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Benzos ⫸Benzo Guide v.1⫷

We should Etizolam; there is evidence that is more effective for long term anxiety than your traditional benzodiazepines, and it has been studied to some extent

And my new favorite benzo, dextofisopam
 
Are those not included? Or at least etizolam.

Damn, yeah no etizolam up there. It is showing up in dead people, so that ought to be in there, thanks.
 
https://www.ncbi.nlm.nih.gov/m/pubmed/8329784/

This is to demonstrate that dosage form can effect rate of absorption;

On the same page, is a link saying that the pharmacokinetic parameters were altered with daytime vs nighttime administration, which is just weird

(Temazapam Tmax 1.2-1.8 in study, can be longer though)
 
Circadian rhythms are underappreciated in pharmacology. Although that might change with recent Nobel prizes for circadian clock research.

It's really fascinating that the cells in your feet are in sync with the cells in your heart.
 
Then again, I had a buddy with a thesis chapter that went to shit. He tried his best with a new theory of genetic bias, but couldn't squeeze out a p-value for "seasonal variation" being the source of his weird results.

In lab yeast. Whose only seasons are the -80C glycerol darkness of the never-ending winter and the balmy, fluorescently-lit, spinning 30C drum summer.



OK, I'll start playing with the updates tonight.

And adding etizolam.

EDIT: Lorne, your temazepam link, isn't the different absorption rate for different doses kind of to be expected, all else being equal?

It's basically pointing out that four tiny ice cubes will melt faster than one large ice cube of equal mass, producing the same final water volume.

The FDA must have that data though. Time to enroll another clinical trial to prove the ice cube thing.

Or is this different with capsules, I guess cause they might have the same surface area?
 
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Great stuff guys, glad to see y'all chipping in with the project :D

One thing any of you can do, even if you can't edit the OP, is format any additions or alterations copypasta style, thusly:


Bromazepam
Onset of action: Peak plasma concentrations occur 0.5 - 4 hours following administration
Half-life: 10-20 hours
Bioavailability of different ROAs: 60-84% orally
Approximately equivalent oral dosage: 3-6mg
Water solubility: 0.0399 mg/mL
Good to know: Most likely metabolized by an enzyme belonging to the CYP family (possibly CYP1A2)
 
Yeah, net connection was frustrating last night and torn between this and opioid thread

Not as good with the formatting, though should be a learning

;)
 
Dude, please check out my edited-in addition of many many amusing anecdotes in the home detox thread. Eventually I'll bring it over here.


I never bad-mouthed Ativan anyway.
 
Wow, perdy stick. Don't forget my little buddy Etizolam Lorne???. Hell I might actually have to do something for OD soon.

With α1β2γ2S subunit combination, etizolam produced a 73% increase in GABA-induced currents with an EC50 of 92 nmol/l.
 
and don't forget the all important Benzo water solubilities already typed up by the Cap'n.. might need the 100ml syringe though.

http://bluelight.org/vb/threads/489494-Benzodiazepines-Solubilities-in-Water

Captain.Heroin said:
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
Click to expand...

www.Drugbank.ca might be useful

&

For contrast:
http://bluelight.org/vb/threads/266339-Bioavailability-Half-life-MEGA-Thread

&
More tables for comparison
http://onlinelibrary.wiley.com/doi/10.1111/j.1365-2125.1981.tb01833.x/pdf
 
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^ atm more concerned with lipophilliicty; have read literature on this and many subjects, as you can(hopefully) imagine, however no longer have access, to textbooks or even some e-books(on old comp)- the relative figures are accurate, though finding multiple sources is the tricky part-relative binding affinities for the big ones would be nice

May make an edited version, or at least edit the ones that call for alterations, and perhaps Scrofula or maybe my now sockless(?) friend Jekly,(or Slow Mobious, if he's done showing off his time tricks) can do it-though Scruffy seems to playing point, so may do that

Etizolam exhibits (seemingly) unique properties, like long lasting effective anxiolytic effects that are apparently resistant to tolerance in some form, and as a thienodiazepine, the common among them are interesting in having the same mechanism as benzodiazepines- acting upon their receptors (GABA-A )

Note that the metabolic listings are somewhat erroneous in a couple of cases; it would take heavy inhibitors to make any significant impact upon many benzodiazepines, like alprazolam which has a high BA% and pharmacokinetics that make inhibition difficult;

What should be pointed out is that halcion can be made probably double the potency(maybe a bit more) because it has a modest BA% (though fast absorption and elimination) and with inhibitors of even moderate strength can make it more potent, which is saying something, considering it's SDU is similar to alprazolam-and an explanation on Valium and it's Duration ad metabolism (yielding only a single meaningful metabolite, and at large l(we) doses at that) and tranxene, aka clorazepate which isn't quite what is commonly thought < different section > :)
 
Maybe he can read our modthread, JA? (I mean the part about lipophilicity, not that thing about you-know-who.) Lorne, if you want to check Cap'n's links, be my guest, please to make leisure with (guest assumes full liability).

Thanks for the link JA. It is, once sealed with the L???SofA, kind of dumb to leave it out of any final draft now. Just to explain where my thinking was (it was with shadow people), the Cap'n pretty much explains you shouldn't shoot benzos . . . dissolved in water (APAP in cold water is better, sometimes). With needle gauge issues already, why should a benzo shooter add math to his problems, when he can use PG? So rather than hunt the numbers for all of them, like in some kind of table, I'd considered not bothering with them, at least right away.

Once together, though, they shan't be discarded.
 
^ I Sa?d maybe you would consider, colonel(you brought up the private)

I dont know what CH has to do with it, was talking about lipophillicity, and, you know, eventual improvement to other things, absent or half- right or wrong(glass full or empty, or what not) just saying lipophillicity is useful, yes we have a table of water affinities for drugs that aren?t water soluble-like having a list of gifts you haven?t gotten, may as well have it-Seriously though

Even said you were the point man!

You?re a meanie!!!

(Sobs into shaky hands)

Jekly has mentioned lipophillicity figures before, and he needs socks- your s cold man, Scrofula-gonna cut myself now
 
May make an edited version, or at least edit the ones that call for alterations, and perhaps Scrofula or maybe my now sockless(?) friend Jekly,(or Slow Mobious, if he's done showing off his time tricks) can do it-though Scruffy seems to playing point, so may do that
Click to expand...

An edited version OF WHAT???11! then?

I was running at less than sub-capacity at the time. Now too, just more "energetically."

Thought you meant JA's solubility link from the Cap'n.

It was all because I used it as an example of a data field that I felt might be less useful than, say, lipophilicity, which is currently not mentioned in the MegaTable. I actually thought Volume of Distribution was a nice round number that implies lipophilicity as well as duration of effect, at least relative to half-life (something of a point of yours, I believe); the large number for alprazolam explains why a drug that persists for days only lasts four hours.

I'm only looking out for My Valentine.
 
^ Just a few couple sections, a couple of the listed benzos w/ figures added; mine was gonna be protein binding, though D, that is excellent Scrofula!

Have mentioned that before, when talking about dzp, actually; why never have really applied it (or attempted to, you know what I mean) makes me feel stupid-now your a meanie again! Guess that is why I can't speak openly about your "mod thread" (cuts himself more)

No no already knew about Cap H's water solubility thread, and was gonna suggest it if no one else did; just wasn't in a hurry, cause ones like, midazolam(?) have good solubility at low PH, though couldn't really be injected-idk, don't want to really encourage people to inject them anyway, although PG and similar solvents are available if someone insists they just gotta get that extra 10%; 90%, insulting -

Man remember am level-headed(most of the time, otherwise cloudy headed and not even in a good way) and want what's best-and know my place(except after a tonic clonic, no idea wtf I' am at or how ended up there)so try to keep that in mind before you know, being, mean. Not jk about that part Scrofula-be funny! Though if anyone knows about not being on full capacity, we'll even this tanuki suit is wearing
 
I've been post-ictal before. Surprisingly pleasant, I thought. Realizing I was in an ambulance in Fresno eventually--I suppose in comparison everything is pleasant.

I still don't know for sure what happened, so I'll go back to . . . sleeping. Somehow, off in my own clouds, the reported post signal sucked me back down to the forum at 3am. The HR batman, goddammit.
 
^ It's a tough job
seriously, VD (no not that kind, distribution) or protein binding

also clonazepam is a primary 3A substrate - post ictal you do feel surprisingly numb at first, though when the confusion wears off have gotten really sore - will try not to trip HR bat signal(cool mascot, though)
 
https://www.ncbi.nlm.nih.gov/m/pubmed/6137021/

This, among other studies, illustrates that the sketchy BA%of triazolam can be increased, likely significantly with basic inhibitors, and it should be mentioned

https://www.ncbi.nlm.nih.gov/m/pubmed/22320086/


https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3684331/

^ The above link provides some decent detail, and effectively confirms my previous lipophillicity listings, which would like to be placed in the sticky

Nite that midazolam, and of course, Valium are the most lipophillic, clonazepam being the least among the common benzodiazepines- lorazepam has low lipohillicity, along with oxazepam; alprazolam’s is fairly high, reported as twice as lipophhillic as clonazepam; triazolam also high lipophillicity. Ones like Temazepam and, possibly Nordazepam fall in the middle

The above link is also quoted as stating that t1/2 does NOT determine recovery from benzodiazepine effects; rather that it is simply a rate of elimination of the substrate from plasma

And bzds typically are biphasic-the primary distribution phase which mostly determines onset and duration, and a longer elimination phase, where the mostly bound(protien) and redistributed benzodiazepine is more Grady eliminated, while otherwise having little effect, except w/ accumulation, especially in larger doses

Will find a couple of more to back this up, then do the “copy pasta” thing CFC referred to, hopefully with mod approval

That is likelywyiu, Scrofula/ harm reduction batman
Interesting literature, anyway that’s that atm

-Lorne/a tanuki frog
 
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