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Benzos The Benzodiazepine MEGA THREAD - Direct Benzo Questions Here v2.0

kleinerkiffer

Bluelight Crew
Joined
Dec 9, 2012
Messages
5,702
Old thread can be found here

What are benzos ?

Benzodiazepines are a class of gabaminergic psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. The first such drug, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955, and made available in 1960 by Hoffmann–La Roche
They are used to treat insomnia (only short term, as tolerance to the hypnotic properties of benzos builds rapidly), anxiety, seizures, muscle spasm and alcohol withdrawal.

How do they work ?
Benzos are positive allosteric modulators of the GABA-A receptor. Unlike other positive allosteric modulators that increase ligand binding, benzodiazepine binding acts as a positive allosteric modulator by increasing the total conduction of chloride ions across the neuronal cell membrane when GABA is already bound to its receptor. So they work by increasing the efficiency of a natural brain chemical, GABA, to decrease the excitability of neurons. This reduces the communication between neurons and, therefore, has a calming effect on many of the functions of the brain.
The GABA-A receptor consist of different subtypes, the predominant subtypes in the brain being those that contain α1-, α2-, α3-, and α5-subunits. Studies show, that α2,3GABA-A receptors are important for mediating the anxiolytic effects of benzodiazepines, while motor effects might involve action primarily at α1GABA-A receptors. The α1-containing αβγ2 receptors seem to mediate sedative, anterograde amnesic, and antimyoclonic actions. Muscle relaxant activity of BZDs is mediated partially by α1-, α2-, α3-, and α5-containing αβγ2 receptors.
So different benzos have different affinities for the subtypes making every benzo unique in it’s effects.

Dosage calculator and half lifes
http://www.benzo.org.uk/bzequiv.htm

Dangerous combinations
Benzodiazepines are CNS depressants and thus can increase the action of other CNS depressants and can increase sedation, provoke a black out, impaired motor coordination, suppressed breathing and other adverse effects that can be lethal.
If you don’t have a extremely high tolerance to both CNS depressants don’t combine ‘em, it’s not worth the risk.
Even a normal dose of a benzo and a few beer can result in a black out.
If you insist on doing it, have someone around to have an eye on you!

Withdrawal
Benzodiazepine withdrawal is no joke and can be lethal in the worth case, as GABA is the most important inhibiting neurotransmitter and going of cold turkey can result in seizures and has the potential to kill you. A taper is advised, look up the Ashton manual, it’s the golden standard for a benzo taper.
http://www.benzo.org.uk/manual/

http://www.ncbi.nlm.nih.gov/pubmed/21815323
Since the first report of benzodiazepine withdrawal seizure in 1961, many case reports have followed. Withdrawal seizures have occurred with short, medium, and long halflife benzodiazepine, if discontinued abruptly. Withdrawal seizures usually occur in patients who have been taking these medications for long periods of time and at high doses. Seizures have also been reported with less than 15 days of use and at therapeutic dosage. Almost all the withdrawal seizures reported were grand mal seizures. The severity of seizures range from a single episode to coma and death. Benzodiazepine dose tapering can be done faster in a hospital setting in high-dose abusers, but must be done more slowly in the outpatient setting in therapeutic dosage users.
Seizures after only 15 days of consecutive use seem to be individual cases and I guess those people were prone to seizures, but still going off cold turkey is a bad idea.
Using a few days in a row can result in rebound symptoms, like rebound anxiety, meaning that your anxiety level will be higher for a few days after using them.

Should I abuse them ?
Imo benzos are not really euphoric on their own, except if you count being anxiety free as euphoric.
Abusing them will result in a increase in tolerance and in the long run can worsen anxiety etc., so imo it’s a bad idea to use them recreational.
If you want to medicate your anxiety maybe try Hydroxizine and other drugs before taking benzos.

FAQ
Snorting -> snorting is a bad idea, as the oral bioavailability is extremely high and most of the benzos are not water soluble, so snorting won’t do much but clog your nose with fillers.
Shooting -> most benzos are not water soluble, so don’t shoot them
Here’s a list of the solubility’s by Captain.heroin

I created this thread so you all know how much water to use to dissolve benzodiazepines for injection. It's come to my attention people are still going to try shooting benzos, even those that aren't as feasible to inject in water only, so I want to help you all instead of leaving you all in the dark.

Hopefully these statistics should reflect water solubility at a pH of 7. If the pH fluctuates, the solubility may increase or decrease. You don't want to inject highly acidic or basic water, so I'm going to list statistics for pH of 7.

Alprazolam (Xanax) - 0.04 mg/mL
Chlordiazepoxide (Librium) - 2 mg/mL
Clonazepam (Klonopin) - < 0.1 mg/mL
Diazepam (Valium) - 0.05 mg/mL
Estazolam (ProSom) - 0.0015 mg/mL
Flurazepam (Dalmane) - 500 mg/mL
Loprazolam (Dormonoct) - 10mg/mL
Lorazepam (Ativan) - 0.08 mg/mL
Midazolam (Dormicum) - 0.024 mg/mL
Oxazepam (Serax) - 0.179 mg/mL
Temazepam (Restoril) - 0.164 mg/mL
Triazolam (Halcion) - 0.00453 mg/mL

Zolpidem (Ambien) - 23 mg/mL
Zopiclone (Imovane) - 0.151 mg/mL at 25°C **

As you can see, only flurazepam and midazolam are feasible for shooting in just water. Loprazolam is too, but I was unable to find information on it. If you can cite a source, please submit it so I can add it to this list. Any information on any other related drugs, or any other benzos of any kind are welcome as well.

For most other benzodiazepines, without having to use a vastly huge volume of water, you would want to use a safe, USP grade solvent, or you would want to avoid taking it IV.

There are many reasons not to inject benzodiazepines. For one, they seem to work better orally. Other than triazolam and midazolam, most benzodiazepines have at least 80% oral BA. Flurazepam is the one closest to 80%, and even then, I would personally prefer taking flurazepam orally over IV. Most benzodiazepines are going to last longer when taken orally. For the most part, they don't take too long to kick in either.

Furthermore, not filtering IV solutions with benzodiazepines with a micron filter may lead to complications, or at least be bad for your lungs and or other bodily organs. Please read the Case Studies thread for more about this.

** 25°C = 77°F
Potentiation ->
http://www.ncbi.nlm.nih.gov/pubmed/12875231
Cytochrome P450(CYP)3A4 is one of the CYP enzymes catalyzing oxidative metabolism, and involved in the metabolism of many drugs. Among benzodiazepines, alprazolam, triazolam, brotizolam and midazolam are mainly metabolished by CYP3A4, and quazepam, diazepam and flunitrazepam are partly metabolised by this enzyme. Azole antifungals, macrolide antibiotics, calcium antagonists and grapefruit juice inhibit CYP3A4 activity, while antiepileptics and rifampicin induce the activity.
So grapefruit juice will help you potentiate those mentioned above.

Toxicity of Nitrobenzodiazepines:
Cytochrome P450 3A4 is the predominant isoform in liver, and it metabolizes more than 50% of the clinical drugs commonly used. However, CYP3A4 is also responsible for metabolic activation of drugs, leading to liver injury. Benzodiazepines are widely used as hypnotics and sedatives for anxiety, but some of them induce liver injury in humans. To clarify whether benzodiazepines are metabolically activated, 14 benzodiazepines were investigated for their cytotoxic effects on HepG2 cells treated with recombinant CYP3A4. By exposure to 100 μM flunitrazepam, nimetazepam, or nitrazepam, the cell viability in the presence of CYP3A4 decreased more than 25% compared with that of the control. In contrast, in the case of other benzodiazepines, the changes in the cell viability between CYP3A4 and control Supersomes were less than 10%. These results suggested that nitrobenzodiazepines such as flunitrazepam, nimetazepam, and nitrazepam were metabolically activated by CYP3A4, which resulted in cytotoxicity. To identify the reactive metabolite, the glutathione adducts of flunitrazepam and nimetazepam were investigated by liquid chromatography-tandem mass spectrometry. The structural analysis for the glutathione adducts of flunitrazepam indicated that a nitrogen atom in the side chain of flunitrazepam was conjugated with the thiol of glutathione. Therefore, the presence of a nitro group in the side chain of benzodiazepines may play a crucial role in the metabolic activation by CYP3A4. The present study suggested that metabolic activation by CYP3A4 was one of the mechanisms of liver injury by nitrobenzodiazepines.
http://dmd.aspetjournals.org/content/37/2/345.full

Benzodiazepine Antagonists:
Flumazenil is a recently discovered pharmacologic antagonist of the CNS effects of benzodiazepines. It acts by binding CNS benzodiazepine receptors and competitively blocking benzodiazepine activation of inhibitory GABAergic synapses. Animal studies and some human studies appear to demonstrate that flumazenil has weak intrinsic agonist activity; on the other hand, studies are inconclusive in demonstrating any inverse agonist effects of this agent. Evidence available suggests that flumazenil is well tolerated in human beings over a broad range of doses when given either orally or parenterally and does not produce serious adverse effects. In the setting of isolated benzodiazepine overdose, flumazenil is capable of completely reversing coma within one to two minutes, with this effect lasting between one and five hours. Repeat doses can be given safely to reverse recurrent effects of longer-acting benzodiazepines. Flumazenil is undergoing further evaluation by the Food and Drug Administration; should this drug receive approval, it is likely to be used in emergency departments as well as in a variety of other clinical settings. First, it could be used to effect rapid reversal of benzodiazepine-induced sedation that has been administered to facilitate medical, orthopedic, and surgical procedures, particularly in the event of inadvertent respiratory depression. Second, flumazenil might have a therapeutic role in the management of patients who have taken benzodiazepine overdoses. Although most of these patients can be managed successfully with supportive therapy alone, it is possible that the use of flumazenil may obviate the need for intubation and respiratory support in such patients and eliminate the possible adverse effects of even short-term endotracheal intubation. Finally, flumazenil could have both diagnostic and therapeutic value in patients with acute alterations of mental status of unknown etiology, particularly when possible drug overdose is a consideration. Because flumazenil appears to be specific in its antagonism of benzodiazepine-induced respiratory and CNS depression, it could be used empirically to confirm or exclude a role of benzodiazepines in the generation of mental status changes in the setting of overdose or coma of unknown origin. This in turn might obviate the need for further expensive (eg, computed tomography) and sometimes invasive (eg, lumbar puncture) diagnostic modalities. This might be particularly useful because there is nothing about benzodiazepine-induced coma that clearly distinguishes it from other causes of coma; thus, there are no signs or symptoms that may reasonably allow benzodiazepine overdose to be confirmed or eliminated on clinical grounds. Further studies will continue to define the ultimate use of this new agent.
http://www.ncbi.nlm.nih.gov/pubmed/1996802


Sources:
https://en.wikipedia.org/wiki/Benzodiazepine
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC545524/
http://pharmrev.aspetjournals.org/co...3.full#title10
 
My favorite Recreational drug, have abused them for years now and can gladly say never had even the slightest hint of withdrawal. And I take doses as high as 10mg Clonazepam in a night. If not used/abused daily you really aren't in jeopardy of developing a dependency.
 
^Not necessairilly. I mean I don't want to sound like a fear monger but it is possible to develop withdrawals after just a few days of heavy use. I knew this one kid who took something like 20-30 xanax bars over the course of two days, and after three days had a seizure-now of course those dosages are beyond insane, especially considering he had no tolerance either, but it is possible.
 
^Not necessairilly. I mean I don't want to sound like a fear monger but it is possible to develop withdrawals after just a few days of heavy use. I knew this one kid who took something like 20-30 xanax bars over the course of two days, and after three days had a seizure-now of course those dosages are beyond insane, especially considering he had no tolerance either, but it is possible.

Exactly, I had pretty bad rebound anxiety after just three days of using alprazolam (around 1mg per day)
 
^Not necessairilly. I mean I don't want to sound like a fear monger but it is possible to develop withdrawals after just a few days of heavy use. I knew this one kid who took something like 20-30 xanax bars over the course of two days, and after three days had a seizure-now of course those dosages are beyond insane, especially considering he had no tolerance either, but it is possible.


I'm surprised I've never had a seizure, then.

I've taken 20-30mg of xanax and klonopin at once for days at a time, then I'd stop.

I've even taken 3-15mg of klonopin a day (varied, everyday - usually took more than 3 a day) for about 2-3 months and quit cold turkey, was fine.

I wonder why...
 
I'm surprised I've never had a seizure, then.

I've taken 20-30mg of xanax and klonopin at once for days at a time, then I'd stop.

I've even taken 3-15mg of klonopin a day (varied, everyday - usually took more than 3 a day) for about 2-3 months and quit cold turkey, was fine.

I wonder why...

You are Superman!!!! Not too smart man. Everybody's body chemistry is diffrent, be thankful you didn't have a problem. If I were you I wouldn't start up again unless you desperately needed them for a medical condition. I'm sure you are young and feel indestructible but benzos don't discriminate.
 
You are Superman!!!! Not too smart man. Everybody's body chemistry is diffrent, be thankful you didn't have a problem. If I were you I wouldn't start up again unless you desperately needed them for a medical condition. I'm sure you are young and feel indestructible but benzos don't discriminate.


I may be young but not indestructible to benzo withdrawal.!

Never again, however, I do like to relax every now and then.

I feel like I am just less susceptible to seizures as I quit gabapentin cold turkey, too. (3600mg/day)
 
Why is it that midazolam is soluble in water and okay to shoot yet its ratio is 0.024mg/ml? Am I missing something?

Wouldn't that make clonazepam (0.1mg / ml) safer to shoot?
 
Im unable to make a new thread because im on mobile and it just wont work for some reason.

But I have a question worth asking before taking action. I have acquired 3 bars, but the thing is I just got over a 2 week withdrawal mostly valium and xanax sometimes klonopin but not very much. Ive been clean from all GABA drugs for atleast a month now, im wondering if I take any amount of these bars will my withdrawals flare back up or what? When is it safe to take any again, in all honesty I miss GABA drugs so much
 
I mean, if it's worth it to risk starting withdrawals again. IME it really takes about two months to completely be withdrawal free from benzos (and even at that point I wouldn't be sleeping too great)-IDK if that's normal or not.

If you're going to take them I'd try to take small dosages, like no more then a mg, and try to space those dosages out with a few days between.
 
Im unable to make a new thread because im on mobile and it just wont work for some reason.

But I have a question worth asking before taking action. I have acquired 3 bars, but the thing is I just got over a 2 week withdrawal mostly valium and xanax sometimes klonopin but not very much. Ive been clean from all GABA drugs for atleast a month now, im wondering if I take any amount of these bars will my withdrawals flare back up or what? When is it safe to take any again, in all honesty I miss GABA drugs so much

It also depends how long you were dependent on them, one dose might reset your withdrawal for a week or two easily.
 
I mean, if it's worth it to risk starting withdrawals again. IME it really takes about two months to completely be withdrawal free from benzos (and even at that point I wouldn't be sleeping too great)-IDK if that's normal or not.

If you're going to take them I'd try to take small dosages, like no more then a mg, and try to space those dosages out with a few days between.
@adder
Thanks for the advice guys, its not worth it, it was the worst 2-3 weeks of my life, also was a cold turkey WD. Worse than hell on earth, just going to shelf them for an emergency, got acouple more today too I dont know why though lol pure torture, again thanks guys
 
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I have done the same with opiats. Being clean cloth to four weeks and then taking a dosage and experience wth drawl again for a few days. Not full blown, but enough to put me back to bed.

Just to make it sure: This was opiats, not benzo's. But hopefully my example can cause you not to do it.
 
I have done the same with opiats. Being clean cloth to four weeks and then taking a dosage and experience wth drawl again for a few days. Not full blown, but enough to put me back to bed.

Just to make it sure: This was opiats, not benzo's. But hopefully my example can cause you not to do it.
Oh yeah been there man, happens almost every other week I just got over severe WD from nucynta for taking a small dose and was bed ridden for 2-3 days ate 2-3 zofran for those 2 days and it still couldnt tame the nausea, without those I wouldve been sick as hell. Still WDing but nothing even close to how I was, right now I just have insomnia and minor sweats. I was clean for like 2-3 weeks, and before that a month. Thats actually why I asked the question because no way im even taking the chance of that with xanax. Thanks for your input brother
 
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Do you think use of benzos once or twice a week for years would have a negative impact on cognitive function? Does anyone have any info on that?
 
^Who knows? How has that regime been for you chasingabee? Do you feel like shit in between doses & on those days off and what benzos are we talking about?
 
I take diazepam or alprazolam trying not to do it more than once a week, about 20mg diazepam or 2mg alprazolam for bad anxiety. Been doing it a few years. Usually I feel more anxious for a couple of days and have a hard time concentrating with my brain.
 
I take diazepam or alprazolam trying not to do it more than once a week, about 20mg diazepam or 2mg alprazolam for bad anxiety. Been doing it a few years. Usually I feel more anxious for a couple of days and have a hard time concentrating with my brain.
That sounds like rebound anxiety. Have you tried other options like therapy or maybe stuff like hydroxizine ? Imo hydroxizine is really great in stopping a panic attack and it's not as addictive/abusable as benzos.

Here's a pretty recent study claiming that
The risk of dementia is slightly higher in people with minimal exposure to benzodiazepines but not with the highest level of exposure. These results do not support a causal association between benzodiazepine use and dementia.
http://www.bmj.com/content/352/bmj.i90
 
I'm curious if any of you snort your benzos. I have severe anxiety and discovered that snorting doesn't make me as tired and is more effective when i am really struggling. Is there any risk to this?
 
I'm curious if any of you snort your benzos. I have severe anxiety and discovered that snorting doesn't make me as tired and is more effective when i am really struggling. Is there any risk to this?

Well, snorting decreases the bioavailability of most benzos and snorting pills is always bad for your lungs because of the fillers.
Have you tried taking them sublingually ?
 
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