylene glycol (PG). This way, it’s much easier to titrate the proper dosage.

Less is more. Ever eaten too many pot brownies? The worst-case scenario from overdosing on THC is nausea, vomiting, anxiety, and sleepiness. But take too much flubromazolam and you run the risk of irrevocably harming your brain and even death!

Keep a benzodiazepine antagonist on hand (if you have access to such drugs). Flumazenil reverses the effects of benzodiazepines by competitive inhibition of the benzodiazepine binding site on the GABA(A) receptor. Thus, flumazenil is said to be a GABA(A) antagonist. It’s, therefore, useful for reversing the effects of flubromazolam (and other benzodiazepines) in overdose situations.

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