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Benzos ⫸Benzo Guide v.1⫷

Scrofula

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KLEINERkIFFER'S BRILLIANTLY UNBOWLDERIZED BENZODIAZEPINE BALLAD
THE BENZODIAZEPINE INFODATADOSEMEGATABLE




Disclaimer:Nobody here is licensed to even drive, do not use this as medicaladvice




What are benzos?
Benzodiazepines are a class ofgabaminergic psychoactive drugs whose core chemical structure is thefusion of a benzene ring and a diazepine ring. The first such drug,chlordiazepoxide (Librium), was discovered accidentally by LeoSternbach in 1955, and made available in 1960 by Hoffmann?€“LaRoche
They are used to treat insomnia (onlyshort term, as tolerance to the hypnotic properties of benzos buildsrapidly), anxiety, seizures, muscle spasm and alcohol withdrawal.


How do they work?
Benzos are positive allostericmodulators of the GABA-A receptor. Unlike other positive allostericmodulators that increase ligand binding, benzodiazepine binding actsas a positive allosteric modulator by increasing the total conductionof chloride ions across the neuronal cell membrane when GABA isalready bound to its receptor. So they work by increasing theefficiency of a natural brain chemical, GABA, to decrease theexcitability of neurons. This reduces the communication betweenneurons and, therefore, has a calming effect on many of the functionsof the brain.
The GABA-A receptor consist ofdifferent subtypes, the predominant subtypes in the brain being thosethat contain alpha1-, alpha2-, alpha3-, and alpha5-subunits. Studiesshow, that ?2,3GABA-A receptors are important for mediating theanxiolytic effects of benzodiazepines, while motor effects mightinvolve action primarily at ?1GABA-A receptors. The alpha1-containing???2 receptors seem to mediate sedative, anterograde amnesic, andantimyoclonic actions. Muscle relaxant activity of BZDs is mediatedpartially by alpha1-, alpha2-, alpha3-, and alpha5-containing ???2receptors.
Hypnotic effects by alpha1 subreceptorsites, anxiolytic, and muscle relaxant effects via alpha2 and alpha3subsites, anticonvulsant properties via alpha5 subsite
So different benzos have differentaffinities for the subtypes making every benzo unique in it?€™seffects.


Dangerous combinations
Benzodiazepines are CNS depressants andthus can increase the action of other CNS depressants and canincrease sedation, provoke a black out, impaired motor coordination,suppressed breathing and other adverse effects that can be lethal.
If you don?€™t have a extremelyhigh tolerance to both CNS depressants don?€™t combine ?€˜em,it?€™s not worth the risk.
Even a normal dose of a benzo and a fewbeer can result in a black out.
If you insist on doing it, have someonearound to have an eye on you!


Withdrawal
Benzodiazepine withdrawal is no jokeand can be lethal in the worth case, as GABA is the most importantinhibiting neurotransmitter and going of cold turkey can result inseizures and has the potential to kill you. A taper is advised, lookup the Ashton manual, it?€™s the golden standard for a benzotaper.


Approximately Equivalent Oral dosagemeans equivalent to 10mg diazepam


Alprazolam
Onset of action: Peak concentrations inthe plasma occur in 1 to 2 hours following administration (slightly longer sublingual)
Onset: 15-30 min
Half life: IR around 12 hours (6-12 h),ER 10-16 hours
Duration of action: For immediaterelease round 4-5 hours ?
Bioavailability of different ROAs:80-90 % orally
Approximately Equivalent Oral dosage:0.5 ?€“ 1mg
Water solubility: 0.04 mg/ml
Good to know: Metabolism by CYP3A4 ->using WGJ (contains bergamottin) will inhibit the metabolism ->longer duration




Bromazepam
Onset of action: Peak concentrations inthe plasma occur in 0.5 - 4 hours following administration
Half life: 10-20 hours
Duration of action:
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 byan enzyme belonging to the CYP family, could be CYP1A2




Chlordiazepoxide
Onset of action: 15-30min
Half life: 5-30 hours; metabolitearound 36-200 hours
Duration of action:
Bioavailability of different ROAs:
Approximately Equivalent Oral dosage:25mg
Water solubility: 2 mg/mL
Good to know:




Clonazepam
Onset of action: 0.5 ?€“ 1 hours
Half life: 18-50 hours (mean 30-40)
Duration of action: 6-12 hours
Bioavailability of different ROAs:Around 90% orally
Approximately Equivalent Oral dosage:0.25-2mg
Water solubility: < 0.1 mg/mL
Good to know:Metabolized by CYP3A4 & N-acetyl transferase 2 ( 3A4 is more abundant in the body, and so it is the de facto enzyme for metabolism) Also, Clonazepam has serotonergic effects unique to benzodiazepines




Chlorazepate
Onset of action: intermediate acting, peaks within < 2 hours
Half life: 18-50 hours and up to 200hours for the main metabolite desmethyldiazepam
Duration of action: 4-12hrs
Bioavailability of different ROAs: 91%orally
Approximately Equivalent Oral dosage:15mg
Water solubility:0.0248 mg/mL
Good to know:prodrug for Nordazepam
Note: Clorazepate is COMPLETELY converted to Nordazepam prior reaching the liver; so, the two drugs are effectively identical, so taking 10mg Chlorazepate (Tranxene) is basically like taking 9 or 10 mg pure nordazepam PO
Brand name Tranxene, and commonly used to taper in gabaergic wd




Diazepam
Onset of action: Within 15 min (Peaks 1-2hrs)
Half life: 20-100 hours and up to 200hours for the main metabolite desmethyldiazepam
Duration of action: 1-6 hours
Bioavailability of different ROAs:93-100% orally; 90% rectal
Approximately Equivalent Oral dosage:10mg
Water solubility: 0.05 mg/mL
Good to know:Metabolized by variousCYPs




Flunitrazepam
Onset of action: 15-30 min
Half life: 18-26 h
Duration of action: 4-8 h
Bioavailability of different ROAs:64?€“77% oral, 50% suppository
Approximately Equivalent Oral dosage: 1mg
Water solubility: 0.00858 mg/ml, 166mg/L, 0.0086 g/L
Good to know:




Flurazolam
Onset of action:
Half life: 18-26 h
Duration of action:
Bioavailability of different ROAs:64-77% orally
Approximately Equivalent Oral dosage:1mg or less
Water solubility:
Good to know: Metabolized mainly viaCYP3A4




Loprazolam
Onset of action: 2 h for peak serumconcentration, but might induce sleep within 30 min
Half life: 6-12 h
Duration of action:
Bioavailability of different ROAs:
Approximately Equivalent Oral dosage:1-2 mg
Water solubility: 10mg/ml
Good to know: 50 % is metabolized intoactive metabolite (half life and potency equivalent to loprazolam)rest is excreted unchanged




Lorazepam
Onset of action: 15-30min / delayed onset, peak 2-3 hours
Half life: 10-20 h
Duration of action: 6-12 h
Bioavailability of different ROAs:85-99% orally; up to 94% sublingually
Approximately Equivalent Oral dosage:1mg
Water solubility:0.08 mg/mL
Good to know:




Midazolam
Onset of action: 15-30 min
Half life: 1.5 ?€“ 4 h
Duration of action: 1-6 h
Bioavailability of different ROAs:31-72% orally
Approximately Equivalent Oral dosage:2-6mg
Water solubility:0.024 mg/mL
Good to know:




Nitrazepam
Onset of action: peak plasmaconcentration in around 2 h
Half life: 15-38 h
Duration of action:
Bioavailability of different ROAs:53-94% oral
Approximately Equivalent Oral dosage:10 mg
Water solubility: 0.0299 mg/mL, 0.03g/L
Good to know: 10 mg seems to be a highdose




Nordazepam
Onset of action:
Half life:
Duration of action:
Bioavailability of different ROAs:
Approximately Equivalent Oral dosage:
Water solubility:57 mg/L
Good to know:




Oxazepam
Onset of action: 30-120 min
Half life: 4-21 h
Duration of action:
Bioavailability of different ROAs:95-96% orally
Approximately Equivalent Oral dosage:20-30mg
Water solubility: 0.179 mg/ml
Good to know: Can suppress cortisollevels [https://www.ncbi.nlm.nih.gov/pubmed/1349754],
Metabolized by glucuronidation




Temazepam
Onset of action: 30-60min
Half life: 8-22 h
Duration of action:
Bioavailability of different ROAs: 96%orally
Approximately Equivalent Oral dosage:20mg
Water solubility:0.164 mg/mL
Good to know: No active metabolites




Triazolam
Onset of action: 15-30 min
Half life: 1-6 h
Duration of action: 1-2 hours
Bioavailability of different ROAs: 44%orally; 53% sublingually
Approximately Equivalent Oral dosage:0.5mg
Water solubility: 0.00453 mg/mL
Good to know:






Z-Drugs (group ofnonbenzodiazepine drugs with effects similar tobenzodiazepines)


Zolpidem
Onset of action: 15 min
Half life: 2-3 h
Duration of action: 3 h
Bioavailability: 70% oral
Dosage: 5-30 mg
MoA/Affinities: Zolpidem has about10-fold lower affinity for the alpha2- and alpha3- subunits than foralpha1, and no appreciable affinity for alpha5 subunit-containingreceptors.
Good to know: belongs to theimidazopyridine class, may cause sleepwalking, can causehallucinations in high doses, The Ambien Effect


Zopiclon
Onset of action: peak plasmaconcentration in 1-2 h
Half life: 3-7 h
Duration of action: 3-9 h
Dosage: 2-7.5 mg
Bioavailability: 75-80% oral
MoA/Affinities: it is regarded as beingunselective in its binding to alpha1, alpha2, alpha3, and alpha5
Good to know: belongs to thecyclopyrrolone class, In the United States, zopiclone is notcommercially available, although its active stereoisomer,eszopiclone, is sold under the name Lunesta




Zaleplon
Onset of action: full concentration inaround 1h
Half life: 1-1.5 h
Duration of action: 1h
Dosage: 5-20 mg
Bioavailability: 30% oral
MoA/Affinities: selectively binds withhigh efficacy to the benzodiazepine site (omega1) on theaplha1-containing GABA-A receptors
Good to know: belongs to thepyrazolopyrimidine class, zaleplon appears to induce sleep withoutdisrupting the natural sleep architecture, may cause hallucinationsin high doses






Antagonist:


Flumazenil

Flumazenil competitively inhibits theactivity at the benzodiazepine recognition site on theGABA/benzodiazepine receptor complex. Because the body does notproduce endogenous benzodiazepines, flumazenil only createsbehavioral effects when administered concurrently with abenzodiazepine receptor agonist or inverse agonist. It can lower theseizure treshold and can cause agitation and anxiety thus should onlybe administered by a trained medical professional in a clinicalsetting
 
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Scrofula

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Gentlemen and Harlots of Bluelight:

Please to offer your peanuts and produce of admiration, and your original research to the contrary of what has been said.
 

Lorne???

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^ Have Study confirming that sublingual alprazolam has delayed onset, and possibly *slightly longer duration?

And relative lipid solubilities; need references for others

And clonazepam has 30-40% intranasal BA%, a more rapid onsets, although a 2nd peak caused by incidental oral administration

Also, have references for Tmax/peak; think this is important so people may get the idea that you cannot simply redose 30-40 minutes later, when even alprazolam takes 1.5-2hrs to peak, and Clonazepam has a tmax that varies from 1-4hrs!

Nice format again
 

Scrofula

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Yeah and I got the opioid one backward when I tried to merge your thread into it. So please, feel free to keep it at it down in the non-sticky zone
 

Slow_Mobius

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IIRC, this is the brainchild of Kleinerkiffer and maybe KittyCat? It was already an ongoing project when I was modded up.

Anyways, we're making it public so anyone can add to it. If you have any info on any of the listed drugs (or new drugs that aren't listed) please post the info. Citations are strongly encouraged. We will then add the info to the list.

Any and all contributions, discussion, etc are strongly encouraged and very appreciated :)
 

Scrofula

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Welcome to the still-sticky v1. I mentioned in the unstickied opioid thread that I'd prefer at least a decent-size update dump before editing, else I might erase the entire board.

Actually, this post is a lot smaller, it's probably safer, but still.

So Lorne, get busy.

Please to let me know contributors to the original who would like their names in the box.
 

Lorne???

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Not to fear, Scrofula, Lorne is here!

No seriously asked about this kinda thing awhile back, appreciate it. Just need a couple of days for substantial updates w/ references
(although in some cases references are not needed or as important, because the info is more basic/can be verified w/google

This or the opioids first? Dealers choice; of course nowadays it is benzodiazepines and breakfast, though things different here in the pacific/southeast

(This suit is getting worn, Tanuki may need a (brief?) break
 

Lorne???

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No, 10'000 words is the limit;

Anymore more and they smack me
 

Throwdown

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Lorne I know you obviously have a really good knowledge in this area but no lie i literally don't understand 90+% of your posts. Loads of scientific abbreviations and mad words its so confusing. I'm sure I' not the only one.

Maybe try simply the information so it's easier to read?

Just a friendly word of advice i mean no disrespect.
 

Lorne???

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^If you check my basic posts I do, however am putting this together almost stream of consciousness like, so am simply trying to put dat, and summarizing the way that is easier for me, as statistics are my thing, and half of this stuff isn't worth explaining, or at least taking the extra time when then figures are there

Appreciate it though
 

Scrofula

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Lorne . . . i literally don't understand 90+% of your posts . . .

Maybe try simply the information so it's easier to read?
In fairness, he's mostly throwing stuff out for inclusion in the table, so only nerds and mods are probably interested.

I've definitely noted the readability issue and general needs for different users, and I'm hoping to turn this into different sections based on that.

SO, at top would be the simplest: dose, duration; and after that the more biochemical stuff.

Not every drug will have some of the more technical data, and there's a niche audience to have interest in relative lipophilicities. Plus there could be contention over the nuances of duration of effect v. half-life, that can be left out of the fast data up top.

And lastly a bonus section on the immune effects.
 

Lorne???

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^ Exactly!

The basic-intermediate information people want/need shall be there, and some other stuff can be included for a smaller audience

duration of action is important, however, wish could explain that to a general audience

I really do try to give to-the-point answers to general posts, HR is still the goal line

(don't forget an ibs section, lest this be in vain)
 

Throwdown

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In fairness, he's mostly throwing stuff out for inclusion in the table, so only nerds and mods are probably interested.

I've definitely noted the readability issue and general needs for different users, and I'm hoping to turn this into different sections based on that.

SO, at top would be the simplest: dose, duration; and after that the more biochemical stuff.

Not every drug will have some of the more technical data, and there's a niche audience to have interest in relative lipophilicities. Plus there could be contention over the nuances of duration of effect v. half-life, that can be left out of the fast data up top.

And lastly a bonus section on the immune effects.

nice, sounds like you have a good plan.

Docyou know anything about this guys background yet because he seems to know some fucking crazy shit.
 

Lorne???

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^ Never! Whahaha

If your asking about me, ask; if not, pass the dossier
 
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