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  • BDD Moderators: Keif’ Richards

benzo question (sublingual)

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phsycra

Bluelighter
Joined
Feb 26, 2012
Messages
127
Hi

If u hold Xanax / Valium under your tongue does it have a quicker on set?

Thanks
 
Yes. Sublingual administration kicks in faster as the drug reaches the bloodstream quicker than oral.
 
This can reduce the peak plasma concentration, not to a great extent however.
 
Howso? I would have thought you'd get a sharper spike in plasma concentration, albeit with subsequent increased clearance..
 
I could be wrong, but I read that peak plasma concentration is reached much quicker but the ph in the mouth can have negative effects on benzodiazapines bioavailability. This may not be true with all benzos, the one it was referring to was clonazepam in which peak plasma levels were usually reached in 1 and 1/2 hours orally and within 40 minutes sublingualy. The peak plasma concentration Was on average 5% higher with patients who ingested it versus sublingual.

Klonopin is not the best benzo for studying these kinds of results. As it is clonazepam varies in effect more than any other benzo. Peak plasma concentration can be reached within an hour for some and take up to 8 hours for others. So I'm not sure you can really take the 5% as much evidence to wether or not the potency will be increased or decreased in that regard.
 
^ you may well be right, it isn't something I have looked into really.. interesting! Shall have to do some research, can you remember where you read that?
 
I read it in some medical journal in my libraries archive but I'm not entirely sure what it was or where to find it. Im there most days studying for school, I will go back and look for it. I would think I'll be able to find it without too much trouble.

I'll paste the text when I do.
 
That is interesting. Stomach pH is much lower than that of the mouth. I'd think any drug adversely affected by the lower pH of saliva would be absolutely killed the the stomachs hydrochloric acid stores.
 
SPC123 said:
That is interesting. Stomach pH is much lower than that of the mouth. I'd think any drug adversely affected by the lower pH of saliva would be absolutely killed the the stomachs hydrochloric acid stores.
Click to expand...

That's where I just don't know enough about it. I would assume from what I read that a lower PH is optimal for bioavailability
 
phsycra said:
Hi

If u hold Xanax / Valium under your tongue does it have a quicker on set?

Thanks
Click to expand...

In a word, no.

If they are meant to be taken orally then they won't kick in much faster (not by a significant enough time to make it worth it) then they would if taken orally. If they were made for sublingual use then yes they will kick in faster. That's why there are tablets and sublingual wafers/tablets. If you parachute them, they will kick in a bit faster.
 
Kokaino can you give me a reasoning and a source for you posting something that goes against everything I've ever read or experienced and also been told by my psychiatrist.

I was instructed that if I was having a panic attack to dissolve my xanax sublingually because it would have a much shorter onset of action.

A professor os Psychiatry and psychopharmacology told me this.

I have take many many grams of numerous benzos through all ROAs and IME sublingual will always kick in faster than oral.
 
Tripman said:
Kokaino can you give me a reasoning and a source for you posting something that goes against everything I've ever read or experienced and also been told by my psychiatrist.

I was instructed that if I was having a panic attack to dissolve my xanax sublingually because it would have a much shorter onset of action.

A professor os Psychiatry and psychopharmacology told me this.

I have take many many grams of numerous benzos through all ROAs and IME sublingual will always kick in faster than oral.
Click to expand...

I didn't say that it wouldn't kick in faster, I said it wouldn't kick in faster enough as opposed to swallowing it. It is a tablet meant for oral use, correct? If tablets for oral use can be used sublingually exactly like a sublingual wafer/tablet, than there would be no need to make wafers or sublingual tablets. Sublingual wafers or sublingual tablets kick in faster, pills/tablets don't get absorbed sublingually exactly the way wafers do. It still requires time for the pill to dissolve, then it takes time to be "absorbed" (some will inevitably be swallowed) before the effects begin to work. With a wafer, it is almost instantaneously dissolved and absorbed all within 2-4 minutes. Parachuting a pill would be a quicker way.

So yes, taking your pill sublingually will kick in somewhat quicker or not at all for some people than just taking it the way it was meant to be taken: orally. Not saying you are wrong or lying. But real wafers/sublingual tablets are the real deal here, they kick in at least 3x quicker than a regular tablet.

That's just common sense, you don't need a study for that.
 
I grind mine up into a very fine powder for SL administration, and it dissolves far quicker than a sublingual suboxone tablet.

Yes obviously i understand wafers and SL tablets obviously work better via this ROA but parachuting is not going to absorb faster than sublingual in this manner.

My Psychiatry professor and I discussed it in length.
 
What about sublingual buprenorphine kokaino? That's a pill which absorbs well and fast via that ROA. What is different about that?

Crushing it up is good as you want a decent surface area for absorption, but there is a rich blood supply under the tongue and you don't need a specifically designed sublingual prep to use that. Drug companies will produce them, as then they have a new product and a new patent, but extrapolating that to say sublingual pills won't work because they aren't designed to be used that way is not good logic IMO..

Pills also often work better plugged, but they aren't specifically designed for rectal administration.

Oral is always going to take a little while to kick in as you need to swallow the pill, it move down your oesophagus into your stomach, be broken down and absorbed. It is then shunted past the liver. Sublingual is straight to the blood stream and misses the portal route and first pass metabolism.
 
At least midazolam has been shown to be more effective sublingually. Can't find studies on other benzos.

http://www.springerlink.com/content/7v28822313p42559/
Purpose: This study compared the sedative effects of sublingual tablet midazolam (Roche Dormicum 7.5 mg) with the oral route as premeditation.

Methods: One hundred ASA physical status I and II gynaecolc~ical patients were randomly selected to receive a 7.5 mg tablet of midazolam either sublingually or orally as premedication about one hour before elective surgery. There were 50 patients in each group. The degree of sedation was assessed according to the Ramsay scale initially and then at 20, 30, 45 and 60 min intervals by a second observer bhnded to the route of administration. The time for complete drug dissolution was studied in the sublingual group by the inspection of tablet residue under the tongue every five minutes for 20 min, then the patients were interviewed regarding their acceptance of the taste.

Results: The sedation scores in the sublingual group were higher than in the oral group at 30 and 60 min after drug administration. (P=0.0054 and P=0.008 ) Seventy-two percent of the sublingual group had complete drug dissolution within I 0 min and 64% of the patients in the sublingual group found the tablet acceptable with regard to its taste.

Conclusion: Midazolam 7.5 mg sublingual is a more effective pre-anaesthetic sedative than by the oral route.
Click to expand...
 
Tripman, I'm not being arrogant or anything but some of us here know more about the drugs we use than our doctors and psychiatrists. You're 21, I'm 28. I have been using/abusing benzos the better half of my life. When you were probably in the 1st or 2nd grade, I was already using two to three 30 mg temazepam capsules along with about 15-20 mg of hydrocodone when I was 16 years old. I've tried about 15 DIFFERENT benzos and I know from experience that putting a drug under your tongue that's meant to be swallowed is not going to work the same for every benzo or for every individual. Most of our "doctors" don't even know the benzos I mention to them or request of them. They immediately go to their big pharmacopeia and look it up.
 
effie said:
What about sublingual buprenorphine kokaino? That's a pill which absorbs well and fast via that ROA. What is different about that?

Crushing it up is good as you want a decent surface area for absorption, but there is a rich blood supply under the tongue and you don't need a specifically designed sublingual prep to use that. Drug companies will produce them, as then they have a new product and a new patent, but extrapolating that to say sublingual pills won't work because they aren't designed to be used that way is not good logic IMO..

Pills also often work better plugged, but they aren't specifically designed for rectal administration.

Oral is always going to take a little while to kick in as you need to swallow the pill, it move down your oesophagus into your stomach, be broken down and absorbed. It is then shunted past the liver. Sublingual is straight to the blood stream and misses the portal route and first pass metabolism.
Click to expand...

Using rectally has more to do with increasing the BA of a particular drug and the quick onset comes along with that. Of course liquid solutions will have a quicker onset.

However, taking a pill meant to be taken orally sublingually will not have a significant increase in time of onset. Not for everyone and not for all benzos.

I don't know, maybe I've just live a little - but its not at simple as Tripman makes it out to be.
 
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