Baclofen Potency

[hangingoninFL]

Baclofen Potency

Maybe I misunderstood one of the earlier posts, but I had thought Dr. Levin was referring to some of the other off-brands manufactured in India such as fexobac,bacmax or pacifen. Even though some of the Lioresal may be manufactured in India, it is still made by Novartis so I would think the chemical composition would be the same as it would be if manufactured in the US.

But, if anyone thinks I am wrong about this, please feel free to enlighten me, I am still new to all this!

[gratitude]

Baclofen Potency

resurrection of this thread. my apologies if this has already been figured out or discussed ad nauseam.
has anyone done a " I reached the switch and this is the brand of bac I used?" thread?this might be enlightening.
also, you guys seem to know alot about the chemistry of bac. can anyone comment on the difference of bac and L-bac?
I am doing some personal research on tinnitus cures for myself. I suffer from this as well as alcoholism. it seems that this is one of the SE's on bac but I've read that bac can have the opposite effect and lessen tinnitus.
I am not currently taking bac. I told myself I would have 5 years sobriety before I would try it. coming up on 4 years and doing alot of research. you might wonder why with 5 years of sobriety I would even try it? well, I still cannot go out with friends or to restaurants or bars and not obsess on alcohol. I still sit there with my cran/ soda and feel out place. I've been working on the psych/social aspects of this disease to no avail. anyway, best to you adventurers who are courageous enough to try bac.

[gratitude]

Baclofen Potency

resurrection of this thread. my apologies if this has already been figured out or discussed ad nauseam.
has anyone done a " I reached the switch and this is the brand of bac I used?" thread?this might be enlightening.
also, you guys seem to know alot about the chemistry of bac. can anyone comment on the difference of bac and L-bac?
I am doing some personal research on tinnitus cures for myself. I suffer from this as well as alcoholism. it seems that this is one of the SE's on bac but I've read that bac can have the opposite effect and lessen tinnitus.
I am not currently taking bac. I told myself I would have 5 years sobriety before I would try it. coming up on 4 years and doing alot of research. you might wonder why with 5 years of sobriety I would even try it? well, I still cannot go out with friends or to restaurants or bars and not obsess on alcohol. I still sit there with my cran/ soda and feel out place. I've been working on the psych/social aspects of this disease to no avail. anyway, best to you adventurers who are courageous enough to try bac.

[Ne/Neva Eva]

Baclofen Potency

Gratitude, I can't contribute any information as to the brands or the efficacy of them. I know that's the purpose of your post ... sorry to hijack.
I wonder why you're waiting? 4years of suffering isn't enough?
IMveryHO it doesn't take courage, it takes commitment. And you obviously have no lack of resolve. Try it, you might like it.

[seeking_serenity]

Baclofen Potency

terryk;1000208 wrote: If you're referring to me, it's *a lot of* and *all*

A while back I started a post about baclofen potency (specifically why some brands may work better/feel stronger than others): Baclofen Potency

Basically, I was exploring the idea that all baclofen preparations available are a mixture of two identical (but mirror opposite, and hence different) molecules that behave in the body differently. R-baclofen seems like the one we might most be interested in, and a prodrug that produces only R-baclofen seems like a very big step in the right direction. -tk

Maybe this has been brought up before (my apologies if it has). but I wanted to give you a heads-up they they have developed a drug like you described. It's called STX209, or Arbaclofen, and is being studied as a treatment for autism.

A Drug Shows Promise in Autism* - Technology Review

New Version of an Old Drug Could Treat Autism (and Addiction Too) ? TIME Healthland

Please read these and let me know what you think! :h Thanks, SS

[GeorgeRof]

Baclofen Potency

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[Eber]

Baclofen Potency

This is all definitely really interesting.. I've noticed that many people equate "potency" with the effects, often side effects, that they experience. I wonder if that may be more be an effect of the wrong enatiomer (did I use that correctly?) in the formulation that they're getting..?

My understanding is that the side effects should be pretty limited, mostly drowsiness.. And that's what I've experienced, going up on the dose fairly rapidly. I've gotten the Ivax made stuff thru my local pharmacy throughout.

[terryk]

A significant finding regarding the isolated enantiomers of baclofen - We've known all along that (r)baclofen is the therapeutically active molecule in the commercially available racemic baclofen that is currently prescribed for alcohol addiction (and that (s)baclofen may be responsible for adverse side-effects). This study not only showed that isolated (r)baclofen reduced ethanol consumption in an animal model, but that (s)baclofen actually increased ethanol intake. This is great news if the results translate to human models with medications of isolated (r)baclofen like arbaclofen placarbil.



Alcohol. 2015 Feb;49(1):37-46. doi: 10.1016/j.alcohol.2014.11.005. Epub 2014 Dec 17.
Bidirectional enantioselective effects of the GABAB receptor agonist baclofen in two mouse models of excessive ethanol consumption.
Kasten CR1, Blasingame SN2, Boehm SL 2nd3.

Abstract

The GABAB receptor agonist baclofen has been studied extensively in preclinical models of alcohol-use disorders, yet results on its efficacy have been uncertain. Racemic baclofen, which is used clinically, can be broken down into separate enantiomers of the drug. Baclofen has been shown to produce enantioselective effects in behavioral assays, including those modeling reflexive and sexual behavior. The current studies sought to characterize the enantioselective effects of baclofen in two separate models of ethanol consumption. The first was a Drinking-in-the-Dark procedure that provides "binge-like" ethanol access to mice by restricting access to a 2-h period, 3 h into the dark cycle. The second was a two-bottle choice procedure that utilized selectively bred High Alcohol Preferring 1 (HAP1) mice to model chronic ethanol access. HAP1 mice are selectively bred to consume pharmacologically relevant amounts of ethanol in a 24-h two-bottle choice paradigm. The results showed that baclofen yields enantioselective effects on ethanol intake in both models, and that these effects are bidirectional. Total ethanol intake was decreased by R(+)-baclofen, while total intake was increased by S(-)-baclofen in the binge-like and chronic drinking models. Whereas overall binge-like saccharin intake was significantly reduced by R(+)-baclofen, chronic intake was not significantly altered. S(-)-baclofen did not significantly alter saccharin intake. Neither enantiomer significantly affected locomotion during binge-like reinforcer consumption. Collectively, these results demonstrate that baclofen produces enantioselective effects on ethanol consumption. More importantly, the modulation of consumption is bidirectional. The opposing enantioselective effects may explain some of the variance seen in published baclofen literature.

Copyright ?? 2015 Elsevier Inc. All rights reserved.

-tk

[Ne/Neva Eva]

Thanks for explaining that, Tk. It's written in Ancient Greek.

How far along the pipeline is arbaclofen? Do we know?

[terryk]

It's got a way to go. As Otter said in another thread, Reckitt Benckiser is conducting clinical trials right now. Here's one:

A Dose-Escalation Study to Determine the Maximum Tolerated Dose of Arbaclofen Placarbil in Subjects With Alcohol Use Disorder

-tk

[Ne/Neva Eva]

So that's a Phase 2 trial. I googled and it looks like there's a Phase 3, then it's marketed (and presumably released to public) and they continue with a Phase 4, which is collecting all the information from the new users.

They expect Phase 2 to be over in December, completed in April 2016. Another 8 months to a year for Phase 3, probably. And then we'll get to try it! Assuming our insurance covers it, since it's bound to be a bajillion dollars. Plus, I like the fact that baclofen is not traditionally used for alcoholism, and our docs do not label us alcoholics, so it's not on our permanent EMRs. (It would be, except we went to rehab LONG before electronic records of any kind. We're that old. Ha.) So maybe we wouldn't take it? We'll see. Plenty of time to debate it.

[knobert]

Hi terryk



I was intrigued with the R and S isomers of baclofen after reading Dr. A's book. If someone else has already noted this I apologize, but in the appendix of his book there is a study with rats and nicotine.

Abstract4: Baclofen antagonizes intravenous self-administration of nicotine in mice and rats.



On page 291 of Dr. A's book it states:



"Furthermore, this effect is sterospecific. R baclofen completely prevented nicotine self-administration at the dose of 0.625mg/kg i.p. whereas

S baclofen was inactive up to the dose of 2.5mg/kg i.p."



If R baclofen pills became available, it would be incredible but I can only imagine what the cost would be. Do you think most of could afford it?



What are your thoughts?



Very curious

Knob:thumbsup:

[knobert]

Also, I just want to add a question.

There are tons and tons of pharmaceutical companies all over the world that supply baclofen and other drugs. Do they manufacture their own bac? Do all of them?

There are suppliers all over the place. Are a lot of these companies just buying from suppliers and then just packaging the meds? I'll put a link below, go check it out. Who is buying this stuff?


Baclofen, Baclofen Suppliers and Manufacturers at Alibaba.com

Here's another for India.

India Baclofen, India Baclofen Manufacturers and Suppliers on Alibaba.com!

Are these pharmaceutical companies that are sending us our bac getting it from places like this? If they are, who knows what we are getting.

What do you know about this?

I appreciate anything you can tell me

Thanks

Knob :thanks:

[terryk]

If R baclofen pills became available, it would be incredible but I can only imagine what the cost would be. Do you think most of could afford it?

What are your thoughts?

Hi Knobert,

Reckitt Benckiser is currently testing a new medication called Arbaclofen Placarbil. It is a prodrug of (R)-Baclofen - you can read about it here and here. If the clinical trials are positive and the drug is eventually approved, it will certainly cost more than generic baclofen. Hopefully, it will offer the same (or higher) efficacy, with a better side-effect profile, and an easier dosing regime.

Also, I just want to add a question.

There are tons and tons of pharmaceutical companies all over the world that supply baclofen and other drugs. Do they manufacture their own bac? Do all of them?

There are suppliers all over the place. Are a lot of these companies just buying from suppliers and then just packaging the meds? I'll put a link below, go check it out. Who is buying this stuff?


Baclofen, Baclofen Suppliers and Manufacturers at Alibaba.com

Here's another for India.

India Baclofen, India Baclofen Manufacturers and Suppliers on Alibaba.com!

Are these pharmaceutical companies that are sending us our bac getting it from places like this? If they are, who knows what we are getting.

What do you know about this?

I appreciate anything you can tell me

Thanks

Knob :thanks:

Baclofen is, indeed, made in pharmaceutical plants around the globe - most of it legitimately manufactured and strictly regulated, and some of it less so.... I have taken baclofen pills that I ordered online that were made in India and Germany, and also ones from a USA FDA regulated pharmacy that have been made in Croatia, Israel, and the US. And if you search for them, you can find find many reports and references on MWO to individuals who have ordered baclofen powder from places like Alibaba to homebrew their own medication, usually in liquid form. I don't have any experience with it, and I don't recommend it for anyone that asks.

-tk

[knobert]

Hi tk



Thanks for posting.

I had already read the study using your link. Thanks for putting it there. If I was in the shape I was in 3 years ago, I would have gladly tried to sign up.



But I still ask, are these pill suppliers like Novartis, etc., could they be buying their product from these suppliers and just pilling it up so to speak?



What do you think?



Very interesting to me



Thanks



Knob :thanks: