Benzos Clonazepam: Debunking Low Intranasal Bioavailability (aka "snorted")

[Valentine4]

Hey all. I haven't posted in a while, but I happened to be doing some research on clonazepam and it's bioavailability intranasally. Before I begin - here is the chart, from the study I reference below, illustrating my points (you'll see the diagram again late in this post):



After checking the journals and studies, I came back to Bluelight and realized that everyone was saying that when you "snort" Clonazepam, that it is ineffective.

The primiere study on this exact subject* found directly contradict the notion that intranasal administration is ineffectual/wasteful. Quite the contrary, the study found that Intranasal administration is a comparable Route of Administration (ROA) to Buccal - and actually superior in achieving higher plasma levels faster. The plasma level testing shows that Intransal administration provides higher plasma concentrations sooner than Buccal.

However, the study ultimately concluded that (since the levels were still similiar), that the time and effort it would take to develop a Intranasal preparation would not be worth the effort - as the studies purpose was to see if Intransal was a viable alternative ROA to Intravenous (IV) administration. Fhey weren't looking for something to replace buccal or oral administration.

So, clinically, the higher Intranasal-resultant plasma concentrations may not be worth it versus existing buccal preparations...

. ..But but if you want it for recreational purposes, it seems Intranasal is very viable and, from the data, the preferable ROA for recreational use (if you are not administering it IV - please don't)


The sole stidy I could locate, that compares the Bioavailability of Intranasal vs Buccal Clonazepam, indicates near identically net-bioavailability over time - but it clearly shows the Plasma levels are higher sooner when Clonazepam's ROA is Intranasal, vs when it's ROA is Buccal.




*Study:

Absorption of clonazepam after intranasal and buccal administration.

M W Schols-Hendriks, J J Lohman, R Janknegt, J J Korten, F W Merkus, and P M Hooymans


Abstract

Serum concentrations of clonazepam after intranasal, buccal and intravenous administration were compared in a cross-over study in seven healthy male volunteers. Each subject received a 1.0 mg dose of clonazepam intranasally and buccally and 0.5 mg intravenously. A Cmax of 6.3 +/- 1.0 ng ml-1 (mean; +/- s.d.) was measured 17.5 min (median) (range 15-20 min) after intranasal administration. A second peak (4.6 +/- 1.3 ng ml-1) caused by oral absorption was seen after 1.7 h (range 0.7-3.0 h). After buccal administration a Cmax of 6.0 +/- 3.0 ng ml-1 was measured after 50 min (range 30-90 min) with a second peak of 6.5 +/- 2.5 ng ml-1 after 3.0 h (range 2.0-4.0 h). Two minutes after i.v. injection of 0.5 mg clonazepam the serum concentration was 27 +/- 18 ng ml-1. It is concluded that intranasal clonazepam is an alternative to buccal administration. However, the Cmax of clonazepam after intranasal administration is not high enough to recommend the intranasal route as an alternative to intravenous injection.

 

[Valentine4]

Note: I use the term "Plasma" when referring to the study's measure of clonazepam concentrations in the body, while the study uses the term "Serum". There is a technical distinction between the two, but for the purposes of data-analysis, the difference is irrelevant to the conclusions reached. I just thought I would clarify that I should actually be using the word "serum", not "plasma" - but also, that this misnomer doesn't effect the validity of my conclusion.

 

[Jen X]

The thing with snorting it is you lose some.

 

[DeathIndustrial88]

Clonazepam & other benzos do work intransally, regardless of what anyone says. It's just not the best way to go about it for a host of reasons.

If they'll work sublingually (which they do), then they'll work intransally. The mucus membranes in your mouth are very similar to the mucus membranes in your nose, so why wouldn't it?

I however don't recommend it though because years & years ago, snorting a clonazepam actually gave me a nose bleed. So unless you're working with pure product, you never know what else is in the inactive ingredients in your pill that could be bad for your nose. Some drugs even use talc & if talc gets in your lungs after snorting, you're going to have serious problems after continuous use.

I once used klonopin intravenously (out of sheer stupidity, I was in my late 20's and wanted to "inject something" for the "fun" of it). But I however didn't notice any effects at all from it. Nothing, not even a hint of relaxation. Although google claims IV clonazepam is an actual thing used in hospitals. So I have no idea why it didn't work for me. Maybe because clonazepam isn't very water soluble. Or maybe it's lipophilic & would need to be dissolved in a fat or some kind of other liquid first. So maybe in a hospital setting, their IV clonazepam is mixed with something that will get it to work. I'd have to read up on that. Anyone else more knowledgeable should fill me. My mom got IV ativan in the hospital too during chemo.

Over all I think benzos should just be taken orally though. Or if you absolutely cannot wait 2 hours for your meds to kick in, sublingual works just as good & kicks in much faster. Save your nose for better drugs.

 

[Cuncefuct]

Clonazepam & other benzos do work intransally, regardless of what anyone says. It's just not the best way to go about it for a host of reasons.

If they'll work sublingually (which they do), then they'll work intransally. The mucus membranes in your mouth are very similar to the mucus membranes in your nose, so why wouldn't it?

I however don't recommend it though because years & years ago, snorting a clonazepam actually gave me a nose bleed. So unless you're working with pure product, you never know what else is in the inactive ingredients in your pill that could be bad for your nose. Some drugs even use talc & if talc gets in your lungs after snorting, you're going to have serious problems after continuous use.

I once used klonopin intravenously (out of sheer stupidity, I was in my late 20's and wanted to "inject something" for the "fun" of it). But I however didn't notice any effects at all from it. Nothing, not even a hint of relaxation. Although google claims IV clonazepam is an actual thing used in hospitals. So I have no idea why it didn't work for me. Maybe because clonazepam isn't very water soluble. Or maybe it's lipophilic & would need to be dissolved in a fat or some kind of other liquid first. So maybe in a hospital setting, their IV clonazepam is mixed with something that will get it to work. I'd have to read up on that. Anyone else more knowledgeable should fill me. My mom got IV ativan in the hospital too during chemo.

Over all I think benzos should just be taken orally though. Or if you absolutely cannot wait 2 hours for your meds to kick in, sublingual works just as good & kicks in much faster. Save your nose for better drugs.

I've always wondered. And I have worried that I have wasted good klonopin pills from this. But is it only the wafers that you can take sublingual or buccally or is it the plain pill form too?

 

[Halif2]

I rubbed some clonazepam into my eyeball once. Unfortunately, I couldn't tell you whether it worked or not because I was so out of it on several different substances that it was all just a blur. Strange times.

 

[DeathIndustrial88]

I've always wondered. And I have worried that I have wasted good klonopin pills from this. But is it only the wafers that you can take sublingual or buccally or is it the plain pill form too?

The pills work sublingually just fine too.

Honestly, I have no idea why they make "sublingual" formulas for klonopin, other than to add more unnecessary inactive ingredients (like a sweetener) when the pills dissolve really fast & taste just fine. In fact they have a sort of slightly numbing mint feel to them.

 

[paltatomate]

Although google claims IV clonazepam is an actual thing used in hospitals.

iv lorazepam is what they use in hospitals, at least they do here (very nice!)

My mom got IV ativan in the hospital too during chemo.

that would be lorazepam

now regarding snorting, i wondered myself once, though never for practical reasons (meaning to actually do it, i don't like snorting stuff)
what i do with my cheap generic clonaz is to dissolve them in the mouth, and the taste alone already gives me a little clona feeling. they never take hours to kick in, maybe 10-15 minutes.
but i might not be a clona poster child because compared to what i read here, i react to it a bit differently than most.

 

[GulpingBatteryLiquid]

I rubbed some clonazepam into my eyeball once. Unfortunately, I couldn't tell you whether it worked or not because I was so out of it on several different substances that it was all just a blur. Strange times.

Despite what Kevin and Perry told you, I don't think eyeballing really works

Probably not good for the old eyes either

 

[4DQSAR]

Is the OP aware that serum concentrations are not accurate measures of concentrations within the brain? Especially if a compound is lipophilic (fat loving). The LogP of clonazepam is around 2.4 i.e. most of it will sit in fat.

Note that the IV was 0.5mg/kg while nasel and buccel are 1mg/kg.

So it appears that clonazepam is being dissolved in fat tissue but IV will ensure that the first fatty tissue the medicine encounters is the brain. The fact that eventually the plasma levels end up the same may well be a function of higher bioavailability.

But IV benzodiazepines have got a VERY bad name. People doing all manner of craazy things. I assume this is why IV benzos are only used by hospitals.

FYI there MAY be a way to dissolve clonazepam in something like propylene glycol (non-toxic) and employ a parentheral ROA.

 

[Vastness]

Interesting.... is this also likely to be true for other benzos, then?

The problem with buccal absorption vs intranasal for most stuff that isn't specifically prepared to be absorbed "bucally" is surely saliva buildup, which seems to be an autonomic response to holding any foreign object in the mouth, but with substances dilutes and interferes with absorption, effectively making a good portion of whatever substance an oral dose, eventually. Anyone who has tried putting a bunch of a typically snorted drug (cocaine, ketamine) under the tongue for whatever reason (acute intolerance to any more insufflation of dry powder, usually, I'd think) can surely attest to the fact that it just doesn't hit the same. And I'm guessing this has got to be the reason. Obviously mucus production in the nose has the same effect after a while but since evolutionarily the nose didn't evolve to have stuff jammed up it the effect is much less pronounced, making snorting generally more effective.

I mean if this wasn't the case surely there'd be a lot less snorting of drugs that are generally snorted when the mouth is so much more resistant to cumulative damage than the nose is.

 

[4DQSAR]

Well, there are some RC nitrobenzodiazepines which reports suggest retain the higher toxicity than equally potent RCs that are not nitrobenzodiazepines.

Here is an odd thing. Flunitrazepam is considered around five times more potent that nitrazepam BUT flunitrazepam is five times more toxic than nitrazepam. It seems like there exists a relationship between toxicity and potency.

I do not know why.

but there is a quite clear ratio beween the active and toxic dose.

So who knows just how toxic things like flunitrazolam are. My bet is that the increased potency will increase toxicity.

I was a bit surprised that RC vendors didn't go on to produce even more potent homologues. There are a few examples that are several times more potent than flunitrazolam and which as far as I could find out, were much less toxic. But these are all chiral, or rather they have two isomers and one is more potent than the other. But I think the racemate would be accepted by the market. After all, some genius thought flunitraolam was a GREAT idea.

 

[Halif2]

Probably not good for the old eyes either

Certainly not good for the ol' peepers, but neither is gulping battery liquid.

The things we do, eh?