RCs Pyrazolam Megathread

[SpiralusSancti]

Beware those that like to take benzos sublingually, though. It is water soluble which is unusual for a benzo, but it's acidic as fuck, so burns/ulcers occur if you try and take the pellets sublingually.

Just as I was thinking how it would be cool to make a nasal spray with this I read what you wrote.
I guess it must be as bad or worse for the nose so it ain't option.

 

[AlsoTapered]

It's water solubility and basic nature are because in place of the usual (2-substituted) pendent benzene ring, it has a 2-pyridyl motif.

It would take a while to list all the reasons we chose that but solubility was one issue. It's not super-absorbent in water but their are alternatives to water for use in a nasal spray.

 

[SpiralusSancti]

It's water solubility and basic nature are because in place of the usual (2-substituted) pendent benzene ring, it has a 2-pyridyl motif.

It would take a while to list all the reasons we chose that but solubility was one issue. It's not super-absorbent in water but their are alternatives to water for use in a nasal spray.

I'm concerned that burns/uclers from sublinguall use are a good sign that it shouldn't be put in the nose either.

 

[JackARoe]

I actually had the chance to test out pyrazolam before a physical exam. I always get nervous at doctors. So I have a lot of anxiety. But just under 1 mg and it took away all that anxiety and I felt good. That is about the best I can get out of benzos. And a situation that I would use them.

I admit when I research these things here and reddit the comments are funny. Ex.

"pyrazolam makes me feel so good, but it is not recreational"
"pyrazolam makes me feel the best out of any benzo but does not get me high"
"I just feel normal on pyrazolam"
"pyrazolam is crap"
"etizolam is crap...."
"pyrazolam gets me higher than any benzo...."

The normal range of responses to any benzo. I think the funniest insult thrown at a benzo is when someone said etizolam feels like diphenhydramine. Then the next person says that about flualprazolam or some benzo. Very funny responses as they are so individual.

I will say pyrazolam should be used as alprazolam is used. I mean I can get sleepy on it but I don't take benzos a lot. But I was aware at how quick it got rid of that anxiety in my chest. I consider it a good benzo. Stronger than is posted about here. 1 mg is strong for me. .5 seems best for those situations.

Also reading through the thread I notice alsotappered said it is not detectable 24 hours after taking. That may be one of the quickest benzos to exit the body. I like that. Not keen on these 48 hour half lives. The quicker it can exit me the better.

 

[axe battler]

I'm concerned that burns/uclers from sublinguall use are a good sign that it shouldn't be put in the nose either.

Yeah, I wouldn't bother putting it up my nose. I may have tried snorting a pellet waaaaybback when it was legal in the UK, but I can't remember if it was really painful, but due to the ulcers I'd get taking it s/l I'd deffo rule out long term nasal use.
Oral was fine and hit quick like alprazolam tbh.
I also agree it should be used in place of alprazolam. Far less likely to cause dickheadedness and blackouts, but a great anxiolitic.

 

[AlsoTapered]

Sublingual use of benzodiazepines - PubMed

Sublingual use of benzodiazepines

pubmed.ncbi.nlm.nih.gov

TO THE EDITOR: Benzodiazepines, available in oral, intravenous, and intramuscular dosage forms, are widely used in the treatment of anxiety, insomnia, and muscle spasms. Some of these agents are also employed in preoperative sedation and in the management of various seizure disorders. The sublingual use of two benzodiazepines (lorazepam and triazolam) was recently described in a review by Sussman.' That information, however, was based on anecdotal reports, according to the author (personal communication, Norman Sussman, M.D., New York University School of Medicine, April 1985).

Reports regarding this unique mode of benzodiazepine administration have been few. Caille and colleagues studied the pharmacokinetic properties of various lorazepam formulations, each given as asingle 2-mg dose! Sublingually administered lorazepam was absorbed more rapidly than that given orally. Furthermore, the sublingual route compared favorably with intramuscular injection into the deltoid muscle. It should be noted that three distinct tablet formulations were tested sublingually, one of which was the trade oral tablet. The absorption of the trade oral tablet when given sub lingually was superior to the same tablet given orally, but was somewhat inferior to a special sublingual tablet. Using the intramuscular preparation as the reference standard, the bioavailability of the oral tablet was higher when administered orally rather than sublingually. The same tablet, when given orally, was slightly more bioavailable than the standard intramuscular form, as was the special sublingual tablet.

Greenblatt and associates in a similar study reported rapid and nearly complete absorption of lorazepam given sublingually either as the trade oral tablet or a specially formulated sublingual tablet using single 2-mg doses. Orally administered lorazepam was comparable with that given by the sublingual route. The intramuscular injection into the deltoid muscle was found to be the most rapidly absorbed of the three preparations, but differences in absorption were reportedly not significant. Gale et al. tested the efficacy of a sublingual preparation of lorazepam against an intramuscular injection of the same as premedication for 150 patients undergoing minor gynecological surgery. A single dose ranging from 2 to 4 rng was selected depending on the patient's weight. Those receiving the drug sublingually had less recall, an earlier onset of sedation, more drowsiness, and a longer recovery time than those who received the drug intramuscularly. The authors concluded that sublingual lorazepam was superior due to its rapid absorption resulting in more drowsiness and amnesia.' It is not known, however, whether the sublingual preparation used in this study was the trade oral tablet or a specially formulated sublingual tablet.
The delivery of lorazepam and other benzodiazepines by the sublingual route may offer significant advantages and increase their versatility. The trade oral tablet currently available in the U.S. is rapidly and nearly completely absorbed from both the oral mucosa and the gastrointestinal tract and, when used sublingually, compares favorably with intramuscular administration. Sublingual use may eliminate the need for intramuscular injections, which are often associated with pain and discomfort. The intramuscular form also requires refrigeration, has a short shelf-life, and is more expensive than oral tablets.' The sublingual route may also be used in patients who are unable to swallow, regardless of the etiology. A more attractive use of sublingual lorazepam may be in patients who are allowed nothing by mouth for whom parenteral administration is the only current alternative. In view of these possible benefits, we believe that the sublingual use of lorazepam and other benzodiazepines warrants further study to correlate pharmacokinetic data with concrete clinical evidence of efficacy.

KARIM A. CALIS, B.S.Pharm.
Pharm.D. Student
School of Pharmacy
University of Maryland
Baltimore, Maryland 21201
RITA A. MITSCH, Pharm.D.

Clinical Assistant Professor
School of Pharmacy
University of Maryland, and
Clinical Pharmacist
Franklin Square Hospital
Baltimore, Maryland 21237

I've tried around 30 different benzodiazepines and in every single case onset is comparable to IM injection. Pyrazolam was specifically designed to be water soluble as we initially intended to produce sublingual films BUT the only manufacturer able to produce the films was based in Japan and the lead-time was about 8 months. Too long since we had no idea how long it would take a Chinese vendor to offer a knock-off version. We need not have worried. I've been shown samples of Chinese-made pyrazolam and in every case it was yellow suggesting the presence of the intermediate thioamide. Now the thioamide isn't toxic BUT anyone who is happy to allow an impure produce is just as likely to leave the intermediate acetyl hydrazide and that most certainly IS something to be concerned about.

In nations like India sublingual clonazepam (banana flavoured) is produced for children. I do not think making tablets taste 'nice' is conducive to safety but their you go, it's not a guess, not even an educated guess. In fact, I note online that 'banana klonapin' was noted by people buying from shady sources.

BTW oral bioavailability of benzodiazepines is still very high but pyrazolam was specifically designed to be a selective anxiolytic with a fast onset and believe me, 1mg of the powder under the tongue worked in a matter of seconds and any you do swallow still winds up with 83% (oral) bioavailability.

 

[emkee_reinvented]

I actually had the chance to test out pyrazolam before a physical exam. I always get nervous at doctors. So I have a lot of anxiety. But just under 1 mg and it took away all that anxiety and I felt good. That is about the best I can get out of benzos. And a situation that I would use them.

I admit when I research these things here and reddit the comments are funny. Ex.

"pyrazolam makes me feel so good, but it is not recreational"
"pyrazolam makes me feel the best out of any benzo but does not get me high"
"I just feel normal on pyrazolam"
"pyrazolam is crap"
"etizolam is crap...."
"pyrazolam gets me higher than any benzo...."

The normal range of responses to any benzo. I think the funniest insult thrown at a benzo is when someone said etizolam feels like diphenhydramine. Then the next person says that about flualprazolam or some benzo. Very funny responses as they are so individual.

I will say pyrazolam should be used as alprazolam is used. I mean I can get sleepy on it but I don't take benzos a lot. But I was aware at how quick it got rid of that anxiety in my chest. I consider it a good benzo. Stronger than is posted about here. 1 mg is strong for me. .5 seems best for those situations.

Also reading through the thread I notice alsotappered said it is not detectable 24 hours after taking. That may be one of the quickest benzos to exit the body. I like that. Not keen on these 48 hour half lives. The quicker it can exit me the better.

The fisrt pellets contained 0.5 mg, but for me it starts working noticeable at about 3 mg. Even then it stays functional, it does make me a bit sleepy. but way lesss forced then Alprazolam. So yes totally agree on that. Its imo the better of the two. But hey what do dr's know .

 

[JackARoe]

The fisrt pellets contained 0.5 mg, but for me it starts working noticeable at about 3 mg.

Yeah I have a low tolerance. But I wonder if those .5 pills from years ago were bunk? Most people say they had to take a lot if you go back in this thread.. And other people said it did nothing. But I can feel .5 mg. I can feel it as it kicks in and takes the anxiety away. Of course it could be low tolerance for me. Some people here can take larger amounts of drugs too naturally.

I notice you found mulungu emkee. I have said it for years, it will become important in the years ahead and a valid drug will come of it. I was using mulungu to come down from psychedelics before I used etizolam. A handful of the bark simmered for 20 minutes for sure affected me like 10 mgs of diazepam. The only issue is there is a lot of bunk bark out there. Valid bark works great though.

 

[axe battler]

Sublingual use of benzodiazepines - PubMed

Sublingual use of benzodiazepines

pubmed.ncbi.nlm.nih.gov

TO THE EDITOR: Benzodiazepines, available in oral, intravenous, and intramuscular dosage forms, are widely used in the treatment of anxiety, insomnia, and muscle spasms. Some of these agents are also employed in preoperative sedation and in the management of various seizure disorders. The sublingual use of two benzodiazepines (lorazepam and triazolam) was recently described in a review by Sussman.' That information, however, was based on anecdotal reports, according to the author (personal communication, Norman Sussman, M.D., New York University School of Medicine, April 1985).

Reports regarding this unique mode of benzodiazepine administration have been few. Caille and colleagues studied the pharmacokinetic properties of various lorazepam formulations, each given as asingle 2-mg dose! Sublingually administered lorazepam was absorbed more rapidly than that given orally. Furthermore, the sublingual route compared favorably with intramuscular injection into the deltoid muscle. It should be noted that three distinct tablet formulations were tested sublingually, one of which was the trade oral tablet. The absorption of the trade oral tablet when given sub lingually was superior to the same tablet given orally, but was somewhat inferior to a special sublingual tablet. Using the intramuscular preparation as the reference standard, the bioavailability of the oral tablet was higher when administered orally rather than sublingually. The same tablet, when given orally, was slightly more bioavailable than the standard intramuscular form, as was the special sublingual tablet.

Greenblatt and associates in a similar study reported rapid and nearly complete absorption of lorazepam given sublingually either as the trade oral tablet or a specially formulated sublingual tablet using single 2-mg doses. Orally administered lorazepam was comparable with that given by the sublingual route. The intramuscular injection into the deltoid muscle was found to be the most rapidly absorbed of the three preparations, but differences in absorption were reportedly not significant. Gale et al. tested the efficacy of a sublingual preparation of lorazepam against an intramuscular injection of the same as premedication for 150 patients undergoing minor gynecological surgery. A single dose ranging from 2 to 4 rng was selected depending on the patient's weight. Those receiving the drug sublingually had less recall, an earlier onset of sedation, more drowsiness, and a longer recovery time than those who received the drug intramuscularly. The authors concluded that sublingual lorazepam was superior due to its rapid absorption resulting in more drowsiness and amnesia.' It is not known, however, whether the sublingual preparation used in this study was the trade oral tablet or a specially formulated sublingual tablet.
The delivery of lorazepam and other benzodiazepines by the sublingual route may offer significant advantages and increase their versatility. The trade oral tablet currently available in the U.S. is rapidly and nearly completely absorbed from both the oral mucosa and the gastrointestinal tract and, when used sublingually, compares favorably with intramuscular administration. Sublingual use may eliminate the need for intramuscular injections, which are often associated with pain and discomfort. The intramuscular form also requires refrigeration, has a short shelf-life, and is more expensive than oral tablets.' The sublingual route may also be used in patients who are unable to swallow, regardless of the etiology. A more attractive use of sublingual lorazepam may be in patients who are allowed nothing by mouth for whom parenteral administration is the only current alternative. In view of these possible benefits, we believe that the sublingual use of lorazepam and other benzodiazepines warrants further study to correlate pharmacokinetic data with concrete clinical evidence of efficacy.

KARIM A. CALIS, B.S.Pharm.
Pharm.D. Student
School of Pharmacy
University of Maryland
Baltimore, Maryland 21201
RITA A. MITSCH, Pharm.D.

Clinical Assistant Professor
School of Pharmacy
University of Maryland, and
Clinical Pharmacist
Franklin Square Hospital
Baltimore, Maryland 21237

I've tried around 30 different benzodiazepines and in every single case onset is comparable to IM injection. Pyrazolam was specifically designed to be water soluble as we initially intended to produce sublingual films BUT the only manufacturer able to produce the films was based in Japan and the lead-time was about 8 months. Too long since we had no idea how long it would take a Chinese vendor to offer a knock-off version. We need not have worried. I've been shown samples of Chinese-made pyrazolam and in every case it was yellow suggesting the presence of the intermediate thioamide. Now the thioamide isn't toxic BUT anyone who is happy to allow an impure produce is just as likely to leave the intermediate acetyl hydrazide and that most certainly IS something to be concerned about.

In nations like India sublingual clonazepam (banana flavoured) is produced for children. I do not think making tablets taste 'nice' is conducive to safety but their you go, it's not a guess, not even an educated guess. In fact, I note online that 'banana klonapin' was noted by people buying from shady sources.

BTW oral bioavailability of benzodiazepines is still very high but pyrazolam was specifically designed to be a selective anxiolytic with a fast onset and believe me, 1mg of the powder under the tongue worked in a matter of seconds and any you do swallow still winds up with 83% (oral) bioavailability.

So the burns/ulcers are due to impurities and not due to the pH of pyrazolam? Or would you add ingredients to the strips to neutralise them?

 

[AlsoTapered]

So the burns/ulcers are due to impurities and not due to the pH of pyrazolam? Or would you add ingredients to the strips to neutralise them?

I have taken dozens of the original 0.5mg tablets sublingually with no issues whatsoever.

Now I've seen images of Chinese-made pyrazolam and it was YELOW and clumpy - I have no idea what the impurities were but I can 100% confirm that pure pyrazolam is white.

 

[axe battler]

I have taken dozens of the original 0.5mg tablets sublingually with no issues whatsoever.

Now I've seen images of Chinese-made pyrazolam and it was YELOW and clumpy - I have no idea what the impurities were but I can 100% confirm that pure pyrazolam is white.

I only ever bought it in pellet form back before the PSA, but every time I noticed it would burn when taken sublingually so fuck knows!

 

[AlsoTapered]

I only ever bought it in pellet form back before the PSA, but every time I noticed it would burn when taken sublingually so fuck knows!

Even when we optimized the synthesis, we still had to use preparative chromatography to obtain the 99.8% purity we deemed safe. But their is a hydrazide intermediate which we decided had to entirely be removed for the product to be safe. Now I'm just guessing that the Chinese didn't male the effort to remove it...

It's also a potential carcinogen so I wouldn't touch it.

In ours the 0.2% was bromazepam (the precursor) and thiobromazepam (one of the intermediates). Both are safe and indeed both are GABA PAMs but just not very potent so they essentially don't alter the subjective effects.

BTW another one from that series might be out soon. It's totally different but worthwhile.

 

[emkee_reinvented]

Yeah I have a low tolerance. But I wonder if those .5 pills from years ago were bunk? Most people say they had to take a lot if you go back in this thread.. And other people said it did nothing. But I can feel .5 mg. I can feel it as it kicks in and takes the anxiety away. Of course it could be low tolerance for me. Some people here can take larger amounts of drugs too naturally.

I notice you found mulungu emkee. I have said it for years, it will become important in the years ahead and a valid drug will come of it. I was using mulungu to come down from psychedelics before I used etizolam. A handful of the bark simmered for 20 minutes for sure affected me like 10 mgs of diazepam. The only issue is there is a lot of bunk bark out there. Valid bark works great though.

Aftter Kratom my vendor suddenly offered Mulungu. Whole bark and a extract. These both were so unique as inducer's of sleep they alway's kept a warm place in my brain.

FFWD 10 + year's and its widely available in many forms. As i developed a sleeping disorder in the recent past. The past week I bought a bag of the Bark. Look's genuine but I have not tested it so fingers crossed. If my memory is correct it should work like a charm. It made me sleep totally unlike a dr. s sleep aid would. Even Melatonine feels more psychoactive then Mulungu as it makes my dreams more lucid.

The best sleepaid imo I've encountered, natural and synthetic's. Works on the cholinergic system, Where Nicotin is a anxiolytic Mulungu acts opposit as anti-anxiolytic. That it also worked against seizure's, anxiety and asthma was new to me.

JackARoe did you ever feel anything from it? As to me it seemed clear off any noticeable activity, it just made me sleep real good. With dreams, no groginess when waking up.

 

[JackARoe]

^ I did feel the mulungu. Similar to how a small dose of diazepam hits but of course wore off quicker and cleaner. I have zero benzo tolerance and at that time had not even had a benzo in years. But coming down from a trip I could for sure feel the mulungu relax the body and mind. I did use it for a few years before I tried etizolam. For a while etizolam was all over and easier to get. I do need to revisit mulungu as the only thing I did not get was amnesia. A regular dose of a benzo will leave me with holes in my memory. Pyrazolam too. But mulungu just sort of slowed me down.

Amnesia from benzos is a very strange thing to me. To almost not feel anything, think you are about sober and then the next day can not remember a bunch of things is a little freaky. Makes me wonder how an amnesiac is used in medicine or if it is just a side effect of benzos.

 

[emkee_reinvented]

^ I did feel the mulungu. Similar to how a small dose of diazepam hits but of course wore off quicker and cleaner. I have zero benzo tolerance and at that time had not even had a benzo in years. But coming down from a trip I could for sure feel the mulungu relax the body and mind. I did use it for a few years before I tried etizolam. For a while etizolam was all over and easier to get. I do need to revisit mulungu as the only thing I did not get was amnesia. A regular dose of a benzo will leave me with holes in my memory. Pyrazolam too. But mulungu just sort of slowed me down.

Amnesia from benzos is a very strange thing to me. To almost not feel anything, think you are about sober and then the next day can not remember a bunch of things is a little freaky. Makes me wonder how an amnesiac is used in medicine or if it is just a side effect of benzos.

Wonder if Mulungu will beat a Benzo in regard's to getting you to sleep? Think so.

There were nights I took hands of Benzo's ( brotizolam, norflurazepam and/ or flubromazepam) only to become relaxed, Muscle relaxation, amnesia and residual grogginess. Without actual sleeping. But Mulungu had non of these aspects. Then again I was pretty Benzo naieve 15 + years ago. And had no sleeping disorder.

Read up in my med records online yesterday.
They write I have Apneu, so should not sleep on my back, and no deep sleep/ NREM. Which means every proces in your body gets disrupted. Healing, immune function, neurogenesis and memory a.o..

Ps. Opipramol an discontinued med also had this effect on me. Clean sleep, nothing that resembled a Benzo or Anti-Histamine.

 

[AlsoTapered]

Mulungu (Erythrina mulungu) appears to contain a mixture of alkaloids including erysotine and hypaphorine (and diverse other alkaloids in lower concentrations).

Now hypaphorine AKA (αS)-α-carboxy-N,N,N-trimethyl-1H-indole-3-ethanaminium, inner salt ANA tryptophan betaine which the body is able to decarboxylate to, wait for it, DMT and tryptophan. I'm sure people aware that the latter allows the body to readily produce serotonin which has previously been used as a sleep aid as the body is able to serotonin and melatonin.

https://www.sciencedirect.com/science/article/abs/pii/S0960894X08006392

 

[JohnnyVodka]

I actually had the chance to test out pyrazolam before a physical exam. I always get nervous at doctors. So I have a lot of anxiety. But just under 1 mg and it took away all that anxiety and I felt good. That is about the best I can get out of benzos. And a situation that I would use them.

I admit when I research these things here and reddit the comments are funny. Ex.

"pyrazolam makes me feel so good, but it is not recreational"
"pyrazolam makes me feel the best out of any benzo but does not get me high"
"I just feel normal on pyrazolam"
"pyrazolam is crap"
"etizolam is crap...."
"pyrazolam gets me higher than any benzo...."

The normal range of responses to any benzo. I think the funniest insult thrown at a benzo is when someone said etizolam feels like diphenhydramine. Then the next person says that about flualprazolam or some benzo. Very funny responses as they are so individual.

I will say pyrazolam should be used as alprazolam is used. I mean I can get sleepy on it but I don't take benzos a lot. But I was aware at how quick it got rid of that anxiety in my chest. I consider it a good benzo. Stronger than is posted about here. 1 mg is strong for me. .5 seems best for those situations.

Also reading through the thread I notice alsotappered said it is not detectable 24 hours after taking. That may be one of the quickest benzos to exit the body. I like that. Not keen on these 48 hour half lives. The quicker it can exit me the better.

I like it and use a (probably) close to placebo amount (0.5mg or less) to dampen down anxiety in situations were I don't want to be sedated.

 

[emkee_reinvented]

Mulungu (Erythrina mulungu) appears to contain a mixture of alkaloids including erysotine and hypaphorine (and diverse other alkaloids in lower concentrations).

Now hypaphorine AKA (αS)-α-carboxy-N,N,N-trimethyl-1H-indole-3-ethanaminium, inner salt ANA tryptophan betaine which the body is able to decarboxylate to, wait for it, DMT and tryptophan. I'm sure people aware that the latter allows the body to readily produce serotonin which has previously been used as a sleep aid as the body is able to serotonin and melatonin.

https://www.sciencedirect.com/science/article/abs/pii/S0960894X08006392

And erythravine and (+)-11α-hydroxy-erythravine.

Those you mention I have not even read about. Do they have similar action. Or other effects?
quoting Wiki about the leaves and bark effects by the two above.:

"traditional medicine as a sedative, to calm an overexcited nervous system, to lower blood pressure, and for insomnia and depression"

 

[emkee_reinvented]

I like it and use a (probably) close to placebo amount (0.5mg or less) to dampen down anxiety in situations were I don't want to be sedated. I'm assuming it would show up in a drugs test tho?

Or it has a ceiling where taking more is not feeling more. Which means I could just aswell be takin a 1/3 pellet?

Clobazam has a ceiling I just recently know, ideal for anxiety btw. Maybe Pyrazolam has one too. At higher doses it does get 'sleepier', 3 mg. Never took more.

Without answering your last question. Look it up its easy but not allowed to answer. Wondering atm how I could methaphorically answer it. And not breaking the rules. No the answer can easy be found check NCBI.com.

 

[JohnnyVodka]

Or it has a ceiling where taking more is not feeling more. Which means I could just aswell be takin a 1/3 pellet?

Clobazam has a ceiling I just recently know, ideal for anxiety btw. Maybe Pyrazolam has one too. At higher doses it does get 'sleepier', 3 mg. Never took more.

Without answering your last question. Look it up its easy but not allowed to answer. Wondering atm how I could methaphorically answer it. And not breaking the rules. No the answer can easy be found check NCBI.com.

Ah, okay, I didn't realise that question isn't allowed, so will edit. Certainly within the range I've taken it, effects ramp up with dosage, as you'd expect, and it is possible to become sleepy on a regular dose. (Most I've done in one go is ~1.5mg.) However, it's not what I'd use if encountering anxiety on stims or trying to get to sleep after a sesh. It's main advantage (to me) is that it can be used for a very light effect. As someone who gets a lot of anxiety, I'd rather use very occasionally and lightly (so almost close to placebo) so as not to become reliant.