Etizolam : Forget everything you knew about benzos

[audacity]

I was looking over some PubMed research on etizolam, and came across some very surprising studies. Etizolam might be a safer anxiolytic than classical benzos, while still retaining high effectiveness and rapid action.

1. Patients with generalized anxiety disorder were either treated with Etizolam (0.5 mg), Alprazolam (0.5 mg), or Bromazepam (3 mg) twice a day. While all three drugs retained their effectiveness over 2 weeks, etizolam actually started to become more effective than the other benzos from to 2 weeks to 4 weeks (reverse tolerance in a way). The researchers also note antidepressant activity in etizolam not seen in the other two drugs tested.

Etizolam in the Treatment of GAD (PubMed Abstract

2. No cognitive deficits over 3 weeks compared to placebo were noticed with etizolam 0.5 mg BID, a curious finding for a BZD agonist

Effects of 0.5 mg BID Etizolam on cognitive performance (PubMed Abstract)

3. When multiple doses of etizolam or lorazepam were administered to rat neurons, lorazepam caused downregulation of alpha-1 BZD sites (aka tolerance/dependence), while etizolam caused an increase in alpha-2 BZD sites (aka reverse tolerance to anti-anxiety effect).

Also, the researchers noted a marked tolerance over time to the anticonvulsant effects of lorazepam, but no significant tolerance to anticonvulsant effects of etizolam.

Quote from abstract: "These data suggest that etizolam is endowed with a reduced liability to induce tolerance and dependence compared with classical benzodiazepines."

Etizolam: Less Tolerance/Dependence than Classical Benzos (PubMed Abstract)

[the chodesman]

Hey man sweet info I just asked a thread about Etizolam as I came into some of them. I've been researching it off and on and I plan on reading those links at a more reasonable hour.

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I already asked this but I can't seem to find info on it. Do you think a person would come up positive for benzodiazepines in a drug screen by solely taking Etizolam?

[etinin]

Midazolam seems to share at least inverse tolerance to hypnotic effects, with 15mg daily administration. Tolerance to anti-convulsive effects is still developed, though.

Efficacy without tolerance or rebound insomnia for midazolam and temazepam after use for one to three months
ScienceDirect.com - Pharmacology Biochemistry and Behavior - Comparison of anticonvulsant tolerance, crosstolerance, and benzodiazepine receptor binding following chronic treatment with diazepam or midazolam

This is rather interesting. The full mechanism remains to be explained. Maybe exposure to benzos with a very short half-life is insufficient to trigger tolerance mechanisms, while keeping the papez circuitry effectively tuned down, but not enough to drive the body to compensate and the neurons might actually "get used" to the new state.

Or maybe some specific interaction due to the -zolam skeleton? Maybe a combination of both? Alprazolam doesn't seem to lose its anxiolytic properties over time either, though dependence to other effects will develop.

My problems with etizolam are:
1. it is not available where I live and it's very boring to measure research chemicals.
2. induction of blepharospasm (a potentially permanent disorder of the eyelids)


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Hey man sweet info I just asked a thread about Etizolam as I came into some of them. I've been researching it off and on and I plan on reading those links at a more reasonable hour.

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I already asked this but I can't seem to find info on it. Do you think a person would come up positive for benzodiazepines in a drug screen by solely taking Etizolam?

According to anecdotal reports, etizolam WILL show up as a benzo.

[the chodesman]

I've never heard much about Midazolam but they give the shit to children to knock them out before surgery so it sounds pretty potent and like something I want no part of.

[etinin]

When used in the right dosage, Midazolam knocks you out just the right amount. It also doesn't seem to mess much with sleep architecture, as opposed with other benzos.
I already liked Midazolam when I started researching about it and it really seems to be good. No shitty daytime hangover like long-lasting benzos. I prefer SSRIs for my anxiety, benzos for me are night-time only.

[the chodesman]

When used in the right dosage, Lorazepam knocks you out just the right amount. It also doesn't seem to mess much with sleep architecture, as opposed with other benzos.
I already liked Midazolam when I started researching about it and it really seems to be good. No shitty daytime hangover like long-lasting benzos. I prefer SSRIs for my anxiety, benzos for me are night-time only.

Lorazepam isn't really popular in my area for some reason. It's either Klonopin or Xanax. I've got a bunch of 2.5 mg Ativans and 1mg Etizolam that aren't moving well.

I'll never take another SSRI, Celexa and Effexor made me manic as hell.

[etinin]

@the codesman
I meant Midazolam LOL
Lorazepam is highly sedating.
If you want meds for anxiety, you should try pregambalin or gabapentin. For sleep, midazolam would be a nice try.

Why isn't etizolam working? Also, ativan=lorazepam. It lasts far too long. Etizolam has a better anxiolytic potential. You can try increasing the dosage to 2mg.

[ohanes]

Thank you, I had never heard of Etizolam, and will look into it to replace Xanax in the future. Any ideas of where to order from would be appreciated. Thanks

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Apparently Midazolam has a short half-life, about 3 hours in the system, about half of what Xanax lasts. Thanks for the info.

[etinin]

Thank you, I had never heard of Etizolam, and will look into it to replace Xanax in the future. Any ideas of where to order from would be appreciated. Thanks

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Apparently Midazolam has a short half-life, about 3 hours in the system, about half of what Xanax lasts. Thanks for the info.

You can get Etizolam in many research chemical websites as a powder (requires a precision scale in order to be used safely). Unfortunately I am not aware of any safe sources to acquire etizolam tablets, but I'm sure they do exist.

Also, just a small correction: alprazolam (xanax) lasts approximately 12 hours in your system!!

[billyboy1965]

There was a thread about this a bit ago and the concern was the sexual side effects for males ~ boner problems and loss of libido. I'm not sure where the research is.

[etinin]

There was a thread about this a bit ago and the concern was the sexual side effects for males ~ boner problems and loss of libido. I'm not sure where the research is.

It really depends on the person, though. For me, nothing can significantly affect my libido and sexual potency (except for insane amounts of alcohol). And when these problems occur, they can often be treated with medications such as bupropion or sulbutiamine.

[audacity]

You can get Etizolam in many research chemical websites as a powder (requires a precision scale in order to be used safely). Unfortunately I am not aware of any safe sources to acquire etizolam tablets, but I'm sure they do exist.

Also, just a small correction: alprazolam (xanax) lasts approximately 12 hours in your system!!

Stay away from research chemical grade etizolam. You have no idea of the purity or weight. Pharmaceutical grade 1 mg etizolam tablets (brand name: Etilaam) are widely available.

[the chodesman]

Stay away from research chemical grade etizolam. You have no idea of the purity or weight. Pharmaceutical grade 1 mg etizolam tablets (brand name: Etilaam) are widely available.

Exactly what I was thinking/typing. Tee hee. Cheap too.

There was a thread about this a bit ago and the concern was the sexual side effects for males ~ boner problems and loss of libido. I'm not sure where the research is.

Anti-psychotics and SSRI's can mess up a man's boners as well. Saphris was the most horrid thing I've ever taken.

[Perromaldido]

A reverse tolerance benzo? Now isn't that something surprising....apart from those 3/4 weeks time I wonder what happens long term, isn't the maetabolite the same of Diaz after all. I'll go through the study... Obrigado pela imformaçao.

Perromaldido

[etinin]

A reverse tolerance benzo? Now isn't that something surprising....apart from those 3/4 weeks time I wonder what happens long term, isn't the maetabolite the same of Diaz after all. I'll go through the study... Obrigado pela imformaçao.

Perromaldido

de nada
I think diaz is metabolized to temazepam and oxazepam. Midazolam is mainly metabolized to some hydroxymidazolam metabolites apparently.
Some benzos are far too evil. All the nitrobenzodiazepines (clonazepam, nitrazepam, etc) can be very toxic to your liver. Alprazolam, temazepam and diazepam seem to be more benefic (each of them has a different strength).
I think the sedative potential of most benzos will be gone permanently after the initial period of 2 months after tolerance settles in, but it should then stabilize. Too bad it would be too expensive to fund a study to find that out and nobody is really interested.

I've been researching and all research seems to indicate midazolam, for example, is a very good drug. No tolerance and subjective sleep quality is reported as being good, even though it does decrease deep sleep (very funny fact, maybe because its main effects only happen in the first hours and after around 7 hours are completely gone). All the research which says tolerance does happen uses insanely high dosages which are nowhere near the ranges used in clinical settings.

Maybe it somehow makes stage 1 and 2 sleep more restful? I have some mild sleep apnea and barely enter stage 3 and 4 sleep. But midazolam has still significantly improved my subjective sleep quality.

Thing is, most of this kind of research date from when midazolam was already off-patent meaning there was no big money to be made there. Instead, they've been preferring to promote more biased studies promoting z-drugs which fare a lot worse. Even with zolpidem (ambien), which has a short half-life, there is still a hangover effect (at least for me) and rebound insomnia does happen, in contrast with midazolam, which can even cause a partial remission.

It is not all about half-life. Triazolam had the shortest half-life of all benzos yet it had a huge potential for dependence.

Too bad benzos are already very badly regarded as being evil and it's very unlikely pharmaceutical companies would invest in a new round of improved benzos. But there's always the chance they may come up with good non-benzodiazepines. Etizolam seems to be nice, but still scary in some aspects, as it could leave your vision crippled for life. IMO Z-drugs are good only when you want to trip a little before going to bed :P

[billyboy1965]

Anti-psychotics and SSRI's can mess up a man's boners as well. Saphris was the most horrid thing I've ever taken.

When my shrink was coming up with the right chemical mix for me, I refused a lot of them just because of that. It was the orgasm that was f'd up. Not all, but more than half I tried. That's pretty well documented.

[Perromaldido]

Right @itinin esp. with your review of Triazolam (Halcion). It's truly abusable and msny like to wash it down with a little booze with the obvious results. When used ''legitly'' their effect is real short. It is a good hypnotic good at putting you to sleep but if you have problems at keep sleeping a decent amount of hours then it woul leave me alone deep at night. The only time in my life I went inpatient I was so psychotic about prolonged lack of sleep they put me on 2x0,25 to put me out + 15 mgs diaz to keep on sleeping. That worked. Of course they did that for a few days then tapered me down, eventually eliminating triaz, then Val dripping, Val tabs and then no more BZD, just a minor dosage of quietapine fumarate. The process took about one month. We don't have Midazolam here, it's an iv/im hospital med only used as a preanestetic, though in the past I ordered a few times the 15 mgs Dormicum and well, 2x made me sleep as my cat on a rainy day.

Perromaldido

PS: On a totally different subjcet is Engove still OTC in BR? In that case I'll ask my ex in BH,MG to send some over...it doesn't exist here but if it did it'd be defintely OTC, i also thought it'd sell just great on weekends ;-)

[etinin]

Right @itinin esp. with your review of Triazolam (Halcion). It's truly abusable and msny like to wash it down with a little booze with the obvious results. When used ''legitly'' their effect is real short. It is a good hypnotic good at putting you to sleep but if you have problems at keep sleeping a decent amount of hours then it woul leave me alone deep at night. The only time in my life I went inpatient I was so psychotic about prolonged lack of sleep they put me on 2x0,25 to put me out + 15 mgs diaz to keep on sleeping. That worked. Of course they did that for a few days then tapered me down, eventually eliminating triaz, then Val dripping, Val tabs and then no more BZD, just a minor dosage of quietapine fumarate. The process took about one month. We don't have Midazolam here, it's an iv/im hospital med only used as a preanestetic, though in the past I ordered a few times the 15 mgs Dormicum and well, 2x made me sleep as my cat on a rainy day.

Perromaldido

PS: On a totally different subjcet is Engove still OTC in BR? In that case I'll ask my ex in BH,MG to send some over...it doesn't exist here but if it did it'd be defintely OTC, i also thought it'd sell just great on weekends ;-)

I mean, triazolam is physically addictive in clinical dosages and midazolam isn't, which is a little surprising. All benzos are abusable. And too bad mida it's hospital only where you live.

Yup, still OTC. Pretty much anything is OTC here, except for psychotropics and anabolic steroids
(officially most stuff require a prescription but, except for the meds which require pharmacies to retain the scripts, the rules are mostly ignored)

I don't particularly like Engov. My friend and I took it once before we started drinking and the result was a pretty crappy alcohol bad trip. My tip for hangovers is vitamin C+600mg acetylcysteine :P

[Perromaldido]

Merda, tudas as vezes que foi no Brasil tinha so que trablhar sem visitar nem uma farmacia...
;-) Gosto do engove, ajuda demais pra mim. Sorry guys but I like Portuguese an Spanish A LOT, I'll now stick to PR's official language , promised....

Perromaldido

[etinin]

By the way, if anyone is looking into getting rich in the pharmaceutical business, I have designed the new perfect intermediate acting benzodiazepine :P
It's like alprazolam but based on a midazolam skeleton instead of triazolam.
It would have a half-life of approximately 12 hours and reduced dependance liability, as compared with alprazolam, while probably remaining a good ansiolytic.

I call it alezolam (my first name is Alexandre :P), since I have not found any reference to it in the literature.

8-chloro-6-phenyl-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine

I lack the knowledge to truly estimate its water solubility. If not water soluble, the compound may be better if the chlorine atom is replaced with a fluorine, in order to make it more polar and, thus, water soluble.

Merda, tudas as vezes que foi no Brasil tinha so que trablhar sem visitar nem uma farmacia...
;-) Gosto do engove, ajuda demais pra mim. Sorry guys but I like Portuguese an Spanish A LOT, I'll now stick to PR's official language , promised....

Perromaldido

muito azar =\
me divirto muito :P