EADD Benzo Discussion V. Waking up in a Wakefield skip

[SpiralusSancti]

I’m just reflecting on nitrobenzos it generally. Have no idea about clobazam beyond being praised by some people here and having different structure than most standard benzos.

But clonazepam is example of a benzo that ime is far more dangerous for beginners (not counting a lot of RCs ofc) than most benzos and doesn’t really work after you had your honey moon/years with benzos. Many years ago I would take clonazepam on very rare occasions and with sole intention to get really fucked up with my ex, we would do 2 – 3mg max and get high that lasted 24+ hours. And even back than, with 0 tolerance to benzos I could esaly do 50mg+ of diazepam and smoke weed along and not really care for it while she would just fall asleep from enough diazepam.

And when my tolerance was so high that I would hardly get any buzz even from equivalent of 100mg+ of diazepam, fucking 5mg of nitrazepam would make me fall asleep, weird as fuck ime. And 5mg nitrazepam pills are considered here as “baby pills” working only for people who haven’t extensively and with dedication abused and used benzos and all kinds of drugs but my experience with nitrazepam is absolutely opposite. Worth noting is that willing not to fall asleep on nitrazepam is easy and you have to get to bad, relax and wait for it to kick in, otherwise it’s useful ime. Few times I did nitrazepam during day I also got some effects inconsistent with my tolerance at the time. If I was in a mindset were getting high from benzos doesn’t sound disgusting and had nitrazepam I could see myself ending in a lot of problems. For a reason (at least here) most doctors prefers to prescribe 10x 5mg of this at a time and avoid prescribing packs with 30 pills or 20mg pills. Still I know cases of people with PTSD who have it prescribed for sleep for decades but that is acceptable case for nitrazepam use imho.

 

[Fertile]

Is clonazepam a nitrobenzodiazepine @Fertile?

Yes - nitrazepam, nimetazepam, fludiazepam and clonazepam are all nitrobenzodiazepines. I think some IDIOT RC vendors have made things like flunitrazolam - and that stuff really will have a TI LOWER than heroin, for example.

We had 19 novel benzodiazepines made and tested, only 2 reached market in bulk - pyrazolam and diclazepam. Why? Because we KNEW that if someone took say 100 tablets then while they may be dazed and confused, they would be OK.

We even messed with nitrobenzodiazpines to see if we could make them less toxic. We did, but the compound was too costly. A shame, because those that tried it (pynazolam 10mg) all noted the huge euphoria. So we wondered WHY it was so euphoric. Because it's a huge serotonin releaser and reuptake inhibitor....

We even wanted to patent it as an antidepressant, but the rats & mice all self-administered like mad which is a good measure of how abusable a compound it is. It was not like diclazepam (for example) as rats trained to differentiate did not substitute pynazolam when they had been trained for doclazepam.

I was still pleased to discover we had NAILED why benzos are euphoric. It's a5b1y1 affinity - same subreceptor class as as alcohol. It's not even like alcohol, bit the a5b1y1 is WHY people enjoy benzos but Z-drugs are considered much less euphoric.

 

[Forever Changes]

I *know* this is from wikipedia and so therefore must be treated with caution as it might not be correct, but:

Nitrazepam has been associated with severe hepatic disorders, similar to other nitrobenzodiazepines. Nitrobenzodiazepines such as nitrazepam, nimetazepam, flunitrazepam, and clonazepam are more toxic to the liver than other benzodiazepines as they are metabolically activated by CYP3A4 which can result in cytotoxicity. This activation can lead to the generation of free radicals and oxidation of thiol, as well as covalent binding with endogenous macromolecules; this results, then, in oxidation of cellular components or inhibition of normal cellular function. Metabolism of a nontoxic drug to reactive metabolites has been causally connected with a variety of adverse reactions.

Nitrazepam - Wikipedia

en.wikipedia.org

 

[axe battler]

Oh, sorry I didn't see it when I searched for nitrobenzos but clearly it is. I still think as long as you're experienced with benzos it's kinda safe. If you're you're not mixing with other depressants, but could be wrong. Hasn't really but me off it anymore than the other benzos I can't even take anymore, they're all too bloody addictive for me

 

[Fertile]

I *know* this is from wikipedia and so therefore must be treated with caution as it might not be correct, but:

Nitrazepam - Wikipedia

en.wikipedia.org

I had not read this, We DID believe that the body reduced the nitro to an amino and THAT is why nitrobenzodiazepines are toxic. But we were working with acute toxicity models. I might add that the body is generally regarded as being an 'oxidative instrument' and so reduction is kind of counterintuitive but anyone who knows the Kreb cycle KNOWS the body will reduce.

So I'm not sure if the article is regarding chronic toxicity or acute toxicity. I just know that in Sweden where nitrobenzodiazepines were widely prescribed, 70% of fatal, intentional overdoses were due to nitrobenzodiazepines ALONE. No alcohol, no other CNS depressant and actually no other drug.

So I guess you can see WHY we avoided them. The cost is no different (China sells ALL of the appropriately substituted benzophenones readily - in fact I had to spend a few days talking to them and doing 'back of a fag packet' calculations to find the very CHEAPEST - and per dose diclazepam IS.

So please, do avoid all of the RC nitrobenzodiazepines. They really are a lot more toxic.

But maybe I'm a moron because I thought outcomes (people not dying or doing crazy stuff) was the best way to avoid RCs becoming highlighted first in the media and then in law enforcement.

I admit we should have made U-47700 tablets (5mg = 25mg of oxycodone) so that people could be sure of what they had taken... but someone in the US offered an amazing price for the rights to distribution in that area and they did not feel so constrained.

BTW Benzo research goes on as does opioid research. We have a legal U-47700 analogue that is x4 more potent and has a higher TI. But I do not suppose we could produce it as cheaply as Mexicans make fentanyl. Still - I do not know anyone who has tried both who thought fentanyl was better. U-93951 has a T1/2 of 6 hours so rather than needing 5 'dirty 30s' to sustain a habit, just 3 (or maybe even 2) of the U4 analogue will keep someone well.

I think I've mentioned it, but never said how it's made and who makes it. I like to give - but I also like to eat, live indoors and not be cold.

 

[Bleaney]

Yes - nitrazepam, nimetazepam, fludiazepam and clonazepam are all nitrobenzodiazepines. I think some IDIOT RC vendors have made things like flunitrazolam - and that stuff really will have a TI LOWER than heroin, for example.

We had 19 novel benzodiazepines made and tested, only 2 reached market in bulk - pyrazolam and diclazepam. Why? Because we KNEW that if someone took say 100 tablets then while they may be dazed and confused, they would be OK.

We even messed with nitrobenzodiazpines to see if we could make them less toxic. We did, but the compound was too costly. A shame, because those that tried it (pynazolam 10mg) all noted the huge euphoria. So we wondered WHY it was so euphoric. Because it's a huge serotonin releaser and reuptake inhibitor....

We even wanted to patent it as an antidepressant, but the rats & mice all self-administered like mad which is a good measure of how abusable a compound it is. It was not like diclazepam (for example) as rats trained to differentiate did not substitute pynazolam when they had been trained for doclazepam.

I was still pleased to discover we had NAILED why benzos are euphoric. It's a5b1y1 affinity - same subreceptor class as as alcohol. It's not even like alcohol, bit the a5b1y1 is WHY people enjoy benzos but Z-drugs are considered much less euphoric.

Pyrazolam was ace, shame it was only available for such a short time.

Is there any explanation as to why practically any benzo is so euphoric on the first time of using, and then it's seldom possible to re-capture that same magic ever again, unless a very long break is taken from that type of benzo?

Maybe it's just the way benzos affect me, and the way I'm wired for them. Heroin could be a similar well known example of so many people reportedly having said the same thing about the first time of use being euphoric and then never being able to recapture that magic ever again.

 

[axe battler]

Yeah, I feel exactly the same. Best to switch benzos up and take breaks. And opiates too. But there's loads: pregabalin, phenibut, mdma, speed, coke/crack all spring to mind.

 

[Fertile]

Pyrazolam was ace, shame it was only available for such a short time.

Is there any explanation as to why practically any benzo is so euphoric on the first time of using, and then it's seldom possible to re-capture that same magic ever again, unless a very long break is taken from that type of benzo?

Maybe it's just the way benzos affect me, and the way I'm wired for them. Heroin could be a similar well known example of so many people reportedly having said the same thing about the first time of use being euphoric and then never being able to recapture that magic ever again.

I am truly honoured that such a well regarded BLr would say such a thing. It was the 19th compound we had made. We waned it to be IMPOSSIBLE to OD on, a good anxiolytic but not something that would lead to serious dependence.

FYW I took 100mg of pyrazolam to test the safety. I slept for a week but I was fine. I am totally bonded with the idea that the guy who designs it should be first into man.

But now a lot of scientists are catching up and saying that pyrazolam is actually a very good medicine. I will not see a penny for my work but it helps people, how do you calculate a profit? But we made 2 others which were better. And anyway -

-Pynazolam which is a seroonin releaser and reuptake inhibitor (think MDMA with no stimulant action)
-Pyeyzolam which is the best alcohol mimic we found (funded by Professor David Nutt at Imperial Collage, London) but TBH he offered us shares or money. We took the money because we told him that the entire alcohol industry would pull strings to prevent it getting a licence - and he could not get a licence.

The cute thing is that the Chinese know of them but cannot make them. It took US about 30 odd attempts to find facile route.

 

[Forever Changes]

I had not read this, We DID believe that the body reduced the nitro to an amino and THAT is why nitrobenzodiazepines are toxic. But we were working with acute toxicity models. I might add that the body is generally regarded as being an 'oxidative instrument' and so reduction is kind of counterintuitive but anyone who knows the Kreb cycle KNOWS the body will reduce.

So I'm not sure if the article is regarding chronic toxicity or acute toxicity. I just know that in Sweden where nitrobenzodiazepines were widely prescribed, 70% of fatal, intentional overdoses were due to nitrobenzodiazepines ALONE. No alcohol, no other CNS depressant and actually no other drug.

So I guess you can see WHY we avoided them. The cost is no different (China sells ALL of the appropriately substituted benzophenones readily - in fact I had to spend a few days talking to them and doing 'back of a fag packet' calculations to find the very CHEAPEST - and per dose diclazepam IS.

So please, do avoid all of the RC nitrobenzodiazepines. They really are a lot more toxic.

But maybe I'm a moron because I thought outcomes (people not dying or doing crazy stuff) was the best way to avoid RCs becoming highlighted first in the media and then in law enforcement.

I admit we should have made U-47700 tablets (5mg = 25mg of oxycodone) so that people could be sure of what they had taken... but someone in the US offered an amazing price for the rights to distribution in that area and they did not feel so constrained.

BTW Benzo research goes on as does opioid research. We have a legal U-47700 analogue that is x4 more potent and has a higher TI. But I do not suppose we could produce it as cheaply as Mexicans make fentanyl. Still - I do not know anyone who has tried both who thought fentanyl was better. U-93951 has a T1/2 of 6 hours so rather than needing 5 'dirty 30s' to sustain a habit, just 3 (or maybe even 2) of the U4 analogue will keep someone well.

I think I've mentioned it, but never said how it's made and who makes it. I like to give - but I also like to eat, live indoors and not be cold.

But does Clonazepam count as an RC? I took 6mg the other night and didn't feel much except it perhaps made it easier for me to sleep. No idea about the state of my liver unless I get a blood test done

 

[axe battler]

But does Clonazepam count as an RC? I took 6mg the other night and didn't feel much except it perhaps made it easier for me to sleep. No idea about the state of my liver unless I get a blood test done

Nah, not an RC. 6mg is a pretty big dose, though. If it does fuck your liver, fair enough it's probably bad, but I find it one of the less spannering benzos out there. Not as bad as nitrazepam, alprazolam or even diazepam IMO. Plus it lasts a good amount of time. I really don't think you'd ever od on it unless you mixed with opiates or booze. But even then, I think @nznity said he takes up to 8mg a day, often with diazepam, morphine and sometimes alcohol, too. Not saying this isn't risky behaviour, but in my rather extensive experience with it, I've never came close to ODing. Only time I ever has was when I blacked out taking clonazOLAM, but I took nearly 50mg with methadone, heroin and diazepam too. Now that's outrageous.
Agreed though @Fertile that pyrazolam was a great RC benzo for anxiety without knocking you out or making you blackout.

 

[fastandbulbous]

Ñìtrobenzos certainly have real soporific effect. First discovered Mogadon (5mg nitrazepam), 40 years ago and still think them the best sleeping non barbiturates tablèts

 

[fastandbulbous]

I don't think clonazepam is a nitrobenzodiazepine. I think he's getting it mixed up with clonazolam as clobezam isn't a nitro either, but clonazolam is.
I think clonazepam is commonly used in INTENTIONAL suicides as it's a very commonly prescribed psych med, especially in the USA.

It is...

 

[Fertile]

Ñìtrobenzos certainly have real soporific effect. First discovered Mogadon (5mg nitrazepam), 40 years ago and still think them the best sleeping non barbiturates tablèts

I GUESS is has a higher affinity for the a1 subunit than anxiolytic benzodiazepines? After all, the Z-drugs are a1 selective and they are also hypnotics.

Did anyone find that it increases levels of serotonin which also has a hypnotic action? We added a triazolo ring so it wouldn't have much a1 affinity and found it was not a hypnotic (at normal doses) BUT unexpectedly caused a huge increase in serotonin. Pynazolam was almost identical (subjectively) to Serotonia (p,4-dimethylaminorex AKA dimethylaminorex).

For optimum serotonin release/reuptake inhibition the amide needs to be tertiary (so I can see why nimetazepam & flunitrazepam abused in some nations) and ideally a triazolo or imidazo ring to add enough biosteric bulk to reduce a1 affinity. Even with one of those rings (that usually increases potency by an order of magnitude over the simple 3-ring amide containing examples, the serotonin-mediated euphoria only REALLY kicks in at about 10mg.

I DID search through the literature but could not find anyone who had noted the serotonin action before us.

Literature References:

Prepn: Sternbach et al., J. Med. Chem. 6, 261 (1963); O. Keller et al., US 3121076 (1964 to Hoffmann-La Roche). Crystal structure: G. Gilli et al., Acta Crystallogr. 33B, 2664 (1977). Pharmacokinetic studies: Rieder, Arzneim.-Forsch. 23, 212 (1973); L. Kangas, Acta Pharmacol. Toxicol. 45, 16 (1979). Toxicity data: Randall et al., Schweiz. Med. Wochenschr. 95, 334 (1965). Review: Rieder, Wendt in Benzodiazepines, S. Garattini et al., Eds. (Raven Press, New York, 1973) pp 99-127. Comprehensive description: H. Y. Aboul-Enein et al., Anal. Profiles Drug Subs. 9, 487-517 (1980).
Properties: Yellow crystals from ethanol, mp 224-226°. uv max (0.1N H2SO4): 277.5 nm (E1%1cm 1500). Sol in alc, acetone, chloroform, ethyl acetate. Practically insol in water, ether, benzene, hexane. LD50 orally in rats: 825 ±80 mg/kg (Randall)

 

[axe battler]

I do enjoy nitrazepam a lot more than a lot of benzos, but think it's due to the heavy sedation and muscle relaxant qualities for me personally.
Would love to try nimetazepam aka "happy 5s".

 

[Forever Changes]

Ñìtrobenzos certainly have real soporific effect. First discovered Mogadon (5mg nitrazepam), 40 years ago and still think them the best sleeping non barbiturates tablèts

What do you think about the claim that they are more damging to the liver than other Benzos?

 

[Fertile]

What do you think about the claim that they are more damging to the liver than other Benzos?

https://ars.els-cdn.com/content/image/1-s2.0-S0006295217304379-fx1_lrg.jpg

The above image shows the nitrazepam metabolite responsible for liver injury and another that is teratotoxic. Sadly, nitrazepam was introduced 10 years before the Ames test came into use and so it's only BECAUSE of people suffering liver injury that researchers went back to test the drug and find the mode of toxcity as late as 2017.

Interestingly flunitrazepam and clonazepam are also noted to cause liver injury, especially when combined with alcohol. It's my opinion that if nitrazepam (and the other nitrobenzodiazepines) were discovered tomorrow, they would never have reached the marketplace.

As it is RCs like nitrazolam and flunitrazolam have been associated with severe liver damage. That is what happens when people who do not understand medicinal chemistry produce and supply compounds with no idea about the potential damage they can cause. I've said this before but sooner or later someone is going to release something that's going to cause chronic damage in a lot of users. As it is, who knows just how much of those RCs people have taken - it will only as the liver injury becomes severe that people will know they were at risk,

That's why only pyrazolam and diclazepam were ultimately produced by us. Yes, we made nitrobenzodiazepines but the TIs were much less favourable and so were rejected. I'm not virtue signalling - but that is HOW one is supposed to develop ned drugs. MOST will be rejected.

 

[Dankyspanky710]

Most of the Clonazepam submitted to Wedinos recently seems to be coming back as genuine. Probably makes it one of the better bets at the moment, seeing as it's a pretty solid all rounder of a benzo.

Totally agreed - I have like 1000 rivotril from
Overseas and I bought this 260 dollar benzo tester and I did this huge test and from what I tested which was rivotril that had the red arrow on the back and the rivotril without it that has veen around most recently are good they were positive for clonazepam as well as the Ksalol which used to be perforated and isn't anymore ( the packaging) and that came back as Xanax quick too. As well as two different brands Valium , I love the dark web I just hate that I could click a button and relapse on the best heroin fentanyl free in the world but having that power is kinda enough for me not to do it

 

[Smuck_Hey_Dee_Hewitt]

u can def chill on bromaz.

To me it feels like a stronger pound by pound version of Diazepam even . You can definitely chill on that .

 

[Bleaney]

I ordered some galenkia alprazolam recently. I have no idea if they actually are what they are supposed to be. I've tried one and it didn't taste as bitter as xanax bars I've had in the past.

I've sent one off to Wedinos to be tested. I won't be overly put out if they turn out to be Bromozolam, but would obviously prefer them to be kosher Aprazolam. More sure of getting properly dosed pills that way for one major point, if they are genuine pharma pills and not fakes.

As I've never had them before, I had trouble discerning what colour they are supposed to be for filling out the wedinos from, there was no option or word that I know for the cross between off white to grey /light green, or light blue that they are, so I selected "colourless". Wasnt sure what that word meant until I saw these pills. Is that normal for this brand of pills?

 

[axe battler]

I ordered some galenkia alprazolam recently. I have no idea if they actually are what they are supposed to be. I've tried one and it didn't taste as bitter as xanax bars I've had in the past.

I've sent one off to Wedinos to be tested. I won't be overly put out if they turn out to be Bromozolam, but would obviously prefer them to be kosher Aprazolam. More sure of getting properly dosed pills that way for one major point, if they are genuine pharma pills and not fakes.

As I've never had them before, I had trouble discerning what colour they are supposed to be for filling out the wedinos from, there was no option or word that I know for the cross between off white to grey /light green, or light blue that they are, so I selected "colourless". Wasnt sure what that word meant until I saw these pills. Is that normal for this brand of pills?

Sort of. Ksalol, even the legittos had very little colour to them, but I'd say light blue was the usual colour. If they were bright blue you definitely got burned. Bromazolam isn't bitter IMO, so they may just be underdosed, which is a major problem with Galenika stuff, I reckon. Especially the diazepam.