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Benzos What dose for using Benzodiazepine's sublingually?

Forever Changes

Forever Changes

Bluelighter
Joined
Dec 10, 2017
Messages
1,772
compared to swallowing them?

Say I normally take 5mg Lorazepam, what would an equivalent strength dose be for under the tongue?
 
Well, see now that's a pretty tricky thing--you got to think about bioavailability, and what you're taking it for, AUC curves, pKa and log P, gastric transit times and nasty gingivitis--but in the end the manufacturers have to design these things so that they're basically identical to the standard down-the-gullet-form.

So 5mg lorazepam is equivalent to 5mg lorazepam, or at least a 5mg oral dose of intended-for-oral-use tablets is equivalent to 5mg sublingual of the sublingual form of the drug.

I'm not making fun of you, at least not much, because I'll bet there's some difference if you try to sublingual a standard tablet. I wouldn't be surprised if they didn't add a whole lot of DMSO to the sublingual to help get it across your membranes.
 
I thought it might hit faster but yeah I get that it's the same dosage in the end. The pills I have are not designed for sublingual use
 
I honestly found a pubmed link comparing routes, with an optimized sublingual. The BA's were all mid 90's, and I think even the time-to-peak wasn't substantially different.

It's not open access, but here's an abridged abstract, translated into Table form:


2mg lorazepam, n=12, single doseCmax (hr)T1/2 abs (min)Abs. BA
IV(quick)NA100%
IM1.1514.295.9%
Oral tablets2.3732.599.8%
Oral tablet, sublingualed2.3528.594.1%
Special Optimized SL forumulation2.2528.798.2%


Basically, no difference via face hole.
 
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Snorting benzos does nothing apparently so dont see how sublingual would be different?
 
Oh, but they're not so bad that way either (up your nose). You just don't really gain anything.

Link to abstract. Lorazepam intranasal BA at 77%.

It's IV that's the bad ROA for benzos, mainly just because of their shit water solubility.
 
With most benzodiazepines, SL results in a delayed onset, and slightly longer duration- so rarely worth it

Stick to oral, with a few exceptions
 
Forever Changes said:
I thought it might hit faster but yeah I get that it's the same dosage in the end. The pills I have are not designed for sublingual use
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Same dose, I can break them down into a power first(which I don't), chew them(which i do but they can get in your teeth), or let them slowly dissolve, and if it takes two long them to break down, a little sip of carbonated soda aids in the process.


I just been popping them lately, but wanted to redose as I did my codeine, and was surprised as to how quick they came on.

I used to always do it, but I'm not a fiend and I got all the time in the world.

Xanax taste like shit, comes on quick as fuck, not really worth the hassle, Valium and Kpins are easier to work with.
 
The smaller you can break the pill up, the better. It absorbs faster. I used to crack a 1 mg clonazepam into .5, and then break that into halves, and it would absorb within minutes. When I tried to just take the whole pills sublingually, it would take much longer to dissolve.
 
Yeah, my last post was early am before work and many toos awake also. It's the mere facts for lorazepam specifically, it won't translate perfectly across that enormous class of drugs.

yteek said:
I just been popping them lately, but wanted to redose as I did my codeine
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This translates to trouble. Please do not "pop" benzos; or yes, do "pop" in the sense of swallowing tablets as Jesus intended, do not "pop" them as you would popcorn, ie., take a whole bottle before the previews are over.

Do not take with opioids, or booze, or other downers. Keep in mind most benzos last a whole lot longer than most opioids. You may be one of the lucky many like me who will feel nothing before a sudden ambulatory amnestic event. Don't keep redosing benzos if you don't feel anything. You will just black out and/or die, and in neither scenario do you feel anything.
 
mp44god said:
The smaller you can break the pill up, the better. It absorbs faster. I used to crack a 1 mg clonazepam into .5, and then break that into halves, and it would absorb within minutes. When I tried to just take the whole pills sublingually, it would take much longer to dissolve.
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do you find the effects came on faster or stronger?
 
Most of the benzos I've had were designed for sublingual use. I find they work about the same way if I swallow them or let them melt in my mouth. The only noticeable difference to me was, as you said, sublingual hit faster.
 
Scrofula said:
Yeah, my last post was early am before work and many toos awake also. It's the mere facts for lorazepam specifically, it won't translate perfectly across that enormous class of drugs.



This translates to trouble. Please do not "pop" benzos; or yes, do "pop" in the sense of swallowing tablets as Jesus intended, do not "pop" them as you would popcorn, ie., take a whole bottle before the previews are over.

Do not take with opioids, or booze, or other downers. Keep in mind most benzos last a whole lot longer than most opioids. You may be one of the lucky many like me who will feel nothing before a sudden ambulatory amnestic event. Don't keep redosing benzos if you don't feel anything. You will just black out and/or die, and in neither scenario do you feel anything.
Click to expand...

That is why I said I as it is not intended for advice. Not that the practice of physicians are the saving grace of reasoning, but there is much more epic combos dished out in comparison to a little codeine and clonazepam. Classic combos of pain managements often consisting of cocktails of much stronger opioids, benzos, somas, and even ambien.

Addictive and of course there is an apparent/present danger in those cases, but despite being one of the rules of harm reduction, oddly one of the go to's in medical practice. Keep in mind, the last thing I would do is rationalize these practices on the merit of the very faulted protocols of prescribing, just an oddity where medical doctrine and harm reduction often rely on the same science behind the reasoning of responsible use, this being an outlier.
 
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Definitely came on faster, within minutes, but it felt about the same as taking them on an empty stomach.
 
AGAIN- sublingual often results in a delayed onset- example Xanax - Tmax =1.5-2hrs PO, vs ~2.5hrs sublingual, they are equivalent, technically, yet SL would result in slightly lower (yet more sustained) plasma peaks

Sublingual is more like rectal than intranasal- seriously they co-relate, sometimes in multiple ways, while there is pretty much no co-relation between intranasal and sublingual- sublingual involves drugs being absorbed into membranes under your tongue, and then eventually at a variable rate, it ends up reaching systemic circulation- just check out buprenorphine SL, as an example- it is often faster than rectal though not always by any means

With Benzodiazepines, just take them by mouth, with few exceptions

And remember, they're is a benzo sticky that covers all of this and more- I could add extra ROA's for the common benzodiazepines if people would use the info-and even point out which benzodiazepines have lower BA% PO, and can be taken by other routes-like Halcion, if you like a fast acting, powerful hypnotic benzo that leaves you asleep or otherwise wears off quite rapidly- and the longest lasting benzodiazepines, and Chronic vs Acute adminstration of said benzodiazepines, that are either long acting or otherwise produce long acting metabolites or, has a slow elimination (and a medium-long acting metabolite, despite the parent drug being a fast acting benzodiazepine, with at best an intermediate duration...)

Anyway, check it out people,and it would answer many of your questions off the bat, and provide stats and info, and many studies and links through the posts with interesting info, that caters to different types:)
 
Speak for yourself. I've taken kpins sublingually many times, and the onset is significantly faster than dosing orally. Otherwise, there would be no point in doing it.
 
Yeah, Lorne listed the Tmax for the two, but that's the time it takes to reach the highest concentration, not the time to onset. I'm not doubting it may be true for some benzos, but its hard to imagine how it could be slower. Even if it doesn't absorb at all buccally, eventually you just swallow it.
 
Why would ativan and xanax be designed for sublingual use if there was not a faster onset? Its certainly not for the delicious taste.
 
they could put a little artificial cherry flavor in the official SL ones, IDK. SL makes me think intended for panic attacks, exactly for faster effects.

I can say that "orally disintegrating tablets" which are not meant to absorb sublingual, so only kind of relevant, are meant for "non-compliant" people. You know, "Behavioral Center" patients.
 
Yes, "odt's are not sublingual; and for non com compliant patients, they can quickly disoolve on top of the tongue, for easy swallowing

I said slower sometimes, other times, there is no advantage; diazepam is already a rapid acting drug, it won't get much faster

And can be slower because as you pointed out, some of these neat chemical additions also alter solubilities-although most are poorly or even practically insoluble in water, and with decent lipophillicity, there are differences; drugs like Clonazepam and lorazepam are to poorly soluble for a "fast" onset; buccal improves it, (for clonazepam at least) however, the BA% is to low to be practical, and there is, AFAIK, a 2nd Tmax/ peak co-re relating with P.o, now don't quote me on the 2nd 2 factors, would have to double check, though alll of the above is true wife intranasal, which is rapid, though you are talking 3-4#% BA, and a second TMAX within 4 hours, from the nasal drip and subsequent oral administration, so that's a no-go

Alprazolam has improved water solubility, apperantly (still too low to snort or inject by far) however it still has only moderate lipid solubility; that it is why it can be slower :)

And Scrofula, check out opioid Sublingual administration, and you'll get it; I guarantee that certain amphetamines gain a delayed onset from sublingual, and rectal(meth notwithstanding)

Onset and Tmax are different, though if Tmax is delayed, so will onset; if Ax is roughly the same, onset should be similiar, although it could certainly improve-it's just important to know that, even with xanax, if you feel great within 40 minutes, wait a bit, it still hasn't peaked! That's especially true with the RC's, like Clonazolam, which can have you great 20-30 minutes later, yet then when it peaks (within 2 hours, precise time is difficult to determine) then your kinda buzZed, and if you redosed-ah man

Anyway, I could post some general reasearch, though check it out for yourself; it's like rectal with opioids, which is really hit and miss, and even with good BA', oxy(codons and morphone) have a delayed onset and reduced plasma levels, yet a longer duration of analgesia and other fun effects, and BA% is similar to P.O. To conclude, most benzodiazepines, by mouth is pretty much the way to go, the most popular have good(sometimes fairly rapid absorption) decent (or better) onset, high BA%; sublingual has a place and feel free to experiment, just telling you facts and pointing out some things /for some reason spell check popped up nihilist? No N's?
 
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