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Increasing bioavailability of benzo's
#31
(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?

RM - I just switched from .5 clon 2x day to 2mg @tivan 2x day, both crushed, both Sub-L...But good grief, the @tivan hits more quickly and has no euphoric effect, just calms.  I think I've found my new benz@ - As long as it is boxed and blistered.
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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#32
(01-12-2018, 08:58 PM)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?

RM - I just switched from .5 clon 2x day to 2mg @tivan 2x day, both crushed, both Sub-L...But good grief, the @tivan hits more quickly and has no euphoric effect, just calms.  I think I've found my new benz@ - As long as it is boxed and blistered.

O,
Just to clarify, did you used to get any euphoric effect from the clowns? Or do you find the neither med brought euphoria? Just curious. My sister-in-law has been maintained on @tivan for something like a decade now. Swears by it. She is cool with me and would have easily let me take if for a test drive, but I never made the request. I don't know if I was afraid to stray from my clowns, or if I thought the two meds might potentially be too similar to bother. I think I will try for a day or two in place of the clowns because if what you said. My doc has offered to switch out the clowns for the l-pam a few different times over the years. He actually prefers to latter because he believes they have more of a calming effect. Thanks a lot.  RM
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#33
(01-12-2018, 09:47 PM)Rafterman Wrote:
(01-12-2018, 08:58 PM)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?

RM - I just switched from .5 clon 2x day to 2mg @tivan 2x day, both crushed, both Sub-L...But good grief, the @tivan hits more quickly and has no euphoric effect, just calms.  I think I've found my new benz@ - As long as it is boxed and blistered.

O,
Just to clarify, did you used to get any euphoric effect from the clowns? Or do you find the neither med brought euphoria? Just curious. My sister-in-law has been maintained on @tivan for something like a decade now. Swears by it. She is cool with me and would have easily let me take if for a test drive, but I never made the request. I don't know if I was afraid to stray from my clowns, or if I thought the two meds might potentially be too similar to bother. I think I will try for a day or two in place of the clowns because if what you said. My doc has offered to switch out the clowns for the l-pam a few different times over the years. He actually prefers to latter because he believes they have more of a calming effect. Thanks a lot.  RM

Hi Rafterman, I know what Oldboy means when he refers to the euphoric effects of clonaz. From what I've read, clonaz has serotonergic effects in addition to the core GABAergic effects. I know someone who tapered off clon after 10 years, and one of their main side effects was severe depression, which could be explained by reduced serotonin signaling. I've read accounts of other people who claim that clonaz withdrawal is tougher than withdrawal from other benzos, which would make sense if it's affecting more neurotransmitters.

Alp has dopaminergic effects, which is probably why it's the most-often abused benzo for recreational purposes.

Personally, I want to take benzos simply for the GABAergic effects, not for any euphoria. Loraz definitely feels like more of a pure GABAergic; no euphoria, just as Oldboy says. Same with bromaz and etiz. These are my 3 main benzos.
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#34
(01-12-2018, 10:58 PM)invisiblejungle Wrote: Alp has dopaminergic effects, which is probably why it's the most-often abused benzo for recreational purposes.

Personally, I want to take benzos simply for the GABAergic effects, not for any euphoria. Loraz definitely feels like more of a pure GABAergic; no euphoria, just as Oldboy says. Same with bromaz and etiz. These are my 3 main benzos.

I can personally testify to the dopaminergic effects of Alp, invisible jungle. 
Over a decade ago a Sleep Specialist physician spent many months cycling me through all the benzos of the day to establish which had the most beneficial effect on my Willis-Ekbom Disease (Restless Legs Syndrome).  I remember him saying that the majority ended up settling on Clonaz.
But not for me. ALP was easily way more effective than any & everything else (and I didn't object to the mildly enjoyable ride to sleep either Blush) . 
He explained it away as " Whatever works for you. Everyone's different". 
The ALPs were later withdrawn Sad in favour of the new and wonderfully effective dopamine agonist drugs.
Itinitially prescribed for patients with Parkinsons, once they got out in the field it was discovered they worked amazingly well for people with with Willis-Ekbom/RLS too.
It was only in 2017 that I read about ALP being the only benzo to also exhibit mild D2 & D3 effects - Idea, finally the link with it's effectiveness with RLS was made.

Same Sleep Specialist also ordered my GP to prescribe Zolpidem for me (on an ongoing basis!) for RLS related sleep onset issues.
But after the ALPs...well, you know...10mg Zolpidem is a bit "Ho Hum" as far as I'm concerned  Rolleyes

Perhaps Alp's dopaminergic effects explain why it's the most-often abused benzo for recreational purposes. Undecided
I reckon you'd need to take a truck load of it before you'd get any dopamine reward/ impulse control / gambling / sex crazed effects kicking in.
You'd be GABA comatose way before then, I think.
Still, it'd make for some great dreams!!!! Big Grin....if you were only able to remember them Rolleyes  Big Grin  
R.
There's a difference between having an opinion and having an informed opinion.
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#35
Hi Rafterman. I'm reporting back after 4 weeks of trialing my @lps via SL.

1) Dissolving under my tongue is the now the only way that I will take my med.
    It's my preferred method and I can offer little explanation as to why.
2) Unfortunately, the onset is not as rapid as I had hoped for - still taking around 30 minutes.
    That said, at 30 mins it's the opposite to the usual slow and gentle movement towards calmness, rather it's a global and enveloping, distinctly rich and full delivery of relief.
         
So my n=1 experiment has converted me. SL is the way to go.
Thank you for opening this thread. I will continue to read it with interest.

R.
There's a difference between having an opinion and having an informed opinion.
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#36
(01-29-2018, 01:47 AM)Richardg8092 Wrote: Hi Rafterman. I'm reporting back after 4 weeks of trialing my @lps via SL.

1) Dissolving under my tongue is the now the only way that I will take my med.
    It's my preferred method and I can offer little explanation as to why.
2) Unfortunately, the onset is not as rapid as I had hoped for - still taking around 30 minutes.
    That said, at 30 mins it's the opposite to the usual slow and gentle movement towards calmness, rather it's a global and enveloping, distinctly rich and full delivery of relief.
         
So my n=1 experiment has converted me. SL is the way to go.
Thank you for opening this thread. I will continue to read it with interest.

R.

Thanks, Rich. I appreciate you doing the experiment and for contributing. That is what I was hoping for when I started the thread. Your conclusion is consistent with my experience. I have gone full SL, too, and don't see myself ever going back. Thanks, again. RM
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#37
Always found that if I have a cup of Chamomile tea (or failing that, Lemon Balm tea) shortly after taking the relevant med it tends to heighten benzo effects with regards to sedation in particular. Not by a significant amount mind you, but a definite yet subtle increase in medicinal relief for certain.
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#38
(02-02-2018, 02:38 PM)Glousck Wrote: Always found that if I have a cup of Chamomile tea (or failing that, Lemon Balm tea) shortly after taking the relevant med it tends to heighten benzo effects with regards to sedation in particular.
Chamomile is a gentle herb - some people (like me) love the taste - but I know that others find it really unpleasant . Huh
Those interested in undertaking a Glousck-like experiment with a group of 'less gentle'  Wink  herbs might like to use a Hops, PassionFlower & Valerian combo tea.
  • Hops modulates the melatonin receptor and increases GABA activity.
  • Passionflower modulates GABA/benzodiazepine and opioid receptors.
  • Valerianic acid interacts with GABAa receptors to promote the release of GABA, inhibits the enzymatic breakdown of GABA in the brain.
When brewed as a tea, the effects of the Hops/Passionflower/Valerian combo would be more pronounced than those of Chamomile alone.
However, at best, I'd describe the taste of this combo as 'wretchedly disgusting'.  Sad

A study in 2013 compared NSF-3* (which contains standardized extracts of these 3 herbs) to Z0lpidem (Stilln0x).
It found a significant improvement in total sleep time, sleep latency, number of nightly awakenings and insomnia severity index scores in both groups.
And - Hooray - no statistically significant difference was observed between the groups (basically meaning the herbs were equivalent in effectiveness to Stillnox).
Here's the link.

I'd be pretty confident that the home brewed putrid-tasting tea would only produce sedative effects (and/or enhancement of benz0med effects).
A tea would not produce the hypnotic/sleep inducing effects of the commercially produced standardized extracts in the NSF-3 product.
But for those suffering from insomnia, who find that a large pharmaceutical dose leaves them groggy the next morning, perhaps it's worth trying a moderate dose of meds swilled down with a cup of mother-earth's herbals.

*The NSF-3 product is manufactured in India; but you'll find an equivalent formula at the local Health Food or On-line store, or even in a larger Pharmacy.
A worthy product will have a label listing the ingredients and stating '...extract equivalent to dry herb standardised to contain..... '.  
Products that simply state "contains 500mg of X" are best left on the shelf.
There's a difference between having an opinion and having an informed opinion.
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#39
Yes, thanks RM!

I'm going to look in to this Cimetidine that keeps coming up.
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#40
RM - Thought you might find this interesting:


Quote:Abstract

Cimetidine has been shown to inhibit the liver microsomal metabolism of the benzodiazepines diazepam and chlordiazepoxide, resulting in an increase in half-life and decrease in the clearance of these two drugs. Patients receiving the combination of diazepam and cimetidine have been noted to be more sedated than when given an equal dose of diazepam alone. Many benzodiazepines undergo N-dealkylation and hydroxylation via the cytochrome P450 oxidase system. Cimetidine is thought to bind to cytochrome P450 oxidase and to interfere with many drugs using this path way. Oxazepam and lorazepam are two benzodiazepines not oxidatively metabolized by cytochrome P450, but are glucuronidated by glucuronyl transferase and are, therefore, not subject to metabolic inhibition by cimetidine. Thus, when clinically indicated, oxazepam and lorazepam may be the benzodiazepines of choice to use in combination with cimetidine to eliminate the clinically significant drug interaction seen with diazepam and chlordiazepoxide.

Link: xxxxx://www.ncbi.nlm.nih.gov/pubmed/6116285 (replace xxxxx with https, of course.
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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