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Increasing bioavailability of benzo's
#1
Since clinical bioavailability studies of benzo's are notoriously inaccurate, the question becomes a more subjective one. It's not really a "one size fits all" thing. I have had the privilege, through my work, of observing the effects of Alp on upwards of 1400 clients (spanning 3 decades). I am also seen it used by friends and family members and I, myself, have been using it for decades for PD and GAD. Since I am smartly not allowed to mention some of the ROA that I have seen used, I will not. I can tell you this, though. I have found that the number one way to increase bioavailability is to take it on an empty stomach. As everyone knows, protein's in the circulatory system compete with benzo's for passage by the blood brain barrier into the brain. When there is nothing else to compete with, the impact is like night and day over someone who has taken them with food. Same could be said of opioids, IMO. Empty stomach not available? Then sub-L would be the go. Every formulation of ALP that I have ever encountered has been lipid-soluble, which means that it will do nicely under the tongue. It's not perfect, as salivary secretions will be begin to break it down if you dawdle, but it sure beats swallowing it on a full stomach. In sum, I believe that an empty stomach trumps an unconventional ROA and also trumps any other substance (Tagamet, grapefruit juice, etc) designed to potentiate benzo's. Just my opinion, though. Your experiences?
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#2
I do agree that any substance will be stronger when taken on an empty stomach, and sublingual should be a bit stronger than swallowing. Some brands of etizolam come in a mouth-dissolving form specifically for sublingual use.
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#3
(10-25-2017, 10:53 AM)invisiblejungle Wrote: I do agree that any substance will be stronger when taken on an empty stomach, and sublingual should be a bit stronger than swallowing. Some brands of etizolam come in a mouth-dissolving form specifically for sublingual use.

If you can afford it or your insurance will cover it, both clonazepam and alprazolam and others come in orally disentgrating tabs from the pharmacy. The Dr will write a script for that no problem if he's already writing the benzo for you. It's just a matter of insurance covering it.
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#4
I take Ativan under my tongue and Saphris which a sublingual tablet for bipolar.
Disabled Veteran.Heavily medicated for your safety Blush
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#5
(10-25-2017, 03:24 PM)cajunbulldog38 Wrote: I take Ativan under my tongue and Saphris which a sublingual tablet for bipolar.

Hey Cajun,
Is the Ativan you take the sublingual tab, or is the thing that looks like a breath strip? My wife used to swear by those breath strip type, but I think they have been discontinued. Have you ever used them? Find any difference between that and the sublingual tab? Just wondering. Thanks  RM
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#6
With certain meds, it is recommended that it be taken with a meal, such as fenofibrate which I take for blood trygliceride, (pardon spelling) levels. It can cause liver issues and I think that with a meal it is not such a punch too the liver? As for the clonazepam I take most mornings, I take it under the tongue and regardless of wether I have eaten or not I feel it in 15 minutes. Some tabs dissolve faster than others. I had carpel tunnel surgery done on both wrist's and the orthopedic surgeons nurse who delivers IV sedation, Clonazepam in fact could not make it in due to a snowstorm. He called me first thing in the morning too warn me about it. I told him I had a script for clonazepam and he informed me that, that is what they use. He said put 1mg under my tongue 1/2 hr before I arrived as too bypass the digestive system, so to speak and get it in my bloodstream, making it more "Bio-Available" sooner. I have taken it that way ever since. They say Alp's are so fast acting and maybe some meant to be taken sublingually are? Just me on my high horse telling those of you who overuse Alps, to give the K-Pins a try? Nice to only have too take 1 dose a day! Best Wishes All, and Thanks for the thread Rafterman-FF
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#7
(10-25-2017, 02:35 AM)Rafterman Wrote: Since clinical bioavailability studies of benzo's are notoriously inaccurate, the question becomes a more subjective one. It's not really a "one size fits all" thing. I have had the privilege, through my work, of observing the effects of Alp on upwards of 1400 clients (spanning 3 decades). I am also seen it used by friends and family members and I, myself, have been using it for decades for PD and GAD. Since I am smartly not allowed to mention some of the ROA that I have seen used, I will not. I can tell you this, though. I have found that the number one way to increase bioavailability is to take it on an empty stomach. As everyone knows, protein's in the circulatory system compete with benzo's for passage by the blood brain barrier into the brain. When there is nothing else to compete with, the impact is like night and day over someone who has taken them with food. Same could be said of opioids, IMO. Empty stomach not available? Then sub-L would be the go. Every formulation of ALP that I have ever encountered has been lipid-soluble, which means that it will do nicely under the tongue. It's not perfect, as salivary secretions will be begin to break it down if you dawdle, but it sure beats swallowing it on a full stomach. In sum, I believe that an empty stomach trumps an unconventional ROA and also trumps any other substance (Tagamet, grapefruit juice, etc) designed to potentiate benzo's. Just my opinion, though. Your experiences?

Rafterman - Couldn't agree more.  An empty stomach far surpasses any other means of hastening the action of any benz@.  I do take generic Cimetidine (much cheaper on Amazon than Tagamet, and it is the same medication) with my evening dosage, but that's only because I usually don't have a completely empty stomach at 5PM, having eaten some sort of small snack at 2PM or 3PM.  There's no definitive study I've found that demonstrates Cimetidine is in fact a benz@ potentiator, but even if the effect is psychosomatic, it does seem to produce the calming effect I need more quickly than if I don't take it.

And of course, as we discussed earlier, Sub-L is the only way I take my clono.  Just from personal experience, it's a much better rate of absorption than swallowing.
A tree is known by its fruit; a man by his deeds. A good deed is never lost; he who sows courtesy reaps friendship, and he who plants kindness gathers love.

-- Saint Basil








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#8
(12-05-2017, 02:38 AM)OldBoy Wrote:
(10-25-2017, 02:35 AM)Rafterman Wrote: Since clinical bioavailability studies of benzo's are notoriously inaccurate, the question becomes a more subjective one. It's not really a "one size fits all" thing. I have had the privilege, through my work, of observing the effects of Alp on upwards of 1400 clients (spanning 3 decades). I am also seen it used by friends and family members and I, myself, have been using it for decades for PD and GAD. Since I am smartly not allowed to mention some of the ROA that I have seen used, I will not. I can tell you this, though. I have found that the number one way to increase bioavailability is to take it on an empty stomach. As everyone knows, protein's in the circulatory system compete with benzo's for passage by the blood brain barrier into the brain. When there is nothing else to compete with, the impact is like night and day over someone who has taken them with food. Same could be said of opioids, IMO. Empty stomach not available? Then sub-L would be the go. Every formulation of ALP that I have ever encountered has been lipid-soluble, which means that it will do nicely under the tongue. It's not perfect, as salivary secretions will be begin to break it down if you dawdle, but it sure beats swallowing it on a full stomach. In sum, I believe that an empty stomach trumps an unconventional ROA and also trumps any other substance (Tagamet, grapefruit juice, etc) designed to potentiate benzo's. Just my opinion, though. Your experiences?

Rafterman - Couldn't agree more.  An empty stomach far surpasses any other means of hastening the action of any benz@.  I do take generic Cimetidine (much cheaper on Amazon than Tagamet, and it is the same medication) with my evening dosage, but that's only because I usually don't have a completely empty stomach at 5PM, having eaten some sort of small snack at 2PM or 3PM.  There's no definitive study I've found that demonstrates Cimetidine is in fact a benz@ potentiator, but even if the effect is psychosomatic, it does seem to produce the calming effect I need more quickly than if I don't take it.

And of course, as we discussed earlier, Sub-L is the only way I take my clono.  Just from personal experience, it's a much better rate of absorption than swallowing.

It's interesting that you would bring up Cimetidine, OB, because that seemed to be the winner on all the potentiation threads that I have ever read over the years. It was uncanny how many people believe that it works. I tried it several times and found the same quicker calming effect that you describe, as opposed to when I didn't take it at all. Nice to hear another first hand story about it!
I also got mine from Amazon..another coincidence. Thanks for contributing.  RM
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#9
what i dont get is there some sort of path in the mouth that benzos are absorbed more quickly ? it secrets saliva is there correlation to that,since while taking it under tongue or dissolwing in mouth eventually you still swallow it,empty stomach makes sense on almost any med to kick in faster as theres no food thus it goes straight into processing.

Also while at this topic is there any way to potentiate it or make last longer, since these days seems when under stress i could take twice the dosage but it does little to calm down, thou in many cases noticed that effects kick in later so guess thats because of food.So would be interested to hear more Rafterman.
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#10
(12-05-2017, 06:57 PM)cmdline Wrote: what i dont get is there some sort of path in the mouth that benzos are absorbed more quickly ? it secrets saliva is there correlation to that,since while taking it under tongue or dissolwing in mouth eventually you still swallow it,empty stomach makes sense on almost any med to kick in faster as theres no food thus it goes straight into processing.

Also while at this topic is there any way to potentiate it or make last longer, since these days seems when under stress i could take twice the dosage but it does little to calm down, thou in many cases noticed that effects kick in later so guess thats because of food.So would be interested to hear more Rafterman.

Howdy C,
The underside of the tongue and the inside of the cheek are loaded with capillaries. Any lipid-soluble med can be quickly absorbed into the bloodstream by them, skipping the trip through the digestive tract. That is also why you will feel the effects sooner. I found that it is best to powder the meds first, whenever possible. There is a more complete absorption that way. In my experience, the effects appear stronger when taken sublingually, probably due to two reasons. The first would be that the onset is more distinct. When taken by swallowing, a person usually has to wait between 20-30 minutes to feel anything. By time that rolls around, they are probably off doing something else and not paying attention to the onset of the effects. When you go sublingually, you can usually feel the effects before you have time to move on to somewhere else. The second reason would be that the med is spared the deterioration that would be caused by the digestive system. As for bioavailability, I have tried it all. Cimetidine (Tagamet) is the only thing that even worked marginally for me, with the big exception of an empty stomach. With me, the effects of taking meds on an empty vs full stomach is like night and day. No food for six hours, particularly no protein...as protein is highly competitive with the meds for passage through the blood brain barrier. I know that it is sometimes impossible to be empty before a dose, but if you are feeling that your normal dose isn't making it anymore when you are under stress, I would definitely try for an empty stomach as often as possible. Many people say that an empty stomach is not important if you are taking the meds sublingually, but it is important. Even though the meds will never actually enter your stomach, what you have recently eaten will still compete for passage through the BBB into your brain. Let me know what you think. Thanks  RM
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